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tucatinib

HER2 selective TKI · Antineoplastic agent

HER2 selective TKIAntineoplastic agent
CDSCO approved
EXCRETION
—
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
D
FDA category + note
Top interactionssee all 12 →
  • AbemaciclibSevereDatabaseDDInter
  • AbirateroneSevereDatabaseDDInter
  • AcalabrutinibSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter

Mechanism

Tucatinib is an orally bioavailable, reversible, highly selective TKI of HER2 with minimal inhibition of EGFR (HER1).

Indications

unresectable or metastatic HER2-positive breast cancers, including patients with brain metastases and pretreated patients (in combination with trastuzumab)

Pharmacokinetics

Half-life
8.5 h
Metabolism
CYP2C8 (mostly), CYP3A (less)

Side effects

Common
diarrhea
Serious
  • hepatotoxicity

Pregnancy & lactation

Pregnancy

D

Drug interactions

Abemaciclib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Abiraterone
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Acalabrutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Alfuzosin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apixaban
Severe
Database

Drug interaction classified as: absorption, metabolism

Source: DDInter

Artemether
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Avanafil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Avapritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Axitinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Benzhydrocodone
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Breast cancer
ESMO · Oncology · 2024
Breast cancer
ICMR · Oncology · 2022
Infant and child nutrition
ICMR · Pediatrics · 2024
Preoperative cardiac evaluation for non-cardiac surgery
AHA · Cardiology · 2025
Systemic lupus erythematosus
EULAR · Rheumatology · 2023

Ask House about tucatinib

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team