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Enhertu (fam-trastuzumab deruxtecan-nxki)
fam-trastuzumab deruxtecan
Black Box Warnings .
Interstitial Lung Disease
including fatal cases have occurred; monitor for new or worsening respiratory signs/symptoms including cough, dyspnea, fever; permanently D/C tx if Grade 2 or higher interstitial lung disease or pneumonitis occurs; advise patients of risk and to immediately report any symptoms
Embryo-Fetal Toxicity
exposure during pregnancy can result in embryo-fetal harm; advise patients of risks and need for effective contraception
Adult Dosing .
Dosage forms: INJ
Special Note
- [drug name clarification]
- Info: nonproprietary name = fam-trastuzumab deruxtecan-nxki
- [equivalency or interchangeability info]
- Info: not interchangeable with ado-trastuzumab emtansine or other trastuzumab-containing products
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses, premeds, and dosing including toxicity-related dose adjustments
breast CA, unresectable or metastatic
- [HER2-positive disease, first-line tx]
- Dose: 5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle; Info: give with pertuzumab
- [HER2-positive progressive disease]
- Dose: 5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle; Info: for patients who have received prior anti-HER2-based regimen
- [HER2-low disease]
- Dose: 5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle; Info: for patients with IHC1+ or IHC2+/ISH-negative disease who have received prior tx
- [hormone receptor-positive HER2-low disease]
- Dose: 5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle; Info: for patients with IHC1+ or IHC2+/ISH-negative disease who have progressed on prior endocrine-based tx
- [hormone receptor-positive HER2-ultralow disease]
- Dose: 5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle; Info: for patients with IHC0 with membrane staining disease who have progressed on prior endocrine-based tx
HER2-mutant non-small cell lung CA, unresectable or metastatic
- [5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle]
- Info: for patients with activating HER2 (ERBB2) mutations who have received prior tx
HER2-positive gastric CA, locally advanced or metastatic
- [6.4 mg/kg/dose IV x1 on day 1 of 21-day cycle]
- Info: for patients with gastric or gastroesophageal junction adenocarcinoma who have received prior trastuzumab-based regimen
HER2-positive solid tumors, unresectable or metastatic
- [5.4 mg/kg/dose IV x1 on day 1 of 21-day cycle]
- Info: for patients with IHC3+ disease who have received prior tx and have no alternative tx options
renal dosing
- [see below]
- CrCl >30: no adjustment; CrCl <30: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- bilirubin 1.1-3x ULN or AST >ULN: no adjustment; bilirubin >3x ULN: not defined
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- avoid: breastfeeding during tx and x7mo after D/C
- caution: patients of childbearing potential
- caution: male patients of reproductive potential
- caution: CrCl <60
- caution: bilirubin >1.5x ULN
Drug Interactions .
Overview
fam-trastuzumab deruxtecan
HER2-directed antibody; topoisomerase inhibitor
- cardiotoxic effects
- immunomodulatory effects
- myelosuppressive oncologic agent
Avoid/Use Alternative
- adenovirus vaccine, live
- ado-trastuzumab emtansine
- chikungunya vaccine, live
- chloramphenicol
- cholera vaccine, live
- cladribine oral
- deferiprone
- dengue vaccine, live
- dexrazoxane
- doxorubicin
- epirubicin
- fam-trastuzumab deruxtecan
- fexinidazole
- ganciclovir
- idarubicin
- influenza nasal vaccine, live
- measles/mumps/rubella vaccine, live
- palifermin
- penicillamine
- primaquine
- rabies vaccine
- radium Ra 223 dichloride
- ropeginterferon alfa-2b
- rotavirus vaccine, live
- smallpox vaccine, live
- trastuzumab
- typhoid vaccine, live
- valganciclovir
- varicella vaccine, live
- yellow fever vaccine, live
Monitor/Modify Tx
- adalimumab
- aficamten
- albendazole
- aldesleukin
- alemtuzumab
- allopurinol
- alogliptin
- anagrelide
- anthrax vaccine
- anti-thymocyte globulin
- asciminib
- atidarsagene autotemcel
- auranofin
- avelumab
- avian influenza vaccine
- axitinib
- azathioprine
- balsalazide
- baricitinib
- benznidazole
- betibeglogene autotemcel
- bevacizumab
- bezlotoxumab
- binimetinib
- bortezomib
- bosutinib
- capecitabine
- carfilzomib
- certolizumab pegol
- chikungunya vaccine
- cidofovir
- cilostazol
- clozapine
- cobimetinib
- colchicine
- copper histidinate
- COVID-19 vaccine
- cyclophosphamide
- dabrafenib
- dapsone
- daunorubicin
- deferasirox
- deuruxolitinib
- diphtheria/tetanus vaccine
- diphtheria/tetanus/pertussis vaccine
- dronedarone
- ebola vaccine, live
- efbemalenograstim alfa
- eflapegrastim (G-CSF)
- elivaldogene autotemcel
- encorafenib
- entrectinib
- etanercept
- etuvetidigene autotemcel
- everolimus
- exagamglogene autotemcel
- filgrastim (G-CSF)
- flucytosine
- fluorouracil
- fluphenazine
- foscarnet
- fosfomycin injection
- fostamatinib
- givinostat
- golimumab
- Haemophilus b vaccine
- hepatitis A vaccine
- hepatitis B vaccine
- human papillomavirus vaccine
- hydroxychloroquine
- hydroxyurea
- ibrutinib
- ifosfamide
- imatinib
- infliximab
- influenza vaccine
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- itraconazole
- Japanese encephalitis vaccine
- lapatinib
- leflunomide
- lenvatinib
- linagliptin
- linezolid
- lonafarnib
- lovotibeglogene autotemcel
- lymphocyte immune globulin, anti-thymocyte globulin
- margetuximab
- marnetegragene autotemcel
- mavacamten
- meningococcal vaccine
- mercaptopurine
- mesalamine
- mesalamine rectal
- methotrexate
- mirdametinib
- mitoxantrone
- mobocertinib
- mycophenolate mofetil
- mycophenolic acid
- olsalazine
- osimertinib
- pazopanib
- pegfilgrastim (G-CSF)
- peginterferon alfa 2a
- peginterferon beta 1a
- pentamidine
- pertuzumab
- pioglitazone
- pneumococcal vaccine
- poliovirus vaccine
- ponatinib
- proguanil
- propafenone
- pyrimethamine
- respiratory syncytial virus vaccine
- ribavirin
- rifabutin
- ripretinib
- rituximab
- rosiglitazone
- ruxolitinib topical
- sargramostim (GM-CSF)
- sarilumab
- satralizumab
- saxagliptin
- selumetinib
- sirolimus
- sitagliptin
- smallpox/mpox vaccine, live
- sorafenib
- stiripentol
- succimer
- sulfasalazine
- sunitinib
- teplizumab
- teriflunomide
- thalidomide
- tick-borne encephalitis vaccine
- tivozanib
- tocilizumab
- tofacitinib
- trabectedin
- trametinib
- trimethoprim
- typhoid vaccine
- upadacitinib
- valproic acid
- vancomycin
- vandetanib
- zanidatamab
- zenocutuzumab
- zidovudine
- zongertinib
Adverse Reactions .
Serious Reactions
- interstitial lung disease
- pneumonitis
- pneumonia
- pulmonary embolism
- pleural effusion
- dyspnea
- neutropenia
- febrile neutropenia
- infection, serious
- anemia
- thrombocytopenia
- lymphopenia
- hemorrhage
- myocarditis
- left ventricular dysfunction
- hypokalemia
- peripheral neuropathy
- intestinal obstruction
- intestinal ischemia
- edema
Common Reactions
- nausea
- fatigue
- alopecia
- vomiting
- constipation
- URI
- appetite decr.
- diarrhea
- anemia
- musculoskeletal pain
- abdominal pain
- headache
- stomatitis
- cough
- interstitial lung disease
- respiratory infection
- weight decr.
- rash
- dizziness
- dyspepsia
- dyspnea
- epistaxis
- fever
- dysgeusia
- COVID-19
- pruritus
- edema
- peripheral neuropathy
- dry eyes
- hypoalbuminemia
- blurred vision
- skin hyperpigmentation
- hemorrhage
- dehydration
- abdominal distension
- neutrophils decr.
- lymphocytes decr.
- Plt decr.
- ALT or AST incr.
- alk phos incr.
- potassium decr.
- Hgb decr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; CBC with diff at baseline, prior to each dose, and as clinically indicated; LVEF at baseline, then at regular intervals as clinically indicated; signs/symptoms of interstitial lung disease
Look/Sound-Alike Drug Names
fam-trastuzumab deruxtecan confused with: trastuzumab, ado-trastuzumab emtansine
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available, though risk of oligohydramnios and oligohydramnios sequence based on limited human data with trastuzumab
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x7mo after D/C in patients of childbearing potential and during tx and x4mo after D/C in male patients
Lactation
Clinical Summary
avoid breastfeeding during tx and x7mo after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for fam-trastuzumab deruxtecan: catabolism; CYP450: unknown; Info: active drug deruxtecan (CYP3A4 substrate)
Excretion: for fam-trastuzumab deruxtecan: unknown; Half-life: 5.4-5.7 days (fam-trastuzumab deruxtecan), 5.4-6.1 days (deruxtecan)
Subclass: HER2 Antagonists ; Immunotherapy, Antibody-Drug Conjugates ; Immunotherapy, HER2 Inhibitors ; Mitosis Inhibitors, Topoisomerase I Inhibitors
Mechanism of Action
for fam-trastuzumab deruxtecan: antibody-drug conjugate binds to HER2-expressing cells, releases active drug deruxtecan intracellularly, which binds to topoisomerase I-DNA complexes, causing DNA damage and apoptosis
Formulary .
No Formulary Selected
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