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Osimertinib: Drug information

Osimertinib: Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Osimertinib: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Tagrisso
Brand Names: Canada
  • Tagrisso
Pharmacologic Category
  • Antineoplastic Agent, Epidermal Growth Factor Receptor (EGFR) Inhibitor;
  • Antineoplastic Agent, Tyrosine Kinase Inhibitor
Dosing: Adult
Non–small cell lung cancer, EGFR exon 19 deletion or exon 21 L858R mutation positive, adjuvant therapy

Non–small cell lung cancer, EGFR exon 19 deletion or exon 21 L858R mutation positive, adjuvant therapy: Note: Select patients for treatment based on the presence of epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations in tumor specimen.

Oral: 80 mg once daily; continue for a total of 3 years or until disease progression or unacceptable toxicity (Ref).

Non–small cell lung cancer, locally advanced, unresectable, EGFR exon 19 deletion or exon 21 L858R mutation positive

Non–small cell lung cancer, locally advanced, unresectable (stage III), EGFR exon 19 deletion or exon 21 L858R mutation positive (following platinum-based chemoradiation therapy): Note: Select patients for treatment based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in tumor specimen.

Oral: 80 mg once daily; continue until disease progression or unacceptable toxicity (Ref).

Non–small cell lung cancer, locally advanced or metastatic, EGFR exon 19 deletion or exon 21 L858R mutation positive, first-line treatment

Non–small cell lung cancer, locally advanced or metastatic, EGFR exon 19 deletion or exon 21 L858R mutation positive, first-line treatment (combination therapy): Note: Select patients for treatment based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in plasma or tumor specimens.

Oral: 80 mg once daily (in combination with pemetrexed and 4 cycles of platinum [cisplatin or carboplatin]-based chemotherapy); continue osimertinib and pemetrexed until disease progression or unacceptable toxicity (Ref).

Non–small cell lung cancer, metastatic, EGFR exon 19 deletion or exon 21 L858R mutation positive, first-line treatment

Non–small cell lung cancer, metastatic, EGFR exon 19 deletion or exon 21 L858R mutation positive, first-line treatment (single-agent): Note: Select patients for treatment based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in tumor or plasma specimens.

Oral: 80 mg once daily; continue until disease progression or unacceptable toxicity (Ref).

Non–small cell lung cancer, metastatic, previously treated, EGFR T790M mutation positive

Non–small cell lung cancer, metastatic, previously treated, EGFR T790M mutation positive: Note: Select patients for treatment based on the presence of EGFR T790M mutations in plasma or tumor specimens.

Oral: 80 mg once daily; continue until disease progression or unacceptable toxicity (Ref).

Non–small cell lung cancer, adenocarcinoma, with leptomeningeal metastases, EGFR mutation positive

Non–small cell lung cancer, adenocarcinoma, with leptomeningeal metastases, EGFR mutation positive (off-label dose): Oral: 160 mg once daily; continue until disease progression or unacceptable toxicity; may continue beyond disease progression if deriving clinical benefit (Ref).

Missed doses: If a dose is missed, do not make up the missed dose, take the next dose as scheduled.

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

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Altered kidney function: No dosage adjustment necessary for any degree of kidney impairment; increased mean exposure of the parent drug was reported in patients with advanced kidney impairment, although there was variability and overlap in reported concentrations across all degrees of kidney dysfunction (Ref). Closer monitoring for toxicity may be warranted (Ref).

Hemodialysis, intermittent (thrice weekly): Unlikely to be significantly dialyzed (high protein binding and large Vd): No dosage adjustment likely to be necessary. Several cases of successful use in patients with end-stage kidney disease have been reported (Ref).

Peritoneal dialysis: Unlikely to be significantly dialyzed (high protein binding and large Vd) (Ref): No dosage adjustment likely to be necessary (Ref).

CRRT: No dosage adjustment likely to be necessary (Ref).

PIRRT (eg, slow, low efficiency hemodiafiltration): No dosage adjustment likely to be necessary (Ref).

Dosing: Liver Impairment: Adult

Mild to moderate impairment (Child-Turcotte-Pugh class A or B or total bilirubin ≤ ULN and AST > ULN or total bilirubin 1 to 3 times ULN and any AST): No dosage adjustment necessary.

Severe impairment (total bilirubin 3 to 10 times ULN and any AST): There are no dosage adjustments provided in the manufacturer's labeling (a recommended dose has not been established).

Dosing: Adjustment for Toxicity: Adult

Note: When used in combination, other concomitant anticancer therapies may also require treatment interruption, dosage reduction, and/or discontinuation.

Recommended Osimertinib Dose Modifications

Target organ

Adverse reaction

Dose modification

Blood and bone marrow

Aplastic anemia

Withhold osimertinib if suspected; obtain hematology consultation. If aplastic anemia is confirmed, permanently discontinue osimertinib.

Cardiotoxicity

QTc interval >500 msec on at least 2 separate ECGs

Withhold osimertinib until QTc interval is <481 msec or recovery to baseline if baseline QTc is ≥481 msec, then resume osimertinib at 40 mg once daily.

QTc interval prolongation with signs/symptoms of life-threatening arrhythmia

Permanently discontinue osimertinib.

Symptomatic heart failure

Permanently discontinue osimertinib.

Cutaneous toxicity

Stevens-Johnson syndrome; erythema multiforme major; toxic epidermal necrolysis

Withhold osimertinib treatment if suspected; permanently discontinue osimertinib if confirmed.

Cutaneous vasculitis (including leukocytoclastic vasculitis, urticarial vasculitis, and IgA vasculitis)

Withhold osimertinib treatment if suspected, evaluate for systemic involvement, and consider dermatology consultation. If no other etiology is identified, consider permanent osimertinib discontinuation (based on severity).

Ocular toxicity

Signs/symptoms of keratitis (eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain and/or red eye)

If signs/symptoms of keratitis develop, promptly refer for ophthalmologic evaluation.

Pulmonary toxicity; patients who have not received recent definitive platinum-based chemoradiation therapy

Interstitial lung disease (ILD)/pneumonitis, any grade

Permanently discontinue osimertinib.

Pulmonary toxicity; patients who have received recent definitive platinum-based chemoradiation therapy

ILD/pneumonitis, grade 1

Withhold (and restart as appropriate) or continue osimertinib as clinically indicated.

ILD/pneumonitis, ≥ grade 2

Permanently discontinue osimertinib.

Other adverse reactions

≥ Grade 3

Withhold osimertinib for up to 3 weeks.

If improvement to grade 0 to 2 within 3 weeks

Resume osimertinib at 80 mg or 40 mg once daily.

If no improvement within 3 weeks

Permanently discontinue osimertinib.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

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

>10%:

Dermatologic: Nail disease (23% to 37%; including leukonychia, nail bed changes, nail discoloration, nail hyperpigmentation, onychoclasis, onycholysis, onychomadesis, paronychia), pruritus (13% to 19%), skin rash (39% to 58%), xeroderma (17% to 36%)

Endocrine & metabolic: Hypermagnesemia (24% to 30%), hypokalemia (16%), hyponatremia (20% to 26%)

Gastrointestinal: Abdominal pain (12%), constipation (15%), decreased appetite (13% to 20%), diarrhea (36% to 58%; grades 3/4: 2%; including enterocolitis), nausea (14%), stomatitis (15% to 32%; grades 3/4: ≤2%), vomiting (11%)

Hematologic & oncologic: Anemia (30% to 59%; grades 3/4: <1%), leukopenia (54% to 66%; grades 3/4: 3%), lymphocytopenia (44% to 70%; grades 3/4: 3% to 6%), neutropenia (26% to 42%; grades 3/4: ≤3%), thrombocytopenia (47% to 51%; grades 3/4: ≤1%)

Hepatic: Hyperbilirubinemia (14%), increased serum alanine aminotransferase (21%), increased serum aspartate aminotransferase (22%)

Nervous system: Fatigue (13% to 21%; including asthenia), headache (12%)

Neuromuscular & skeletal: Musculoskeletal pain (18% to 20%)

Renal: Increased serum creatinine (9% to 19%)

Respiratory: Cough (17% to 20%), dyspnea (8% to 13%), interstitial lung disease (≤56%), nasopharyngitis (14%), pneumonia (2% to 15%), pneumonitis (≤56%), upper respiratory tract infection (10% to 13%)

1% to 10%:

Cardiovascular: Decreased left ventricular ejection fraction (2% to 3%), prolonged QT interval on ECG (≤10%), pulmonary embolism (2%)

Dermatologic: Alopecia (1% to 7%), palmar-plantar erythrodysesthesia (1% to 2%), skin hyperpigmentation (≤2%), urticaria (1% to 2%)

Gastrointestinal: Gastroenteritis (1%)

Genitourinary: Urinary tract infection (8% to 10%)

Nervous system: Dizziness (10%)

Respiratory: Epistaxis (≤6%)

Miscellaneous: Fever (10%)

<1%:

Dermatologic: Erythema multiforme

Hematologic & oncologic: Aplastic anemia

Ophthalmic: Keratitis

Frequency not defined:

Cardiovascular: Cardiomyopathy

Neuromuscular & skeletal: Increased creatine phosphokinase in blood specimen

Postmarketing:

Dermatologic: Dermatologic disorder (erythema dyschromicum perstans), Stevens-Johnson syndrome, toxic epidermal necrolysis

Hematologic & oncologic: Henoch-Schönlein purpura

Hypersensitivity: Hypersensitivity angiitis (including urticarial vasculitis)

Contraindications

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

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

Warnings/Precautions

Concerns related to adverse effects:

• Aplastic anemia: Aplastic anemia has been reported in a small number of patients; some cases were fatal. Signs/symptoms of aplastic anemia may include new or persistent fevers, bruising, bleeding, and/or pallor.

• Cardiovascular toxicity: Cardiomyopathy (cardiac failure, chronic cardiac failure, congestive heart failure, pulmonary edema, or decreased ejection fraction) has been observed; some events were fatal. In some studies, a left ventricular ejection fraction (LVEF) decline of ≥10% from baseline or a drop to <50% were noted in a small percentage of patients (single-agent and combination therapy). Prolongation of the QTc interval may occur; QTc >500 msec and an increase from baseline of >60 msec have been reported, although no QTc-related arrhythmias have been reported. Patients with a baseline QTc of ≥470 were excluded from clinical trials.

• Cutaneous toxicity: Cases of Stevens-Johnson syndrome, erythema multiforme major, toxic epidermal necrolysis, and cutaneous vasculitis (including leukocytoclastic vasculitis, urticarial vasculitis, and IgA vasculitis) have been reported.

• Ocular toxicity: Keratitis has been reported (rarely) in clinical trials.

• Pulmonary toxicity: Interstitial lung disease (ILD) and pneumonitis were observed in clinical studies (including patients who have and have not received osimertinib following platinum-based definitive chemoradiation therapy); some events were fatal. Respiratory symptoms which may be indicative of ILD include dyspnea, cough, and/or fever. Approximately one half of patients who received osimertinib following definitive platinum-based chemoradiation therapy developed ILD/pneumonitis (including radiation pneumonitis); some patients required dose modification and permanent discontinuation. Among patients who were rechallenged, 11% had recurrence of ILD/pneumonitis. Of the patients who developed ILD/pneumonitis, equal numbers of patients either had resolution (with/or without sequalae) or did not have symptoms resolve. Cases of transient asymptomatic pulmonary opacities (TAPOs; apparent clinically benign areas of localized ground-glass opacities) have been observed with osimertinib. TAPOs may be mistaken for isolated pulmonary progression of disease or the beginning of more severe pneumonitis. Some TAPOs cases resolved during continued osimertinib treatment; monitor closely (Noonan 2016).

Special populations:

• Older adults: A higher incidence of ≥ grade 3 adverse reactions and more frequent dose modifications for adverse reactions were observed in patients ≥65 years of age as compared to those <65 years of age treated with osimertinib (single-agent therapy and combination therapy).

Other warnings/precautions:

• Appropriate use: Confirm the presence of epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations in tumor specimen (for adjuvant therapy or in locally advanced, unresectable [stage III] disease following completion of platinum-based definitive chemoradiation therapy) or in tumor or plasma specimen for first-line treatment of locally advanced or metastatic non-small cell lung cancer. Confirm the presence of an EGFR T790M mutation in tumor or plasma specimen prior to treatment initiation in patients receiving treatment following progression on or after EGFR tyrosine kinase inhibitor therapy. Circulating tumor cells from plasma sample may be used as a surrogate marker for detection of T790M in tumor tissue (Remon 2017). Information on diagnostic tests approved for detection of EGFR mutations may be found at www.fda.gov/companiondiagnostics.

Dosage Forms: US

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

Tablet, Oral:

Tagrisso: 40 mg

Tablet, Oral, as mesylate:

Tagrisso: 80 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Tagrisso Oral)

40 mg (per each): $705.23

80 mg (per each): $705.23

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.

Tablet, Oral:

Tagrisso: 40 mg

Tablet, Oral, as mesylate:

Tagrisso: 80 mg

Prescribing and Access Restrictions

Available through specialty pharmacies and distributors. Further information may be obtained from the manufacturer, Astra Zeneca, at 1-844-275-2360 or at https://www.tagrisso.com.

Administration: Adult

Oral: May be administered with or without food. For patients who have difficulty swallowing tablets, disperse tablet in 60 mL of noncarbonated water (only), stir until tablet is dispersed into small pieces (will not dissolve completely) and immediately swallow. Rinse container with 120 to 240 mL of water and immediately drink. Do not crush, heat, or ultrasonicate during preparation.

NG tube: Disperse the tablet in 15 mL of noncarbonated water; use an additional 15 mL of water to transfer residue to the syringe. Administer the 30 mL of liquid via the nasogastric tube and flush appropriately (with ~30 mL of water). Repeat process until no pieces remain in the syringe to ensure the full dose is administered. Administer tablet dispersion and residues within 30 minutes of the addition of the tablets to water. Do not crush, heat, or ultrasonicate during preparation.

Use: Labeled Indications

Non–small cell lung cancer, EGFR exon 19 deletion or exon 21 L858R mutation positive, adjuvant therapy: Adjuvant therapy (as a single agent) of non–small cell lung cancer (NSCLC) following tumor resection in adults whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations (as detected by an approved test).

Non–small cell lung cancer, locally advanced, unresectable, EGFR exon 19 deletion or exon 21 L858R mutation positive: Treatment (as a single agent) of locally advanced, unresectable (stage III) NSCLC in adults without progression following concurrent or sequential platinum-based chemoradiation therapy and whose tumors EGFR exon 19 deletions or exon 21 L858R mutations (as detected by an approved test).

Non–small cell lung cancer, locally advanced or metastatic, EGFR exon 19 deletion or exon 21 L858R mutation positive, first-line treatment: First-line treatment (in combination with pemetrexed and platinum-based chemotherapy) of locally advanced or metastatic NSCLC in adults whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations (as detected by an approved test).

Non–small cell lung cancer, metastatic, EGFR exon 19 deletion or exon 21 L858R mutation positive: First-line treatment (as single agent) of metastatic NSCLC in adults whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations (as detected by an approved test).

Non–small cell lung cancer, metastatic, previously treated, EGFR T790M mutation positive: Treatment (as single agent) of metastatic EGFR T790M mutation-positive (as detected by an approved test) NSCLC in adults with disease progression on or after EGFR tyrosine kinase inhibitor therapy.

Use: Off-Label: Adult

Non-small cell lung cancer, adenocarcinoma, with leptomeningeal metastases, EGFR mutation-positive

Medication Safety Issues
Sound-alike/look-alike issues:

Osimertinib may be confused with dacomitinib, erlotinib, olaparib, ospemifene.

Tagrisso may be confused with Targretin, Tasigna.

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 with inducers), CYP3A4 (Minor with inhibitors), P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP, 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.

5-Aminosalicylic Acid Derivatives: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

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

Amisulpride (Oral): May increase QTc-prolonging effects of QT-prolonging Agents (Moderate Risk). Risk C: Monitor

Antithyroid Agents: Myelosuppressive Agents may increase neutropenic effects of Antithyroid Agents. Risk C: Monitor

Azithromycin (Systemic): QT-prolonging Kinase Inhibitors (Moderate Risk) may increase QTc-prolonging effects of Azithromycin (Systemic). 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

BCG (Intravesical): Myelosuppressive Agents may decrease therapeutic effects of BCG (Intravesical). Myelosuppressive Agents may increase adverse/toxic effects of BCG (Intravesical). Risk X: Avoid

BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors): Osimertinib 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

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

Chloramphenicol (Ophthalmic): May increase adverse/toxic effects of Myelosuppressive Agents. Risk C: Monitor

Chloramphenicol (Systemic): Myelosuppressive Agents may increase myelosuppressive effects of Chloramphenicol (Systemic). Risk X: Avoid

Cladribine: May increase myelosuppressive effects of Myelosuppressive Agents. Risk X: Avoid

CloZAPine: May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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

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

CYP3A4 Inducers (Moderate): May decrease serum concentration of Osimertinib. Risk C: Monitor

CYP3A4 Inducers (Strong): May decrease serum concentration of Osimertinib. Management: Avoid coadministration of osimertinib and strong CYP3A4 inducers if possible. If coadministration is unavoidable, increase osimertinib to 160 mg daily. Reduce osimertinib to 80 mg daily 3 weeks after discontinuation of the strong CYP3A4 inducer. Risk D: Consider Therapy Modification

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

Dabrafenib: Osimertinib may increase QTc-prolonging effects of Dabrafenib. Dabrafenib may decrease serum concentration of Osimertinib. Management: Monitor for decreased osimertinib efficacy, QTc interval prolongation and ventricular arrhythmias, including torsades de pointes when these agents are combined. Risk C: Monitor

Deferiprone: Myelosuppressive Agents may increase neutropenic effects of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider Therapy Modification

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 (Moderate Risk) may increase QTc-prolonging effects of Domperidone. Risk X: Avoid

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

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

Encorafenib: Osimertinib may increase QTc-prolonging effects of Encorafenib. Encorafenib may decrease serum concentration of Osimertinib. Management: Avoid coadministration of osimertinib and encorafenib if possible. If coadministration is unavoidable, increase osimertinib to 160 mg daily. Reduce osimertinib to 80 mg daily 3 weeks after encorafenib discontinuation. Monitor for QTc interval prolongation Risk D: Consider Therapy Modification

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

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: Myelosuppressive Agents may increase myelosuppressive effects of Fexinidazole. Risk X: Avoid

Fluorouracil Products: May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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

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

Haloperidol: QT-prolonging Kinase Inhibitors (Moderate Risk) may increase QTc-prolonging effects of Haloperidol. 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

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

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

Linezolid: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

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

Midostaurin: May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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

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

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

OLANZapine: May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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

Olaparib: Myelosuppressive Agents may increase myelosuppressive effects of Olaparib. Risk C: Monitor

Ondansetron: May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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

PAZOPanib: Osimertinib may increase QTc-prolonging effects of PAZOPanib. Osimertinib may increase serum concentration of PAZOPanib. Risk X: Avoid

Pentamidine (Systemic): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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

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

Piperaquine: QT-prolonging Agents (Moderate 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

Promazine: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

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

QT-prolonging Antidepressants (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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 Antipsychotics (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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 IC Antiarrhythmics (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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 Inhalational Anesthetics (Moderate Risk): QT-prolonging Kinase Inhibitors (Moderate Risk) may increase QTc-prolonging effects of QT-Prolonging Inhalational Anesthetics (Moderate 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 Kinase Inhibitors (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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 Miscellaneous Agents (Moderate Risk): QT-prolonging Kinase Inhibitors (Moderate Risk) may increase QTc-prolonging effects of QT-prolonging Miscellaneous Agents (Moderate 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 Moderate CYP3A4 Inhibitors (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase serum concentration of QT-prolonging Kinase Inhibitors (Moderate Risk). Risk C: Monitor

QT-prolonging Quinolone Antibiotics (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Kinase Inhibitors (Moderate 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 Strong CYP3A4 Inhibitors (Moderate Risk): Osimertinib may increase QTc-prolonging effects of QT-prolonging Strong CYP3A4 Inhibitors (Moderate 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

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

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

RisperiDONE: QT-prolonging Kinase Inhibitors (Moderate Risk) may increase QTc-prolonging effects of RisperiDONE. 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

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

Ropeginterferon Alfa-2b: Myelosuppressive Agents may increase myelosuppressive effects of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider Therapy Modification

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

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

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

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

Thioridazine: QT-prolonging Agents (Moderate 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

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

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

Verify pregnancy status prior to initiating osimertinib in patients who could become pregnant. Patients who could become pregnant should use effective contraception during therapy and for 6 weeks after the last osimertinib dose. Patients with partners who could become pregnant should use effective contraception during therapy and for 4 months after the last osimertinib dose.

Pregnancy Considerations

Based on data from animal reproduction studies and the mechanism of action, use during pregnancy is expected to cause fetal harm.

Breastfeeding Considerations

It is not known if osimertinib (or its active metabolites) are present in breast milk. Because of the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 2 weeks after the last osimertinib dose.

Monitoring Parameters

Prior to treatment, test for epidermal growth factor receptor (EGFR) exon 19 deletions, exon 21 L858R mutations, or for EGFR T790M mutation status; see table below.

Osimertinib Patient Selection Criteria for Treatment

Indication

Required mutation

Specimen type

a NSCLC = non–small cell lung cancer

NSCLCa, EGFR mutation-positive, adjuvant therapy (single agent therapy)

EGFR exon 19 deletion or exon 21 L858R mutations

Tumor

NSCLC, locally advanced, unresectable (stage III), EGFR mutation-positive (single agent therapy; following completion of platinum-based chemoradiation therapy)

EGFR exon 19 deletion or exon 21 L858R mutations

Tumor

NSCLC, locally advanced or metastatic, first-line treatment, EGFR mutation-positive, first-line treatment (in combination with pemetrexed and platinum [cisplatin or carboplatin]-based chemotherapy)

EGFR exon 19 deletion or exon 21 L858R mutations

Plasma or tumor

NSCLC, metastatic EGFR mutation-positive, first-line treatment (single agent therapy)

EGFR exon 19 deletion or exon 21 L858R mutations

Plasma or tumor

NSCLC, metastatic, previously treated, EGFR T790M mutation positive (single agent therapy)

EGFR T970M mutation

Plasma or tumor

CBC with differential (baseline and periodically; more frequently if indicated). Evaluate pregnancy status (prior to therapy initiation in patients who could become pregnant). Monitor ECG and electrolytes periodically (in patients with a history of congenital long QTc syndrome, heart failure, electrolyte abnormalities, and/or those taking concurrent medications known to prolong the QTc interval). Assess cardiac function, including left ventricular ejection fraction prior to treatment and while on treatment in patients with cardiac risk factors (single-agent therapy) or in all patients (combination therapy), and assess in patients who develop cardiac signs/symptoms. Monitor for signs/symptoms of interstitial lung disease or pneumonitis, aplastic anemia, dermatologic, ocular toxicity (refer for ophthalmologic evaluation promptly for signs/symptoms of keratitis), and gastrointestinal toxicity. Monitor adherence.

The American Society of Clinical Oncology hepatitis B screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends hepatitis B virus (HBV) screening with hepatitis B surface antigen (HBsAg), hepatitis B core antibody (anti-HBc), total Ig or IgG, and antibody to hepatitis B surface antigen (anti-HBs) 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.

Additional cardiovascular monitoring: Comprehensive assessment prior to treatment including a history and physical examination, screening for cardiovascular disease risk factors such as hypertension, diabetes, dyslipidemia, obesity, and smoking (ASCO [Armenian 2017]; ESC [Lyon 2022]). Obtain echocardiography at baseline and every 3 months (ESC [Lyon 2022]).

Mechanism of Action

Osimertinib is an irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor which binds to select mutant forms of EGFR, including T790M, L858R, and exon 19 deletion at lower concentrations than wild-type. Osimertinib exhibits less activity against wild-type EGFR (as compared to other EGFR inhibitors) and is selective for sensitizing mutations and the T790M resistance mutation, which is the most common mechanism of resistance to EGFR tyrosine kinase inhibitors (Janne 2015).

Pharmacokinetics (Adult Data Unless Noted)

Distribution: Vss/F: 918 L; penetrates blood brain barrier (Soria 2018; Yang 2020).

Protein binding: 95%.

Metabolism: Hepatic; predominantly oxidation (via CYP3A) and dealkylation to 2 active metabolites (AZ7550 and AZ5104).

Bioavailability: AUC is increased by 19% with a high-fat, high-calorie meal.

Half-life, elimination: Mean (estimated): 48 hours.

Time to peak: Median: 6 hours (range: 3 to 24 hours).

Excretion: Feces (68%; ~2% as unchanged drug); Urine (14%; ~2% as unchanged drug).

Clearance: 14.3 L/hour.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Tagrisso;
  • (AR) Argentina: Ositerib | Tagrisso;
  • (AT) Austria: Tagrisso;
  • (AU) Australia: Tagrisso;
  • (BD) Bangladesh: Osicent | Osimert | Osinib | Tagrisso | Tagrix;
  • (BE) Belgium: Tagrisso;
  • (BG) Bulgaria: Tagrisso;
  • (BR) Brazil: Tagrisso;
  • (CH) Switzerland: Tagrisso;
  • (CL) Chile: Tagrisso;
  • (CN) China: Osimertinib mesylate | Tagrisso;
  • (CO) Colombia: Tagrisso;
  • (CZ) Czech Republic: Tagrisso;
  • (DE) Germany: Tagrisso;
  • (DO) Dominican Republic: Tagrisso;
  • (EC) Ecuador: Tagrisso;
  • (EE) Estonia: Azd9291 | Tagrisso;
  • (EG) Egypt: Tagrisso;
  • (ES) Spain: Tagrisso;
  • (FR) France: Tagrisso;
  • (GB) United Kingdom: Tagrisso;
  • (GR) Greece: Tagrisso;
  • (HK) Hong Kong: Tagrisso;
  • (HR) Croatia: Tagrisso;
  • (HU) Hungary: Tagrisso;
  • (ID) Indonesia: Tagrisso;
  • (IE) Ireland: Tagrisso;
  • (IN) India: Tagrisso;
  • (IT) Italy: Tagrisso;
  • (JO) Jordan: Tagrisso;
  • (JP) Japan: Tagrisso;
  • (KR) Korea, Republic of: Tagrisso;
  • (KW) Kuwait: Tagrisso;
  • (LB) Lebanon: Tagrisso;
  • (LT) Lithuania: Tagrisso;
  • (LV) Latvia: Tagrisso;
  • (MX) Mexico: Tagrisso;
  • (MY) Malaysia: Tagrisso;
  • (NL) Netherlands: Tagrisso;
  • (NO) Norway: Tagrisso;
  • (NZ) New Zealand: Tagrisso;
  • (PA) Panama: Tagrisso;
  • (PE) Peru: Tagrisso;
  • (PH) Philippines: Tagrisso;
  • (PL) Poland: Tagrisso;
  • (PR) Puerto Rico: Tagrisso;
  • (PT) Portugal: Tagrisso;
  • (QA) Qatar: Tagrisso;
  • (RO) Romania: Tagrisso;
  • (RU) Russian Federation: Tagrisso;
  • (SA) Saudi Arabia: Tagrisso;
  • (SE) Sweden: Tagrisso;
  • (SG) Singapore: Tagrisso;
  • (SI) Slovenia: Tagrisso;
  • (SK) Slovakia: Tagrisso;
  • (TH) Thailand: Tagrisso;
  • (TR) Turkey: Tagrisso;
  • (TW) Taiwan: Tagrisso;
  • (UA) Ukraine: Tagrisso;
  • (UY) Uruguay: Tagrisso;
  • (ZA) South Africa: Tagrisso
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