Selpercatinib: Drug information

For additional information see "Selpercatinib: Pediatric drug information" and "Selpercatinib: Patient drug information"

For abbreviations, symbols, and age group definitions show table

Brand Names: US

Retevmo

Brand Names: Canada

Retevmo

Pharmacologic Category

Antineoplastic Agent, RET Kinase Inhibitor;
Antineoplastic Agent, Tyrosine Kinase Inhibitor

Dosing: Adult

Dosage guidance:

Safety: Withhold selpercatinib for at least 7 days prior to elective surgery; do not administer for at least 2 weeks following major surgery and until adequate wound healing has occurred. Optimize BP prior to initiating treatment; do not initiate selpercatinib in patients with uncontrolled hypertension. Correct hypokalemia, hypomagnesemia, and hypocalcemia prior to selpercatinib initiation and during treatment. Consider appropriate tumor lysis syndrome prophylaxis (including hydration) as clinically necessary.

Clinical considerations: Select patients for selpercatinib treatment based on the presence of a RET gene fusion (with non-small cell lung cancer, other solid tumors, or thyroid cancer) or based on specific RET gene mutation (medullary thyroid cancer) in tumor specimens.

Non–small cell lung cancer, locally advanced or metastatic, RET fusion positive

Non–small cell lung cancer, locally advanced or metastatic, RET fusion positive :

Patients ≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity (Ref).

Patients <50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

Solid tumors, RET fusion positive

Solid tumors, RET fusion positive:

Patients ≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity (Ref).

Patients <50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

Thyroid cancer, medullary, RET mutant

Thyroid cancer, medullary, RET mutant:

Patients ≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity (Ref).

Patients <50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

Thyroid cancer, RET fusion positive

Thyroid cancer, RET fusion positive:

Patients ≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity (Ref).

Patients <50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

Missed dose: Do not administer a missed dose unless it is >6 hours until next scheduled dose. If vomiting occurs after selpercatinib administration, do not administer an additional dose and continue to the next scheduled time for the next dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Note: Kidney function estimated by Modification of Diet in Renal Disease (MDRD) equation.

eGFR ≥15 mL/minute: No dosage adjustment necessary.

End-stage kidney disease: There are no dosage adjustments provided in the manufacturer's labeling (has not been established).

Dosing: Liver Impairment: Adult

Hepatic impairment at treatment initiation:

Mild (total bilirubin ≤ ULN with AST > ULN or total bilirubin >1 to 1.5 times ULN with any AST) or moderate (total bilirubin >1.5 to 3 times ULN and any AST) impairment: No initial dosage adjustment necessary. Monitor for adverse reactions.

Severe impairment (total bilirubin >3 to 10 times ULN and any AST): Current dose of 120 mg twice daily or 160 mg twice daily: Reduce dose to 80 mg twice daily. Monitor for adverse reactions.

Hepatotoxicity during treatment: Grade 3 or 4: Withhold selpercatinib and monitor AST and ALT once weekly until resolves to grade 1 or baseline. Resume selpercatinib with the dose reduced by 2 dose levels; monitor AST and ALT once weekly. After a minimum of 2 weeks without recurrence, increase selpercatinib dose by 1 dose level. Then, after a minimum of 4 weeks without recurrence, increase selpercatinib to dose taken prior to the onset of grade 3 or 4 AST or ALT elevation. Continue monitoring AST and ALT once weekly until 4 weeks after reaching dose taken prior to the onset of grade 3 or 4 AST or ALT elevation.

Dosing: Adjustment for Toxicity: Adult

**Recommended Selpercatinib Dosage Reduction Levels**
Dose reduction	Patients <50 kg	Patients ≥50 kg
Initial (usual) dose	120 mg twice daily	160 mg twice daily
First dose reduction level	80 mg twice daily	120 mg twice daily
Second dose reduction level	40 mg twice daily	80 mg twice daily
Third dose reduction level	40 mg once daily	40 mg twice daily
Permanently discontinue selpercatinib if unable to tolerate 3 dose reductions.

**Selpercatinib Dosage Adjustment for Toxicities**
Toxicity	Severity	Selpercatinib dose modification
Hemorrhagic events	Grade 3 or 4	Withhold selpercatinib until recovery to baseline or grade 0 or 1. Permanently discontinue selpercatinib for severe or life-threatening hemorrhagic events.
Hypersensitivity reactions	All grades	Withhold selpercatinib until resolution of the hypersensitivity event. Initiate corticosteroids (at a dose of 1 mg/kg prednisone [or equivalent]). Resume selpercatinib with the dose reduced by 3 dose levels while continuing corticosteroids. Increase dose by 1 dose level each week until achieving the dose administered prior to the onset of hypersensitivity, then taper corticosteroids.
Hypersensitivity reactions	Recurrent hypersensitivity	Permanently discontinue selpercatinib.
Hypertension	Grade 3	Initiate or optimize hypertensive therapy. Withhold selpercatinib for grade 3 hypertension that persists despite management with optimal antihypertensive therapy. Resume selpercatinib at a reduced dose when hypertension is controlled.
Hypertension	Grade 4	Discontinue selpercatinib.
Hypothyroidism	Grade 3 or 4	Withhold selpercatinib until resolution to grade 1 or baseline. Discontinue selpercatinib based on severity. Manage with thyroid hormone replacement therapy as clinically appropriate.
Pulmonary toxicity (interstitial lung disease [ILD]/pneumonitis)	Grade 2	Withhold selpercatinib until resolution, then resume at a reduced dose. Discontinue selpercatinib permanently for recurrent ILD/pneumonitis.
	Grade 3 or 4	Discontinue selpercatinib permanently for confirmed ILD/pneumonitis.
QT interval prolongation	Grade 3	Withhold selpercatinib until recovery to baseline or grade 0 or 1, then resume selpercatinib at a reduced dose or permanently discontinue selpercatinib.
QT interval prolongation	Grade 4	Discontinue selpercatinib.
Other adverse reactions	Grade 3 or 4	Withhold selpercatinib until recovery to baseline or grade 0 or 1, then resume selpercatinib at a reduced dose.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Selpercatinib: Pediatric drug information")

Dosage guidance:

Clinical considerations: Select patients for selpercatinib treatment based on the presence of a rearranged during transfection (RET) gene fusion (thyroid cancer or solid tumors) or based on specific RET gene mutation (medullary thyroid cancer) in tumor specimens or plasma.

Solid tumors, RET fusion positive

Solid tumors, RET fusion positive:

Children 2 to <12 years: Note: Dosing based on body surface area:

<0.33 m²: Use not recommended.

0.33 to 0.65 m²: Oral: 40 mg three times daily until disease progression or unacceptable toxicity.

0.66 to 1.08 m²: Oral: 80 mg twice daily until disease progression or unacceptable toxicity.

1.09 to 1.52 m²: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

≥1.53 m²: Oral: 160 mg twice daily until disease progression or unacceptable toxicity.

Children ≥12 years and Adolescents: Note: Dosing based on body weight:

<50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity.

Thyroid cancer, medullary, RET mutant

Thyroid cancer, medullary, RET mutant:

Children 2 to <12 years: Note: Dosing based on body surface area:

<0.33 m²: Use not recommended.

0.33 to 0.65 m²: Oral: 40 mg three times daily until disease progression or unacceptable toxicity.

0.66 to 1.08 m²: Oral: 80 mg twice daily until disease progression or unacceptable toxicity.

1.09 to 1.52 m²: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

≥1.53 m²: Oral: 160 mg twice daily until disease progression or unacceptable toxicity.

Children ≥12 years and Adolescents: Note: Dosing based on body weight:

<50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity.

Thyroid cancer, RET fusion positive

Thyroid cancer, RET fusion positive:

Children 2 to <12 years: Note: Dosing based on body surface area:

<0.33 m²: Use not recommended.

0.33 to 0.65 m²: Oral: 40 mg three times daily until disease progression or unacceptable toxicity.

0.66 to 1.08 m²: Oral: 80 mg twice daily until disease progression or unacceptable toxicity.

1.09 to 1.52 m²: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

≥1.53 m²: Oral: 160 mg twice daily until disease progression or unacceptable toxicity.

Children ≥12 years and Adolescents: Note: Dosing based on body weight:

<50 kg: Oral: 120 mg twice daily until disease progression or unacceptable toxicity.

≥50 kg: Oral: 160 mg twice daily until disease progression or unacceptable toxicity.

Dosing adjustment for toxicity:

Children ≥2 years and Adolescents: Oral:

Recommended Selpercatinib Dosage Reduction Levels
Dose reduction level
Initial dosage	40 mg three times daily	80 mg twice daily	120 mg twice daily	160 mg twice daily
First dose reduction level	40 mg twice daily	40 mg twice daily	80 mg twice daily	120 mg twice daily
Second dose reduction level	40 mg once daily	40 mg once daily	40 mg twice daily	80 mg twice daily
Third dose reduction level	Permanently discontinue	Permanently discontinue	40 mg once daily	40 mg twice daily
			Permanently discontinue in patients unable to tolerate 3 dose reductions.

Dose modifications for toxicities:

Toxicity	Severity	Selpercatinib dose modification
Hemorrhagic events	Grade 3 or 4	Withhold selpercatinib until recovery to baseline or grade 0 or 1. Discontinue selpercatinib (permanently) for severe or life-threatening hemorrhagic events.
Hypersensitivity reactions	All grades	Withhold selpercatinib and initiate corticosteroids (at a dose of 1 mg/kg prednisone [or equivalent]). After resolution, resume selpercatinib with the dose reduced by 3 dose levels while continuing corticosteroids. Increase dose by 1 dose level each week until achieving the dose administered prior to the onset of hypersensitivity, then taper corticosteroids.
Hypersensitivity reactions	Recurrent hypersensitivity	Permanently discontinue selpercatinib.
Hypertension	Grade 3	Initiate or optimize hypertensive therapy. Withhold selpercatinib for grade 3 hypertension that persists despite management with optimal antihypertensive therapy. Resume selpercatinib at a reduced dose when hypertension is controlled.
Hypertension	Grade 4	Discontinue selpercatinib.
Hypothyroidism	Grade 3 or 4	Withhold selpercatinib until resolution to grade 1 or baseline. Permanently discontinue selpercatinib based on severity. Manage with thyroid hormone replacement therapy as clinically appropriate.
Pulmonary toxicity (interstitial lung disease [ILD]/pneumonitis)	Grade 2	Withhold selpercatinib until resolution, then resume at a reduced dose. Discontinue selpercatinib permanently for recurrent ILD/pneumonitis.
	Grade 3 or 4	Discontinue selpercatinib permanently for confirmed ILD/pneumonitis.
QT interval prolongation	Grade 3	Withhold selpercatinib until recovery to baseline or grade 0 or 1, then resume selpercatinib at a reduced dose or permanently discontinue.
QT interval prolongation	Grade 4	Discontinue selpercatinib.
Other adverse reactions	Grade 3 or 4	Withhold selpercatinib until recovery to baseline or grade 0 or 1, then resume selpercatinib at a reduced dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Altered kidney function:

Note: Kidney function estimated by Modification of Diet in Renal Disease (MDRD) equation.

Children ≥2 years and Adolescents: Oral:

Mild to severe impairment (eGFR ≥15 mL/minute): No dosage adjustment recommended.

End-stage renal disease: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Liver Impairment: Pediatric

Children ≥2 years and Adolescents: Oral:

Hepatic impairment at treatment initiation:

Mild impairment (total bilirubin ≤ ULN with AST > ULN or total bilirubin >1 to 1.5 times ULN with any AST): No initial dosage adjustment necessary. Monitor for adverse reactions.

Moderate impairment (total bilirubin >1.5 to 3 times ULN with any AST): No initial dosage adjustment necessary. Monitor for adverse reactions.

Severe impairment (bilirubin >3 to 10 times ULN with any AST):

For initial dose of 40 mg three times daily or 80 mg twice daily: Reduce dose to 40 mg twice daily. Monitor for adverse reactions.

For initial dose of 120 mg twice daily or 160 mg twice daily: Reduce dose to 80 mg twice daily. Monitor for adverse reactions.

Hepatotoxicity during treatment: Grade 3 or 4: Withhold selpercatinib and monitor AST and ALT once weekly. When AST/ALT return to grade 1 or baseline, resume at dose reduced by 2 dose levels; monitor AST and ALT once weekly. After a minimum of 2 weeks without recurrence, increase selpercatinib dose by 1 dose level. Then after a minimum of 4 weeks without recurrence, increase selpercatinib to dose taken prior to onset of grade 3 or 4 AST or ALT elevation. Continue monitoring AST and ALT once weekly until 4 weeks after reaching dose taken prior to the onset of grade 3 or 4 AST or ALT elevation. See recommended selpercatinib dosage reduction levels in "Dosing Adjustment for Toxicity."

Adverse Reactions (Significant): Considerations

Hemorrhage

Selpercatinib may cause grade ≥3 hemorrhage; serious and fatal hemorrhagic events have occurred, including cerebral hemorrhage, tracheostomy site hemorrhage, and hemoptysis.

Hepatotoxicity

Selpercatinib may cause hepatotoxicity, including increased serum alanine aminotransferase (ALT), increased serum alkaline phosphatase, and increased serum aspartate aminotransferase (AST) (Ref). Hepatoxicity may require dosage interruption, reduction, and/or discontinuation.

Onset: Varied; median time to first onset of elevated ALT was 5.8 weeks (range: 1 day to 2.5 years) and AST was 6 weeks (range: 1 day to 3.4 years) in clinical trials.

Risk factors:

• Preexisting severe hepatic impairment

Hypersensitivity reactions

Hypersensitivity reactions have occurred (including grade 3 events); reactions include fever, skin rash, and arthralgias or myalgias with concurrent hypotension, thrombocytopenia, or transaminitis (Ref).

Mechanism: Not clearly established; immunologic (Ref).

Onset: Varied; median time to onset was 1.4 weeks (range: 5 days to 2 years) (Ref).

Risk factors:

• Previous treatment with immune checkpoint inhibitor therapy (Ref)

Hypertension

Hypertension may occur, including grade 3 and grade 4 events (Ref); some patients may require dose interruption, dose reduction, and/or anti-hypertensive treatment.

Risk factors:

• Preexisting uncontrolled hypertension

Pulmonary toxicity

Severe or life-threatening interstitial lung disease (ILD)/pneumonitis may occur with selpercatinib; grade 3 or 4 events and fatal cases have been reported (Ref).

QT prolongation

Selpercatinib may cause concentration dependent prolonged QT interval on ECG with observed increases in QTcF interval to >500 msec and increases in the QTcF interval of at least 60 msec over baseline; some patients require dose interruption or reduction.

Mechanism: Dose-related (concentration dependent); exact mechanism is unknown.

Onset: Varied; effect is concentration-dependent; therefore, timing may be impacted by high doses or accumulation.

Risk factors:

In general, risk factors for drug-induced QT prolongation include (Ref):

• Females

• Age >65 years

• Structural heart disease (eg, history of myocardial infarction or heart failure with reduced ejection fraction)

• Genetic defects of cardiac ion channels

• History of drug-induced torsades de pointes

• Congenital long QT syndrome

• Baseline QTc interval prolongation (eg, >500 msec) or lengthening of the QTc by ≥60 msec

• Electrolyte disturbances (eg, hypocalcemia, hypokalemia, or hypomagnesemia)

• Bradycardia

• Hepatic impairment

• Kidney impairment

• Loop diuretic use

• Sepsis

• Concurrent use of strong and moderate CYP3A inhibitors

• Concurrent administration of multiple medications (≥2) that prolong the QT interval or drug interactions that increase serum drug concentrations of QT-prolonging medications

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adolescents and adults, unless otherwise specified.

>10%:

Cardiovascular: Edema (41% to 49%), hypertension (41% to 48%), prolonged QT interval on ECG (20% to 21%)

Dermatologic: Skin rash (33%)

Endocrine & metabolic: Decreased serum albumin (25% to 56%), decreased serum calcium (53% to 59%), decreased serum glucose (34%), decreased serum magnesium (16% to 33%), decreased serum potassium (adults: 17%), decreased serum sodium (31% to 42%), hypercholesterolemia (35%), hypothyroidism (9% to 13%), increased serum glucose (53%), increased serum potassium (34%)

Gastrointestinal: Abdominal pain (25% to 34%), constipation (22% to 33%), decreased appetite (adults: 17%), diarrhea (44% to 47%; grade 3: 1% to 5%), nausea (13% to 31%; grade 3: 1%), stomatitis (adults: 18%), vomiting (13% to 22%; grade 3: 2%), xerostomia (39% to 43%)

Genitourinary: Urinary tract infection (adults: 12%)

Hematologic & oncologic: Decreased hemoglobin (21% to 28%; grades 3/4: 4%), decreased neutrophils (25% to 53%; grades 3/4: 2% to 3%), decreased platelet count (37% to 53%; grades 3/4: 3%), hemorrhage (13% to 22%; grades 3/4: 3%), lymphocytopenia (52% to 53%; grades 3/4: 8% to 20%)

Hepatic: Increased serum alanine aminotransferase (56% to 81%), increased serum alkaline phosphatase (35% to 40%), increased serum aspartate aminotransferase (59% to 77%), increased serum bilirubin (30% to 52%)

Nervous system: Fatigue (32% to 46%), headache (14% to 28%)

Neuromuscular & skeletal: Arthralgia (21%), musculoskeletal pain (adults: 25%)

Renal: Increased serum creatinine (23% to 47%)

Respiratory: Cough (24%), dyspnea (22%), pneumonia (9% to 11%)

Miscellaneous: Fever (adults: 13%)

1% to 10%:

Hematologic & oncologic: Tumor lysis syndrome (<2%)

Hepatic: Ascites (adults: chylous: <2%), hepatotoxicity (3%)

Hypersensitivity: Hypersensitivity reaction (≤6%)

Nervous system: Dizziness (adults: 8%)

Respiratory: Interstitial lung disease (≤4%), pleural disease (adults: chylothorax: <2%), pleural effusion (≥2%), pneumonitis (≤4%)

<1%: Neuromuscular & skeletal: Slipped capital femoral epiphysis (adolescents)

Frequency not defined:

Cardiovascular: Acute myocardial infarction (adults)

Infection: Sepsis

Contraindications

There are no contraindications listed in the manufacturer's US labeling.

Canadian labeling: Hypersensitivity to selpercatinib or any component of the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Tumor lysis syndrome: Tumor lysis syndrome (TLS) has been reported rarely when used for the treatment of medullary thyroid carcinoma. Risk factors for TLS include rapidly proliferating tumors, a high tumor burden, kidney dysfunction, and dehydration.

Disease-related concerns:

• Kidney function: Elevations in serum creatinine were noted after 10 days (in healthy patients). If persistent serum creatinine elevations are observed, consider alternative markers for kidney function evaluation.

Special populations:

• Pediatric patients: Cases of slipped capital femoral epiphysis/slipped upper femoral epiphysis have been reported in adolescents who received selpercatinib.

Other warnings/precautions:

• RET gene status: Select patients for selpercatinib treatment based on the presence of a RET gene fusion (with non-small cell lung cancer, other solid tumors, or thyroid cancer) or based on specific RET gene mutation (medullary thyroid cancer) in tumor specimens. Information on approved test(s) for the detection of RET gene fusions and mutations is available at https://www.fda.gov/CompanionDiagnostics.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule, Oral:

Retevmo: 40 mg [DSC]

Retevmo: 80 mg [DSC] [contains fd&c blue #1 (brilliant blue)]

Tablet, Oral:

Retevmo: 40 mg, 80 mg, 120 mg, 160 mg

Generic Equivalent Available: US

Pricing: US

Tablets (Retevmo Oral)

40 mg (per each): $158.18

80 mg (per each): $237.27

120 mg (per each): $474.55

160 mg (per each): $474.55

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Retevmo: 40 mg

Retevmo: 80 mg [contains fd&c blue #1 (brilliant blue)]

Administration: Adult

Oral: May administer with or without food (unless coadministered with a proton pump inhibitor [PPI]). Swallow whole; do not crush or chew.

Administration with acid-reducing agents: Avoid concomitant use of a PPI, a histamine-2 (H₂) receptor antagonist, or a locally-acting antacid with selpercatinib. If concomitant use cannot be avoided, administer selpercatinib with food when coadministered with a PPI; administer selpercatinib 2 hours before or 10 hours after administration of an H₂ receptor antagonist; administer selpercatinib 2 hours before or 2 hours after administration of a locally acting antacid.

Administration: Pediatric

Oral: May administer with or without food (unless administered with a proton pump inhibitor [PPI]). Swallow whole; do not crush or chew. If vomiting occurs after administration, do not take an additional dose; continue to the next scheduled dose.

Administration with acid-reducing agents: Avoid concomitant use of a PPI, a histamine-2 (H₂) receptor antagonist, or a locally-acting antacid with selpercatinib. If concomitant use cannot be avoided, administer selpercatinib with food when coadministered with a PPI; administer selpercatinib 2 hours before or 10 hours after administration of an H₂ receptor antagonist; administer selpercatinib 2 hours before or 2 hours after administration of a locally-acting antacid.

Missed dose: Do not take a missed dose unless it is more than 6 hours until next scheduled dose.

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2024) list; however, it may meet the criteria for a hazardous drug. Selpercatinib may cause reproductive toxicity and teratogenicity.

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Non–small cell lung cancer, locally advanced or metastatic, RET fusion positive: Treatment of locally advanced or metastatic non–small cell lung cancer (NSCLC) in adults with a rearranged during transfection (RET) gene fusion, as detected by an approved test.

Solid tumors, RET fusion positive: Treatment of locally advanced or metastatic solid tumors with a RET gene fusion, as detected by an approved test, in adults and pediatric patients ≥2 years of age with progression on or following prior systemic treatment or who have no satisfactory alternative treatment options.

Thyroid cancer, medullary, RET mutant: Treatment of advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an approved test, in adults and pediatric patients ≥2 years of age who require systemic therapy.

Thyroid cancer, RET fusion positive: Treatment of advanced or metastatic thyroid cancer with a RET gene fusion, as detected by an approved test, in adults and pediatric patients ≥2 years of age who require systemic therapy and who are refractory to radioactive iodine (if radioactive iodine is appropriate).

Medication Safety Issues

Sound-alike/look-alike issues:

Retevmo may be confused with Retrovir.

Selpercatinib may be confused with pralsetinib, selinexor, selumetinib, sunitinib, tucatinib.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).

Metabolism/Transport Effects

Substrate of BCRP, CYP3A4 (Major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP, CYP2C8 (Moderate), CYP3A4 (Weak), P-glycoprotein;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Afatinib. Management: If combined, administer the P-gp inhibitor simultaneously with, or after, the dose of afatinib. Monitor closely for signs and symptoms of afatinib toxicity and if the combination is not tolerated, reduce the afatinib dose by 10 mg. Risk D: Consider Therapy Modification

Aliskiren: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Aliskiren. Risk C: Monitor

Alpelisib: BCRP/ABCG2 Inhibitors may increase serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Risk D: Consider Therapy Modification

ALPRAZolam: CYP3A4 Inhibitors (Weak) may increase serum concentration of ALPRAZolam. Risk C: Monitor

Amiodarone: QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of Amiodarone. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Amisulpride (Oral): QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Amisulpride (Oral). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even greater risk. Risk D: Consider Therapy Modification

Amodiaquine: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Amodiaquine. Risk X: Avoid

Androgens: Hypertension-Associated Agents may increase hypertensive effects of Androgens. Risk C: Monitor

Antacids: May decrease serum concentration of Selpercatinib. Management: Coadministration of selpercatinib and antacids should be avoided. If coadministration cannot be avoided, selpercatinib should be administered 2 hours before or 2 hours after antacids. Risk D: Consider Therapy Modification

Azithromycin (Systemic): QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Azithromycin (Systemic). Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors): Selpercatinib may increase serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor

Beta-Acetyldigoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Beta-Acetyldigoxin. Risk C: Monitor

Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Bilastine. Risk X: Avoid

Carbetocin: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Celiprolol. Risk C: Monitor

Chloroquine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Chloroquine. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Citalopram: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Citalopram. Risk X: Avoid

Cladribine: BCRP/ABCG2 Inhibitors may increase serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration. Risk D: Consider Therapy Modification

Clarithromycin: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Clarithromycin. Risk X: Avoid

Clofazimine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Clofazimine. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

ClomiPRAMINE: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

CloZAPine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of CloZAPine. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: This combination is often contraindicated, but combined use may be permitted with dose adjustment and monitoring. Recommendations vary based on brand, indication, use of CYP3A4 inhibitors, and hepatic/renal function. See interaction monograph for details. Risk D: Consider Therapy Modification

CycloSPORINE (Systemic): CYP3A4 Inhibitors (Weak) may increase serum concentration of CycloSPORINE (Systemic). Risk C: Monitor

CycloSPORINE (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of CycloSPORINE (Systemic). Risk C: Monitor

CYP3A4 Inducers (Moderate): May decrease serum concentration of Selpercatinib. Risk X: Avoid

CYP3A4 Inducers (Strong): May decrease serum concentration of Selpercatinib. Risk X: Avoid

CYP3A4 Inducers (Weak): May decrease serum concentration of Selpercatinib. Risk C: Monitor

CYP3A4 Inhibitors (Moderate): May increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120 mg twice/day to 80 mg twice/day, or from 160 mg twice/day to 120 mg twice/day. Risk D: Consider Therapy Modification

CYP3A4 Inhibitors (Strong): May increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120 mg twice/day to 40 mg twice/day, or from 160 mg twice/day to 80 mg twice/day. Risk D: Consider Therapy Modification

Dabigatran Etexilate: P-glycoprotein/ABCB1 Inhibitors may increase active metabolite exposure of Dabigatran Etexilate. Risk C: Monitor

Dabrafenib: May increase QTc-prolonging effects of Selpercatinib. Dabrafenib may decrease serum concentration of Selpercatinib. Risk X: Avoid

Daprodustat: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Daprodustat. Management: Reduce the daprodustat starting dose by half if combined with moderate CYP2C8 inhibitors, unless the dose is 1 mg, then no dose adjustment is required. Monitor hemoglobin and adjust daprodustat dose when starting or stopping moderate CYP2C8 inhibitors. Risk D: Consider Therapy Modification

Dasabuvir: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Dasabuvir. Risk C: Monitor

Dasatinib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Dasatinib. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Desloratadine: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Desloratadine. Risk C: Monitor

Digitoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digitoxin. Risk C: Monitor

Digoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digoxin. Management: Measure digoxin serum concentrations before initiating treatment with these P-glycoprotein (P-gp) inhibitors. Reduce digoxin concentrations by either reducing the digoxin dose by 15% to 30% or by modifying the dosing frequency. Risk D: Consider Therapy Modification

Domperidone: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Domperidone. Risk X: Avoid

Doxepin-Containing Products: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Doxepin-Containing Products. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Conventional). Risk X: Avoid

DOXOrubicin (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Liposomal). Risk C: Monitor

Dronedarone: Selpercatinib may increase QTc-prolonging effects of Dronedarone. Dronedarone may increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120mg twice/day to 80mg twice/day, or from 160mg twice/day to 120mg twice/day. Monitor QT interval more closely for QTc interval prolongation and arrhythmias. Risk D: Consider Therapy Modification

DroPERidol: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of DroPERidol. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Edoxaban. Risk C: Monitor

Encorafenib: May increase QTc-prolonging effects of Selpercatinib. Encorafenib may decrease serum concentration of Selpercatinib. Risk X: Avoid

Ensartinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ensartinib. Risk X: Avoid

Entrectinib: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Risk X: Avoid

Escitalopram: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Escitalopram. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Etelcalcetide: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide Phosphate. Risk C: Monitor

Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide. Risk C: Monitor

Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Everolimus. Risk C: Monitor

Fexinidazole: May increase QTc-prolonging effects of Selpercatinib. Fexinidazole may decrease serum concentration of Selpercatinib. Risk X: Avoid

Finerenone: CYP3A4 Inhibitors (Weak) may increase serum concentration of Finerenone. Risk C: Monitor

Fingolimod: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias (including TdP) with a continuous overnight ECG when fingolimod is combined with QT prolonging drugs. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor

Flecainide: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Flecainide. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Flibanserin: CYP3A4 Inhibitors (Weak) may increase serum concentration of Flibanserin. Risk C: Monitor

Fluorouracil Products: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Fluorouracil Products. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Flupentixol: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Flupentixol. Risk X: Avoid

Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification

Gadobenate Dimeglumine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Gadobenate Dimeglumine. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Gemifloxacin: QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of Gemifloxacin. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Gilteritinib: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this combination. If use is necessary, monitor for QTc interval prolongation and arrhythmias. Risk D: Consider Therapy Modification

Glecaprevir and Pibrentasvir: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Glecaprevir and Pibrentasvir. Risk C: Monitor

Grapefruit Juice: May increase serum concentration of Selpercatinib. Management: Avoid consumption of grapefruit juice, a moderate CYP3A4 inhibitor, with selpercatinib whenever possible. Because grapefruit juice consumption is highly variable, typical dose adjustments associated with moderate CYP3A4 inhibitors are not likely feasible. Risk D: Consider Therapy Modification

Halofantrine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Halofantrine. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Haloperidol: QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of Haloperidol. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Histamine H2 Receptor Antagonists: May decrease serum concentration of Selpercatinib. Management: Coadministration of selpercatinib and H2 receptor antagonists should be avoided. If coadministration cannot be avoided, selpercatinib should be administered 2 hours before or 10 hours after H2 receptor antagonists. Risk D: Consider Therapy Modification

HydrOXYzine: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Risk C: Monitor

Imipramine: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Inhibitors of the Proton Pump (PPIs and PCABs): May decrease serum concentration of Selpercatinib. Management: Coadministration of selpercatinib and PPIs or PCABs should be avoided. If coadministration cannot be avoided, selpercatinib and PPIs or PCABs should be administered simultaneously with food. Risk D: Consider Therapy Modification

Inotuzumab Ozogamicin: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Inotuzumab Ozogamicin. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Ixabepilone: CYP3A4 Inhibitors (Weak) may increase serum concentration of Ixabepilone. Risk C: Monitor

Lapatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Lapatinib. Risk C: Monitor

Larotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Larotrectinib. Risk C: Monitor

Lefamulin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets with P-glycoprotein/ABCB1 inhibitors. If concomitant use is required, monitor for lefamulin adverse effects. Risk D: Consider Therapy Modification

Lemborexant: CYP3A4 Inhibitors (Weak) may increase serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Levofloxacin-Containing Products (Systemic): QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of Levofloxacin-Containing Products (Systemic). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Levoketoconazole: QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of Levoketoconazole. Risk X: Avoid

Lofexidine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Lofexidine. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Lomitapide: CYP3A4 Inhibitors (Weak) may increase serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Risk D: Consider Therapy Modification

Lonafarnib: May increase QTc-prolonging effects of Selpercatinib. Lonafarnib may increase serum concentration of Selpercatinib. Management: Avoid this combination if possible. If coadministration is required, reduce selpercatinib from 120 mg twice daily to 40 mg twice daily, or from 160 mg to 80 mg twice daily. Monitor for QT prolongation. Risk D: Consider Therapy Modification

Mavorixafor: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Mavorixafor. Risk C: Monitor

Meglumine Antimoniate: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Methadone: QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of Methadone. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Midazolam: CYP3A4 Inhibitors (Weak) may increase serum concentration of Midazolam. Risk C: Monitor

Midostaurin: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Midostaurin. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Morphine (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Morphine (Systemic). Risk C: Monitor

Moxifloxacin (Systemic): QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Moxifloxacin (Systemic). Risk X: Avoid

Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Nadolol. Risk C: Monitor

Naldemedine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Naldemedine. Risk C: Monitor

Naloxegol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Naloxegol. Risk C: Monitor

Nilotinib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Nilotinib. Risk X: Avoid

NiMODipine: CYP3A4 Inhibitors (Weak) may increase serum concentration of NiMODipine. Risk C: Monitor

OLANZapine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of OLANZapine. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Ondansetron: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Ondansetron. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Osimertinib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Osimertinib. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Oxytocin: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Ozanimod: CYP2C8 Inhibitors (Moderate) may increase active metabolite exposure of Ozanimod. Risk C: Monitor

PACLitaxel (Conventional): CYP2C8 Inhibitors (Moderate) may increase serum concentration of PACLitaxel (Conventional). Risk C: Monitor

PACLitaxel (Protein Bound): CYP2C8 Inhibitors (Moderate) may increase serum concentration of PACLitaxel (Protein Bound). Risk C: Monitor

PAZOPanib: BCRP/ABCG2 Inhibitors may increase serum concentration of PAZOPanib. Risk X: Avoid

PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of PAZOPanib. Risk X: Avoid

PAZOPanib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of PAZOPanib. Risk X: Avoid

Pentamidine (Systemic): QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Pentamidine (Systemic). Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Pilsicainide: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Pilsicainide. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Pimozide: CYP3A4 Inhibitors (Weak) may increase serum concentration of Pimozide. Risk X: Avoid

Pimozide: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Pimozide. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk X: Avoid

Pioglitazone: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Pioglitazone. Risk C: Monitor

Piperaquine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Piperaquine. Risk X: Avoid

Pralsetinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Pralsetinib. Management: If this combo cannot be avoided, decrease pralsetinib dose from 400 mg daily to 300 mg daily; from 300 mg daily to 200 mg daily; and from 200 mg daily to 100 mg daily. Risk D: Consider Therapy Modification

Probucol: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Probucol. Risk X: Avoid

Propafenone: May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

Propofol: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

QT-prolonging Agents (Indeterminate Risk - Avoid): May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor

QT-prolonging Agents (Indeterminate Risk - Caution): May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor

QT-prolonging Class IA Antiarrhythmics (Highest Risk): QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of QT-prolonging Class IA Antiarrhythmics (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

QT-prolonging Class III Antiarrhythmics (Highest Risk): QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of QT-prolonging Class III Antiarrhythmics (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

QT-Prolonging Inhalational Anesthetics (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

QT-prolonging Kinase Inhibitors (Highest Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Highest Risk). Risk X: Avoid

QT-prolonging Miscellaneous Agents (Highest Risk): QT-prolonging Kinase Inhibitors (Highest Risk) may increase QTc-prolonging effects of QT-prolonging Miscellaneous Agents (Highest Risk). Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk): May increase QTc-prolonging effects of Selpercatinib. QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120mg twice/day to 80mg twice/day, or from 160mg twice/day to 120mg twice/day. Monitor QT interval more closely for QTc interval prolongation and arrhythmias. Risk D: Consider Therapy Modification

QT-prolonging Strong CYP3A4 Inhibitors (Highest Risk): May increase QTc-prolonging effects of Selpercatinib. QT-prolonging Strong CYP3A4 Inhibitors (Highest Risk) may increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120mg twice/day to 40mg twice/day, or from 160mg twice/day to 80mg twice/day. Monitor QT interval more closely for QTc interval prolongation and arrhythmias. Risk D: Consider Therapy Modification

QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk): May increase QTc-prolonging effects of Selpercatinib. QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk) may increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120mg twice/day to 40mg twice/day, or from 160mg twice/day to 80mg twice/day. Monitor QT interval more closely for QTc interval prolongation and arrhythmias. Risk D: Consider Therapy Modification

QUEtiapine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of QUEtiapine. Risk X: Avoid

Quizartinib: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Ranolazine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ranolazine. Risk C: Monitor

Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider Therapy Modification

Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider Therapy Modification

Repaglinide: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Repaglinide. Risk C: Monitor

Repotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Repotrectinib. Risk X: Avoid

Resmetirom: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Resmetirom. Management: During coadministration with moderate CYP2C8 inhibitors reduce the resmetirom dose to 80 mg daily for patients weighing 100 kg or more, or reduce the resmetirom dose to 60 mg daily for patients weighing less than 100 kg. Risk D: Consider Therapy Modification

Ribociclib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Ribociclib. Risk X: Avoid

RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RifAXIMin. Risk C: Monitor

Rimegepant: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Rimegepant. Management: Avoid administration of another dose of rimegepant within 48 hours if given concomitantly with a P-glycoprotein (P-gp) inhibitor. Risk D: Consider Therapy Modification

RisperiDONE: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of RisperiDONE. QT-prolonging Agents (Highest Risk) may increase CNS depressant effects of RisperiDONE. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification

RomiDEPsin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RomiDEPsin. Risk C: Monitor

Rosuvastatin: BCRP/ABCG2 Inhibitors may increase serum concentration of Rosuvastatin. Risk C: Monitor

Seladelpar: BCRP/ABCG2 Inhibitors may increase serum concentration of Seladelpar. Risk C: Monitor

Selexipag: CYP2C8 Inhibitors (Moderate) may increase active metabolite exposure of Selexipag. Management: Reduce the selexipag dose to once daily when combined with moderate CYP2C8 inhibitors. Revert back to twice daily selexipag dosing upon stopping the moderate CYP2C8 inhibitor. Risk D: Consider Therapy Modification

Sertindole: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Risk X: Avoid

Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Silodosin. Risk C: Monitor

Simvastatin: CYP3A4 Inhibitors (Weak) may increase serum concentration of Simvastatin. CYP3A4 Inhibitors (Weak) may increase active metabolite exposure of Simvastatin. Risk C: Monitor

Sirolimus (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with P-glycoprotein (P-gp) inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Monitor for increased sirolimus concentrations/toxicity if combined. Risk D: Consider Therapy Modification

Sirolimus (Protein Bound): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Protein Bound). Risk X: Avoid

Solriamfetol: May increase hypertensive effects of Hypertension-Associated Agents. Risk C: Monitor

Sparfloxacin: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Sparfloxacin. Risk X: Avoid

SUNItinib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of SUNItinib. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase serum concentration of Tacrolimus (Systemic). Risk C: Monitor

Tacrolimus (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tacrolimus (Systemic). Risk C: Monitor

Talazoparib: BCRP/ABCG2 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor

Talazoparib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor

Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Teniposide. Risk C: Monitor

Tenofovir Disoproxil Fumarate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor

Terbutaline: May increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Thioridazine: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Thioridazine. Risk X: Avoid

Topotecan: BCRP/ABCG2 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid

Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid

Toremifene: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Toremifene. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Tovorafenib: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Tovorafenib. Risk X: Avoid

Treprostinil: CYP2C8 Inhibitors (Moderate) may increase serum concentration of Treprostinil. Risk C: Monitor

Triazolam: CYP3A4 Inhibitors (Weak) may increase serum concentration of Triazolam. Risk C: Monitor

Ubrogepant: BCRP/ABCG2 Inhibitors may increase serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a BCRP inhibitor. Risk D: Consider Therapy Modification

Ubrogepant: CYP3A4 Inhibitors (Weak) may increase serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (given at least 2 hours later if needed) of ubrogepant should be limited to 50 mg. Risk D: Consider Therapy Modification

Ubrogepant: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a P-gp inhibitor. Risk D: Consider Therapy Modification

Vemurafenib: QT-prolonging Agents (Highest Risk) may increase QTc-prolonging effects of Vemurafenib. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification

Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring concomitant treatment with P-glycoprotein (P-gp) inhibitors. Resume the previous venetoclax dose 2 to 3 days after discontinuation of a P-gp inhibitor. Risk D: Consider Therapy Modification

VinCRIStine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of VinCRIStine. Risk X: Avoid

Reproductive Considerations

Evaluate pregnancy status prior to use in patients who could become pregnant.

Patients who could become pregnant should use effective contraception during therapy and for 1 week after the last selpercatinib dose. Patients with partners who could become pregnant should use effective contraception during therapy and for 1 week after the last selpercatinib dose.

Pregnancy Considerations

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to selpercatinib may cause fetal harm.

Breastfeeding Considerations

It is not known if selpercatinib is present in breast milk.

Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 1 week after the last selpercatinib dose.

Monitoring Parameters

Evaluate RET gene fusion status (non-small cell lung cancer, other solid tumors, or thyroid cancer) or specific RET gene mutation (medullary thyroid cancer) in tumor specimens. Monitor ALT and AST prior to treatment initiation, every 2 weeks during the first 3 months, then monthly thereafter, and as clinically indicated. Assess QT interval, electrolytes, and thyroid-stimulating hormone/thyroid function at baseline and periodically during treatment; adjust monitoring frequency based upon risk factors (including diarrhea); monitor QT interval more frequently in patients with concomitant strong and moderate CYP3A inhibitors or medications known to prolong QTc interval. Monitor for QT interval prolongation in patients at significant risk (known long QT syndromes, clinically significant bradyarrhythmias, severe or uncontrolled heart failure). Evaluate pregnancy status prior to use in patients who could become pregnant. Monitor BP at baseline, after 1 week, at least monthly thereafter, and as clinically indicated. Monitor for signs/symptoms of pulmonary toxicity (eg, dyspnea, cough, fever); promptly evaluate for interstitial lung disease for acute or worsening respiratory symptoms. Monitor for signs/symptoms of hypersensitivity, hemorrhage, impaired wound healing, and tumor lysis syndrome. Monitor growth plates in pediatric patients with open growth plates; monitor for symptoms indicative of slipped capital/upper femoral epiphysis in pediatric patients. Monitor adherence.

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.

Mechanism of Action

Selpercatinib is a highly selective anti-RET (REarranged during Transfection) kinase inhibitor (Solomon 2020). Selpercatinib inhibits wild-type RET, multiple mutated RET isoforms, vascular endothelial growth factor receptors 1 and 3 (VEGFR1 and VEGFR3), and fibroblast growth factor receptor (FGFR) 1, 2, and 3. Certain point mutations in RET or chromosomal rearrangements involving in-frame fusions of RET can result in constitutively activated chimeric RET fusion proteins, which may act as oncogenic drivers, promoting tumor cell line proliferation. Selpercatinib has demonstrated anti-tumor activity in cells harboring constitutive activation of RET proteins resulting from gene fusions and mutations (including CCDC6-RET, KIF5B-RET, RET V804M, and RET M918T).

Pharmacokinetics (Adult Data Unless Noted)

Note: Tablets are bioequivalent to capsules.

Distribution: V_ss/F: 203 L.

Protein binding: 96%.

Metabolism: Predominantly via CYP3A4.

Bioavailability: Capsule: 73% (range: 60% to 82%).

Half-life elimination: 32 hours.

Time to peak: 2 hours.

Excretion: Feces: 69% (14% as unchanged drug); urine: 24% (12% as unchanged drug).

Clearance: 6 L/hour.

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Hepatic function impairment: Selpercatinib AUC_0-∞ increased by 1.1-fold, 1.3-fold, and 1.8-fold in subjects with mild (total bilirubin ≤ ULN with AST > ULN or total bilirubin > 1 to 1.5 times ULN with any AST), moderate (total bilirubin >1.5 to 3 times ULN and any AST), and severe (total bilirubin >3 to 10 times ULN and any AST) hepatic impairment, respectively, compared to subjects with normal hepatic function.

Weight: Selpercatinib apparent volume of distribution and clearance increase with increasing body weight (9.6 kg to 179 kg).

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Retevmo;
(AT) Austria: Retsevmo;
(BE) Belgium: Retsevmo;
(CH) Switzerland: Retsevmo;
(CZ) Czech Republic: Retsevmo;
(DE) Germany: Retsevmo;
(EE) Estonia: Retsevmo;
(ES) Spain: Retsevmo;
(FI) Finland: Retsevmo;
(FR) France: Retsevmo;
(GB) United Kingdom: Retsevmo;
(HU) Hungary: Retsevmo;
(IT) Italy: Retsevmo;
(JP) Japan: Retevmo;
(KR) Korea, Republic of: Retevmo;
(LU) Luxembourg: Retsevmo;
(NL) Netherlands: Retsevmo;
(NO) Norway: Retsevmo;
(PL) Poland: Retsevmo;
(PR) Puerto Rico: Retevmo;
(PT) Portugal: Retsevmo;
(QA) Qatar: Retevmo;
(SA) Saudi Arabia: Retevmo;
(SE) Sweden: Retsevmo;
(SI) Slovenia: Retsevmo;
(SK) Slovakia: Retsevmo;
(TW) Taiwan: Retsevmo

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Retevmo (selpercatinib) [prescribing information]. Indianapolis, IN: Lilly USA LLC; December 2024.
Retevmo (selpercatinib) [product monograph]. Toronto, Ontario, Canada: Eli Lilly Canada Inc; October 2023.
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Topic 128157 Version 155.0

خرید پکیج

Selpercatinib: Drug information