Fam-trastuzumab deruxtecan: Drug information

For additional information see "Fam-trastuzumab deruxtecan: Patient drug information"

For abbreviations, symbols, and age group definitions show table

ALERT: US Boxed Warning

Interstitial lung disease:

Interstitial lung disease (ILD) and pneumonitis, including fatal cases, have been reported with fam-trastuzumab deruxtecan. Monitor for and promptly investigate signs and symptoms including cough, dyspnea, fever, and other new or worsening respiratory symptoms. Permanently discontinue fam-trastuzumab deruxtecan in all patients with ≥ grade 2 ILD/pneumonitis. Advise patients of the risk and the need to immediately report symptoms.

Embryo-fetal toxicity:

Exposure to fam-trastuzumab deruxtecan during pregnancy can cause embryo-fetal harm. Advise patients of these risks and the need for effective contraception.

Brand Names: US

Enhertu

Brand Names: Canada

Enhertu

Pharmacologic Category

Antineoplastic Agent, Anti-HER2;
Antineoplastic Agent, Antibody Drug Conjugate;
Antineoplastic Agent, Monoclonal Antibody;
Antineoplastic Agent, Topoisomerase I Inhibitor

Dosing: Adult

Dosage guidance:

Safety: Actively manage modifiable cardiac risk factors (smoking, hypertension, diabetes, dyslipidemia, obesity) before initiating treatment (Ref). Do not substitute fam-trastuzumab deruxtecan for or with ado-trastuzumab emtansine, conventional trastuzumab (or trastuzumab biosimilars), pertuzumab/trastuzumab/hyaluronidase, or trastuzumab/hyaluronidase; products are different and are NOT interchangeable.

Clinical considerations: Fam-trastuzumab deruxtecan is associated with a moderate to high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Ref); delayed nausea and/or vomiting may occur. Refer to the protocol or institutional guidance for additional details of off-label dosing.

Breast cancer, unresectable or metastatic, hormone receptor positive, HER2 low or HER2 ultralow

Breast cancer, unresectable or metastatic, hormone receptor positive, HER2 low or HER2 ultralow (previously treated) : IV: 5.4 mg/kg once every 3 weeks; continue until disease progression or unacceptable toxicity (Ref).

Breast cancer, unresectable or metastatic, HER2 low

Breast cancer, unresectable or metastatic, HER2 low (previously treated): IV: 5.4 mg/kg once every 3 weeks; continue until disease progression or unacceptable toxicity (Ref).

Breast cancer, unresectable or metastatic, HER2 positive

Breast cancer, unresectable or metastatic, HER2 positive (previously treated): IV: 5.4 mg/kg once every 3 weeks; continue until disease progression or unacceptable toxicity (Ref).

Gastric cancer, locally advanced or metastatic, HER2 positive

Gastric cancer, locally advanced or metastatic, HER2 positive (gastric or gastroesophageal junction adenocarcinoma; previously treated): IV: 6.4 mg/kg once every 3 weeks; continue until disease progression or unacceptable toxicity (Ref).

Non–small cell lung cancer, unresectable or metastatic, HER2 mutation positive

Non–small cell lung cancer, unresectable or metastatic, HER2 (ERBB2) mutation positive (previously treated): IV: 5.4 mg/kg once every 3 weeks; continue until disease progression or unacceptable toxicity (Ref).

Solid tumors, unresectable or metastatic, HER2 positive

Solid tumors, unresectable or metastatic, HER2 positive (previously treated): IV: 5.4 mg/kg once every 3 weeks; continue until disease progression or unacceptable toxicity (Ref).

Missed dose: If a planned dose is delayed or missed, administer the dose as soon as possible (do not wait until the next planned cycle) and then adjust the administration schedule to maintain a 3-week interval between doses. Infuse the missed/delayed dose at the dose and rate the patient tolerated in the most recent infusion.

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

CrCl ≥30 mL/minute: No dosage adjustment necessary. Monitor more frequently for interstitial lung disease in patients with moderate kidney impairment.

CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (a recommended dose has not been established).

Dosing: Liver Impairment: Adult

Mild (total bilirubin ≤ ULN and any AST > ULN or total bilirubin >1 to 1.5 times ULN and any AST) or moderate (total bilirubin >1.5 to 3 times ULN and any AST) impairment: No dosage adjustment necessary. Monitor closely for toxicities in patients with moderate hepatic impairment.

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

Dosing: Obesity: Adult

American Society of Clinical Oncology guidelines for appropriate systemic therapy dosing in adults with cancer with a BMI ≥30 kg/m² : Utilize patient's actual body weight for calculation of BSA- or weight-based dosing; manage regimen-related toxicities in the same manner as for patients with a BMI <30 kg/m² (ASCO [Griggs 2021]). Note: Per the manufacturer's labeling, do not re-escalate fam-trastuzumab deruxtecan dose following a dose reduction.

Dosing: Adjustment for Toxicity: Adult

Adverse reaction management may require treatment interruption, dosage reduction, and/or discontinuation. Do not re-escalate the fam-trastuzumab deruxtecan dose after a dosage reduction is made.

**Recommended Fam-Trastuzumab Deruxtecan Dosage Reduction Levels**
Dose reduction schedule	Breast cancer, non–small cell lung cancer, and IHC 3+ solid tumors	Gastric cancer
Initial (usual) dose	5.4 mg/kg	6.4 mg/kg
First dose reduction level	4.4 mg/kg	5.4 mg/kg
Second dose reduction level	3.2 mg/kg	4.4 mg/kg
Further dosage adjustment required	Discontinue treatment	Discontinue treatment

**Fam-Trastuzumab Deruxtecan Dosage Adjustment for Toxicities**
Toxicity	Severity		Fam-Trastuzumab Deruxtecan Dose Modification
^a Asymptomatic heart disease: Consider initiating heart failure medications (eg, angiotensin-converting enzyme inhibitors or an angiotensin receptor blocker, and/or beta-blockers) in patients with asymptomatic (stage B) heart disease (ASCO [Armenian 2017], ESC (Lyon 2022]). For mild cardiac dysfunction, continue treatment with close cardiovascular monitoring; for moderate dysfunction, consider continuing treatment with close cardiovascular monitoring - initiation of heart failure medications is recommended; for severe dysfunction, interrupt treatment and utilize a multidisciplinary approach when deciding if/when to restart - initiation of heart failure medications is recommended (ESC [Lyon 2022]). Symptomatic heart disease: Initiate heart failure medications; for mild cardiac dysfunction, consider a multidisciplinary approach for decisions regarding treatment interruption versus continuation; for moderate or severe cardiac dysfunction, interrupt treatment and consider a multidisciplinary approach for decisions regarding treatment reinitiation (ESC [Lyon 2022]).
Neutropenia	Grade 3 (ANC 500 to <1,000/mm³)		Interrupt fam-trastuzumab deruxtecan until resolved to ≤ grade 2, then maintain dose.
Neutropenia	Grade 4 (ANC <500/mm³)		Interrupt fam-trastuzumab deruxtecan until resolved to ≤ grade 2, then reduce dose by one dose level.
Neutropenic fever	ANC <1,000/mm³ and temperature >38.3°C or a sustained temperature of ≥38°C for >1 hour		Interrupt fam-trastuzumab deruxtecan until resolved, then reduce dose by one dose level.
Thrombocytopenia	Grade 3 (platelets 25,000 to <50,000/mm³)		Interrupt fam-trastuzumab deruxtecan until resolved to ≤ grade 1, then maintain dose.
Thrombocytopenia	Grade 4 (platelets <25,000/mm³)		Interrupt fam-trastuzumab deruxtecan until resolved to ≤ grade 1, then reduce dose by one dose level.
Cardiotoxicity^a: Left ventricular dysfunction	Left ventricular ejection fraction (LVEF) >45% and absolute decrease from baseline is 10% to 20%		Continue fam-trastuzumab deruxtecan treatment.
	LVEF 40% to 45%	And absolute decrease from baseline is <10%	Continue fam-trastuzumab deruxtecan treatment and repeat LVEF assessment within 3 weeks.
	LVEF 40% to 45%	And absolute decrease from baseline is 10% to 20%	Interrupt fam-trastuzumab deruxtecan treatment. Repeat LVEF assessment within 3 weeks. If LVEF has not recovered to within 10% from baseline, permanently discontinue fam-trastuzumab deruxtecan. If LVEF recovers to within 10% from baseline, resume fam-trastuzumab deruxtecan treatment at the same dose.
	LVEF <40% or absolute decrease from baseline is >20%		Interrupt fam-trastuzumab deruxtecan treatment. Repeat LVEF assessment within 3 weeks. If LVEF of <40% or absolute decrease from baseline of >20% is confirmed, permanently discontinue fam-trastuzumab deruxtecan.
	Symptomatic heart failure		Permanently discontinue fam-trastuzumab deruxtecan.
Infusion reaction	Infusion-related symptoms		Interrupt infusion or slow infusion rate.
Infusion reaction	Severe infusion reaction		Permanently discontinue fam-trastuzumab deruxtecan.
Pulmonary toxicity: Interstitial lung disease (ILD)/pneumonitis	Asymptomatic ILD/pneumonitis (grade 1)		Interrupt fam-trastuzumab deruxtecan until resolved to grade 0, then: • If resolved in ≤28 days from date of onset, maintain dose. • If resolved in >28 days from date of onset, reduce dose by one dose level. • Consider corticosteroid treatment as soon as ILD/pneumonitis is suspected (eg, ≥0.5 mg/kg/day prednisolone [or equivalent], followed by a gradual taper, if necessary). • Consider consultation with a pulmonologist.
	Symptomatic ILD/pneumonitis (≥ grade 2)		Permanently discontinue fam-trastuzumab deruxtecan. Promptly initiate systemic corticosteroid treatment as soon as ILD/pneumonitis is suspected (eg, ≥1 mg/kg/day prednisolone [or equivalent] for at least 14 days followed by a gradual taper over at least 4 weeks). Consider consultation with a pulmonologist.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions (Significant): Considerations

Bone marrow suppression

Neutropenia, including severe grades 3 and 4 toxicity, and febrile neutropenia, has been reported. Therapy interruption and/or dose reduction may be warranted, depending on severity.

Mechanism: Dose-related.

Onset: Varied; median time to first onset of decreased neutrophil count was 16 days (range: 4 to 187) for locally advanced or metastatic gastric cancer and 22 days (range: 2 to 939) for metastatic breast cancer and anti-human epidermal growth factor receptor 2 (HER2)-mutant non-small cell lung cancer (NSCLC).

Cardiotoxicity

Patients treated with fam-trastuzumab deruxtecan may be at an increased risk of left ventricular dysfunction. Decreased left ventricular ejection fraction (LVEF) has been reported with anti-human epidermal growth factor receptor 2 (HER2) therapies, including fam-trastuzumab deruxtecan. Therapy interruption and/or permanent discontinuation may be warranted, depending on severity. Patients with a history of clinically significant cardiac disease or LVEF <50% prior to treatment have not been studied.

GI effects

Nausea, vomiting, constipation, diarrhea, and stomatitis were reported with fam-trastuzumab deruxtecan. Fam-trastuzumab deruxtecan is associated with moderate to high emetic potential; antiemetics are recommended for prevention (Ref).

Pulmonary toxicity

Interstitial lung disease (ILD) and pneumonitis have been reported with fam-trastuzumab deruxtecan. Fatal cases have occurred; however, most patients experienced Grade 1 or 2 events (Ref). Similar anti-human epidermal growth factor receptor 2 (HER2)-directed therapies, such as trastuzumab, trastuzumab emtansine, and topoisomerase I inhibitors have also been associated with pulmonary toxicity (Ref). Therapy interruption and/or permanent discontinuation may be warranted, depending on severity.

Mechanism: Dose-related; not clearly established. May involve alveolar macrophage uptake and redistribution of trastuzumab deruxtecan (Ref).

Onset: Delayed; median time to first onset was 2.8 months (range: 1.2 to 21) for locally advanced or metastatic gastric cancer and 5.5 months (range: 0.9 to 31.5) for metastatic breast cancer and HER2-mutant non-small cell lung cancer (NSCLC). In a pooled analysis of nine phase I and II monotherapy studies, the median time to onset was 5.4 months (range: <0.1 to 46.8 months) in heavily pretreated patients across all doses and tumor types (Ref).

Risk factors:

• Dose >6.4 mg/kg (Ref)

• Age <65 years (Ref)

• Baseline oxygen saturation <95% (Ref)

• Moderate to severe kidney impairment (Ref)

• Pulmonary comorbidities (ie, asthma, COPD, prior ILD/pneumonitis, pulmonary fibrosis, pulmonary emphysema, radiation pneumonitis) (Ref)

• Time since initial diagnosis >4 years (Ref)

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.

>10%:

Cardiovascular: Edema (11%; peripheral edema [8% to 10%])

Dermatologic: Alopecia (21% to 48%), skin rash (3% to 13%; including bullous rash, dermatitis, erythema multiforme, maculopapular rash, palmar-plantar erythrodysesthesia)

Endocrine & metabolic: Decreased serum albumin (39%), decreased serum potassium (17% to 35%), decreased serum sodium (22%), weight loss (7% to 18%)

Gastrointestinal: Abdominal pain (9% to 22%), constipation (24% to 35%), decreased appetite (29% to 60%), diarrhea (19% to 34%; grades 3/4: 1% to 4%), dysgeusia (6% to 12%), dyspepsia (11% to 12%), nausea (61% to 79%; grades 3/4: 2% to 7%), stomatitis (11% to 20%; grades 3/4: ≤2%), vomiting (26% to 49%; grades 3/4: 1% to 4%)

Hematologic & oncologic: Decreased hemoglobin (58% to 75%; grades 3/4: 7% to 38%), decreased neutrophils (52% to 75%; grades 3/4: 12% to 51%), decreased platelet count (37% to 68%; grades 3/4: 3% to 12%), decreased white blood cell count (60% to 86%; grades 3/4: 4% to 29%), hemorrhage (16%), lymphocytopenia (43% to 70%; grades 3/4: 14% to 28%)

Hepatic: Increased serum alanine aminotransferase (34% to 53%), increased serum alkaline phosphatase (22% to 54%), increased serum aspartate aminotransferase (35% to 67%), increased serum bilirubin (15% to 24%)

Nervous system: Dizziness (8% to 13%; including orthostatic dizziness, vertigo), fatigue (32% to 62%; including asthenia, malaise), headache (4% to 22%), peripheral neuropathy (13%; grades 3/4: <1%)

Neuromuscular & skeletal: Musculoskeletal pain (15% to 32%)

Ophthalmic: Dry eye syndrome (6% to 11%)

Renal: Increased serum creatinine (7% to 16%)

Respiratory: Cough (10% to 20%), dyspnea (5% to 13%), epistaxis (3% to 13%), interstitial lung disease (6% to 16%; including pneumonitis, respiratory failure), respiratory tract infection (22%; including bronchitis, influenza, lower respiratory tract infection, pneumonia, respiratory syncytial virus infection), upper respiratory tract infection (4% to 20%)

Miscellaneous: Fever (11% to 24%)

1% to 10%:

Cardiovascular: Decreased left ventricular ejection fraction (3% to 8%; may be asymptomatic)

Dermatologic: Pruritus (3% to 8%), skin hyperpigmentation (≤6%)

Endocrine & metabolic: Dehydration (2% to 6%)

Gastrointestinal: Abdominal distention (3% to 5%), flatulence (2%), gastritis (≤3%)

Hematologic & oncologic: Febrile neutropenia (≤5%; grades 3/4: 5%)

Hepatic: Hepatic impairment (8%)

Hypersensitivity: Infusion-related reaction (≤3%; including anaphylaxis, hypersensitivity reaction)

Immunologic: Antibody development (2% to 3%; neutralizing: 6%)

Ophthalmic: Blurred vision (3% to 5%; including visual impairment)

Frequency not defined:

Cardiovascular: Myocarditis, troponin increased in blood specimen

Dermatologic: Cellulitis

Endocrine & metabolic: Hypercalcemia, hypomagnesemia

Gastrointestinal: Intestinal obstruction

Genitourinary: Urinary tract infection

Hematologic & oncologic: Tumor hemorrhage

Hepatic: Cholestatic jaundice

Infection: Sepsis

Respiratory: Pleural effusion

Postmarketing: Gastrointestinal: Gastrointestinal perforation (pyloric perforation) (Al-Tweigeri 2023)

Contraindications

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

Canadian labeling: Hypersensitivity to fam-trastuzumab deruxtecan or any component of the formulation.

Warnings/Precautions

Special populations:

• Older adults: Patients with breast cancer (HER2-positive, HER2-low, or HER2-ultralow) who were ≥65 years of age experienced a higher incidence of grade 3 or 4 adverse events, compared to patients <65 years of age.

Dosage form specific issues:

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.

Other warnings/precautions:

• Do not interchange: Fam-trastuzumab deruxtecan and ado-trastuzumab emtansine, conventional trastuzumab (or trastuzumab biosimilars), pertuzumab/trastuzumab/hyaluronidase, or trastuzumab/hyaluronidase products are different and are NOT interchangeable. Do not substitute. Dosing and treatment schedules among the various trastuzumab-based products differ; confusion between the products may potentially cause harm to the patient. Verify product label prior to reconstitution and administration to prevent medication errors.

• HER2 status: For HER2-low (immunohistochemical [IHC] 1+ or IHC 2+ and negative in situ hybridization [ISH]) or HER2-ultralow (IHC 0 with membrane staining) breast cancer, select patients for therapy based on HER2 expression. For HER2-positive breast cancer, HER2-positivity is based on IHC 3+ or ISH positive. For gastric cancer, select patients for therapy based on HER2 protein overexpression or HER2 gene amplification (IHC 3+ or IHC 2+ and ISH positive); reassess HER2 status in between the prior trastuzumab therapy and fam-trastuzumab deruxtecan if feasible to obtain a new tumor specimen. For HER2-mutant non-small cell lunger cancer, select patients for therapy based on the presence of activating HER2 (ERBB2) mutations in tumor or plasma specimen (if no mutation is present in plasma specimen, test tumor tissue). For HER2-positive solid tumors, select patients for therapy based on HER2-positive expression (IHC 3+). Information on approved tests for HER2 protein expression, HER2 gene amplifications, and activating HER2 mutations is available at http://www.fda.gov/CompanionDiagnostics.

Dosage Forms: US

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

Solution Reconstituted, Intravenous [preservative free]:

Enhertu: fam-trastuzumab deruxtecan-nxki 100 mg (1 ea) [contains polysorbate 80]

Generic Equivalent Available: US

Pricing: US

Solution (reconstituted) (Enhertu Intravenous)

100 mg (per each): $3,521.70

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.

Solution Reconstituted, Intravenous:

Enhertu: fam-trastuzumab deruxtecan-nxki 100 mg (1 ea) [contains polysorbate 80]

Administration: Adult

IV: Administer the first infusion over 90 minutes. If initial infusion was tolerated well, administer subsequent infusions over 30 minutes. Do not administer as an IV push or bolus. Administer only with an infusion set made of polyolefin or polybutadiene and a 0.2- or 0.22-micron in-line polyethersulfone or polysulfone filter. If solution prepared for infusion was refrigerated, allow solution to reach room temperature prior to administration. Cover infusion bag during infusion to protect from light. Slow or interrupt the infusion rate if infusion-related symptoms develop; discontinue permanently for severe infusion reactions. Do not administer with other drugs through the same IV line.

Fam-trastuzumab deruxtecan is associated with a moderate to high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Ref); delayed nausea and/or vomiting may occur.

Check label to ensure appropriate product is being administered; fam-trastuzumab deruxtecan, trastuzumab/hyaluronidase, conventional trastuzumab products, ado-trastuzumab emtansine, and pertuzumab/trastuzumab/hyaluronidase are different products and are NOT interchangeable.

Hazardous Drugs Handling Considerations

Hazardous agent (NIOSH 2024 [table 1]).

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).

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:

Enhertu: https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/761139s032s035lbl.pdf#page=50

Use: Labeled Indications

Breast cancer, unresectable or metastatic, hormone receptor positive, HER2-low or HER2- ultralow: Treatment of unresectable or metastatic human epidermal growth factor receptor 2 (HER2)-low (immunohistochemical [IHC] 1+ or IHC 2+ and negative in situ hybridization [ISH-]) or HER2-ultralow (IHC 0 with membrane staining) breast cancer (as determined by an approved test) in adults with progression on ≥1 endocrine therapies in the metastatic setting.

Breast cancer, unresectable or metastatic, HER2-low: Treatment of unresectable or metastatic HER2-low (IHC 1+ or IHC 2+/ISH-) breast cancer (as determined by an approved test) in adults who have received a prior chemotherapy in the metastatic setting or developed disease recurrence during or within 6 months of completing adjuvant chemotherapy.

Breast cancer, unresectable or metastatic, HER2-positive : Treatment of unresectable or metastatic HER2-positive (IHC 3+ or ISH positive) breast cancer in adults who have received a prior anti–HER2-based regimen either in the metastatic setting, or in the neoadjuvant or adjuvant setting and have developed disease recurrence during or within 6 months of completing therapy.

Gastric cancer, locally advanced or metastatic, HER2-positive: Treatment of locally advanced or metastatic HER2-positive (IHC 3+ or IHC 2+ and ISH positive) gastric or gastroesophageal junction adenocarcinoma in adults who have received a prior trastuzumab-based regimen.

Non–small cell lung cancer, unresectable or metastatic, HER2 (ERBB2)-mutation positive: Treatment of unresectable or metastatic non–small cell lung cancer with activating HER2 (ERBB2) mutations (as detected by an approved test) in adults who have received a prior systemic therapy.

Solid tumors, unresectable or metastatic, HER2- positive: Treatment of unresectable or metastatic HER2-positive (IHC 3+) solid tumors in adults who have received prior systemic treatment and have no satisfactory alternative treatment options.

Medication Safety Issues

Sound-alike/look-alike issues:

Fam-trastuzumab deruxtecan may be confused with ado-trastuzumab emtansine, brentuximab vedotin, datopotamab deruxtecan, pertuzumab, pertuzumab/trastuzumab/hyaluronidase, sacituzumab govitecan, trastuzumab (conventional [or trastuzumab biosimilars]), trastuzumab/hyaluronidase.

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).

Other safety concerns:

Fam-trastuzumab deruxtecan (Enhertu) may be confused with ado-trastuzumab emtansine (Kadcyla), conventional trastuzumab (Herceptin), pertuzumab/trastuzumab/hyaluronidase (Phesgo), trastuzumab biosimilars, and/or trastuzumab/hyaluronidase (Herceptin Hylecta); products are not interchangeable.

Metabolism/Transport Effects

Substrate of BCRP, CYP3A4 (Minor), OATP1B1/1B3, P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;

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

Abrocitinib: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid

Anthracyclines: Fam-Trastuzumab Deruxtecan may increase cardiotoxic effects of Anthracyclines. Management: When possible, patients treated with fam-trastuzumab deruxtecan should avoid anthracycline-based therapy for up to 7 months after stopping fam-trastuzumab deruxtecan. Monitor closely for cardiac dysfunction in patients receiving this combination. Risk D: Consider Therapy Modification

Antithymocyte Globulin (Equine): Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Antithymocyte Globulin (Equine). Specifically, these effects may be unmasked if the dose of immunosuppressive therapy is reduced. Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Antithymocyte Globulin (Equine). Specifically, infections may occur with greater severity and/or atypical presentations. Risk C: Monitor

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

Baricitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Baricitinib. Risk X: Avoid

BCG Products: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of BCG Products. Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Brincidofovir: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Brincidofovir. Risk C: Monitor

Brivudine: May increase adverse/toxic effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid

Chikungunya Vaccine (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Chikungunya Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Chikungunya Vaccine (Live). Risk X: Avoid

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: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Cladribine. Risk X: Avoid

CloZAPine: Myelosuppressive Agents may increase adverse/toxic effects of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor

Coccidioides immitis Skin Test: Coadministration of Immunosuppressants (Miscellaneous Oncologic Agents) and Coccidioides immitis Skin Test may alter diagnostic results. Management: Consider discontinuing these oncologic agents several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider Therapy Modification

COVID-19 Vaccine (Inactivated Virus): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of COVID-19 Vaccine (Inactivated Virus). Risk C: Monitor

COVID-19 Vaccine (mRNA): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of COVID-19 Vaccine (mRNA). Management: Give a 3-dose primary series for all patients aged 6 months and older taking immunosuppressive medications or therapies. Booster doses are recommended for certain age groups. See CDC guidance for details. Risk D: Consider Therapy Modification

COVID-19 Vaccine (Subunit): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of COVID-19 Vaccine (Subunit). 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

Dengue Tetravalent Vaccine (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Dengue Tetravalent Vaccine (Live). Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Denosumab: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and immunosuppressants. If combined, monitor patients for signs/symptoms of serious infections. Risk D: Consider Therapy Modification

Deucravacitinib: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid

Efgartigimod Alfa: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor

Etrasimod: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid

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

Filgotinib: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid

Inebilizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Inebilizumab. Risk C: Monitor

Influenza Virus Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating immunosuppressants if possible. If vaccination occurs less than 2 weeks prior to or during therapy, revaccinate at least 3 months after therapy discontinued if immune competence restored. Risk D: Consider Therapy Modification

Leflunomide: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents. Risk D: Consider Therapy Modification

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

Mumps- Rubella- or Varicella-Containing Live Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Mumps- Rubella- or Varicella-Containing Live Vaccines may increase adverse/toxic effects of Immunosuppressants (Miscellaneous Oncologic Agents). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Nadofaragene Firadenovec: Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Nadofaragene Firadenovec. Specifically, the risk of disseminated adenovirus infection may be increased. Risk X: Avoid

Natalizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Natalizumab. Risk X: Avoid

Nipocalimab: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor

Ocrelizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Ocrelizumab. Risk C: Monitor

Ofatumumab: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Ofatumumab. Risk C: Monitor

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

Pidotimod: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Pidotimod. Risk C: Monitor

Pimecrolimus: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid

Pneumococcal Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Pneumococcal Vaccines. Risk C: Monitor

Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Polymethylmethacrylate: Immunosuppressants (Miscellaneous Oncologic Agents) may increase hypersensitivity effects of Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider Therapy Modification

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

Rabies Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider Therapy Modification

Ritlecitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Ritlecitinib. Risk X: Avoid

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

Rozanolixizumab: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor

Ruxolitinib (Topical): Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Ruxolitinib (Topical). Risk X: Avoid

Sipuleucel-T: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants prior to initiating sipuleucel-T therapy. Risk D: Consider Therapy Modification

Sphingosine 1-Phosphate (S1P) Receptor Modulators: May increase immunosuppressive effects of Immunosuppressants (Miscellaneous Oncologic Agents). Risk C: Monitor

Tacrolimus (Topical): Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Tacrolimus (Topical). Risk X: Avoid

Talimogene Laherparepvec: Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid

Tertomotide: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Tertomotide. Risk X: Avoid

Tofacitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Tofacitinib. Risk X: Avoid

Typhoid Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Typhoid Vaccine. Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Ublituximab: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Ublituximab. Risk C: Monitor

Upadacitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may increase immunosuppressive effects of Upadacitinib. Risk X: Avoid

Vaccines (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Vaccines (Live). Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Vaccines (Non-Live/Inactivated/Non-Replicating): Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Vaccines (Non-Live/Inactivated/Non-Replicating). Management: Give non-live/inactivated/non-replicating vaccines at least 2 weeks prior to initiation of immunosuppressants when possible. Patients vaccinated less than 14 days before or during therapy should be revaccinated at least 3 months after therapy is complete. Risk D: Consider Therapy Modification

Yellow Fever Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Yellow Fever Vaccine. Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Zoster Vaccine (Live/Attenuated): Immunosuppressants (Miscellaneous Oncologic Agents) may increase adverse/toxic effects of Zoster Vaccine (Live/Attenuated). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may decrease therapeutic effects of Zoster Vaccine (Live/Attenuated). Risk X: Avoid

Reproductive Considerations

In utero exposure to fam-trastuzumab deruxtecan can result in embryo-fetal harm. Advise patients of these risks and the need for effective contraception.

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 7 months after the last fam-trastuzumab deruxtecan dose. Patients with partners who could become pregnant should use effective contraception during therapy and for 4 months after the last dose of fam-trastuzumab deruxtecan.

Pregnancy Considerations

Based on the mechanism of action and postmarketing data, in utero exposure to fam-trastuzumab deruxtecan can result in embryo-fetal harm. Advise patients of these risks and the need for effective contraception.

Oligohydramnios and oligohydramnios sequence (manifested as pulmonary hypoplasia, skeletal malformations, and neonatal death) were observed following trastuzumab exposure during pregnancy (trastuzumab is the antibody component of fam-trastuzumab deruxtecan). Monitor for oligohydramnios if trastuzumab exposure occurs during pregnancy or within 7 months prior to conception; conduct appropriate fetal testing if oligohydramnios occurs.

Breastfeeding Considerations

It is not known if fam-trastuzumab deruxtecan 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 7 months after the last fam-trastuzumab deruxtecan dose.

Monitoring Parameters

HER2 status:

**Fam-Trastuzumab Deruxtecan Selection Criteria for Treatment^a**
Indication	Patient selection criteria	Specimen type
^aERBB2 = erythroblastic leukemia viral oncogene 2; HER2 = human epidermal growth factor 2; IHC = immunohistochemical; ISH = in situ hybridization
^b Reassess HER2 status if feasible to obtain a new tumor specimen after prior trastuzumab-based therapy and before treatment with fam-trastuzumab deruxtecan.
^c If no mutation is detected in the plasma specimen, test tumor tissue.
Breast cancer, unresectable or metastatic, hormone receptor positive, HER2-low or HER2-ultralow	HER2 expression: HER2-low: IHC 1+ or IHC 2+/ISH- HER2-ultralow: IHC 0 with membrane staining	Tumor
Breast cancer, unresectable or metastatic, HER2-low	HER2 expression: HER2-low: IHC 1+ or IHC 2+/ISH-	Tumor
Breast cancer, unresectable or metastatic, HER2-positive	HER2 expression: IHC 3+ or ISH positive	Tumor
Gastric cancer, locally advanced or metastatic, HER2-positive	HER2 protein overexpression or HER2 gene amplification: IHC 3+ or IHC 2+/ISH positive^b	Tumor
Non–small cell lung cancer, unresectable or metastatic, HER2 (ERBB2)-mutation positive	Presence of activating HER2 (ERBB2) mutations	Tumor or plasma^c
Solid tumors, unresectable or metastatic, HER2-positive	HER2 expression: IHC 3+	Tumor

CBC (prior to treatment initiation, prior to each dose, and as clinically indicated). Assess left ventricular ejection fraction prior to fam-trastuzumab deruxtecan initiation and at regular intervals during treatment as clinically indicated. Evaluate pregnancy status prior to therapy (in patients who could become pregnant). Monitor for signs/symptoms of interstitial lung disease/pneumonitis (eg, cough, dyspnea, fever, and/or any new or worsening respiratory symptoms [particularly in patients with kidney impairment]; promptly investigate and obtain radiographic imaging for suspected interstitial lung disease). Monitor for infusion reactions.

Additional cardiovascular monitoring (guideline recommendations): 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 a baseline echocardiography (transthoracic preferred) and repeat every 3 months during treatment (may reduce to every 4 to 6 months if normal and asymptomatic), assess more frequently if clinically indicated and obtain echocardiography within 12 months after completion; in high- and very high-risk patients, assess troponin and natriuretic peptide at baseline and consider assessing every 2 to 3 cycles, and at 3 and 12 months after completion of therapy; in low- and moderate-risk patients, consider troponin and natriuretic peptide at baseline (post-anthracycline), every 3 months and 12 months after completion of therapy (ESC [Lyon 2022]).

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

Fam-trastuzumab deruxtecan is a HER2-directed antibody-drug conjugate composed of a humanized IgG1 monoclonal antibody, which has the same amino acid sequence as trastuzumab (and targets HER2), a cleavable tetrapeptide-based linker, and the cytotoxic component, a topoisomerase I inhibitor (Modi 2020). The deruxtecan component is a cleavable linker and the topoisomerase inhibitor, DXd (an exatecan derivative). Upon binding to HER2 on tumor cells, fam-trastuzumab deruxtecan undergoes internalization and intracellular linker cleavage by lysosomal enzymes, releasing DXd and resulting in DNA damage and cell death.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: V_d: Fam-trastuzumab deruxtecan: 2.68 L.

Protein binding: DXd: ~97% (to plasma proteins).

Metabolism: Fam-trastuzumab deruxtecan: Degradation via catabolic pathways into small peptides and amino acids; DXd: Primarily via CYP3A4.

Half-life elimination: Fam-trastuzumab deruxtecan: 5.4 to 5.7 days; DXd: 5.4 to 6.1 days.

Excretion: Clearance: Fam-trastuzumab deruxtecan: 0.41 L/day; DXd: 18.3 L/hour.

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Enhertu;
(AR) Argentina: Enhertu;
(AT) Austria: Enhertu;
(BE) Belgium: Enhertu;
(BG) Bulgaria: Enhertu;
(BR) Brazil: Enhertu;
(CH) Switzerland: Enhertu;
(CZ) Czech Republic: Enhertu;
(EE) Estonia: Enhertu;
(EG) Egypt: Enhertu;
(ES) Spain: Enhertu;
(FI) Finland: Enhertu;
(FR) France: Enhertu;
(GB) United Kingdom: Enhertu;
(HK) Hong Kong: Enhertu;
(HU) Hungary: Enhertu;
(IE) Ireland: Enhertu;
(IT) Italy: Enhertu;
(JO) Jordan: Enhertu;
(JP) Japan: Enhertu;
(KW) Kuwait: Enhertu;
(LT) Lithuania: Enhertu;
(LV) Latvia: Enhertu;
(MX) Mexico: Enhertu;
(NL) Netherlands: Enhertu;
(NO) Norway: Enhertu;
(NZ) New Zealand: Enhertu;
(PR) Puerto Rico: Enhertu;
(PT) Portugal: Enhertu;
(QA) Qatar: Enhertu;
(RO) Romania: Enhertu;
(RU) Russian Federation: Enhertu;
(SA) Saudi Arabia: Enhertu;
(SE) Sweden: Enhertu;
(SG) Singapore: Enhertu;
(SI) Slovenia: Enhertu;
(SK) Slovakia: Enhertu;
(TW) Taiwan: Enhertu

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Fam-trastuzumab deruxtecan: Drug information