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Larotrectinib

Tyrosine Kinase Inhibitor · Antineoplastic agent

Tyrosine Kinase InhibitorAntineoplastic agent
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Manufacturer advises avoid—limited information available.
FDA category + note
Top interactionssee all 12
  • AmprenavirSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter
  • BoceprevirSevereDatabaseDDInter

Mechanism

Larotrectinib is a tropomyosin receptor kinase inhibitor.

Indications

Solid tumours with neurotrophic tyrosine receptor kinase gene fusion (initiated by a specialist)systemic therapy of follicular cell-derived thyroid cancers with NTRK fusion gene driver mutationsany cancers with TRK gene fusions without resistance mutation

Dosing

Adult
100 mg twice daily. For dose adjustments, treatment interruption, or discontinuation due to side-effects, consult product literature. If concomitant use with potent CYP3A4 inhibitors is unavoidable, reduce dose by 50%.

Pharmacokinetics

Half-life
2.9 h
Metabolism
Metabolized via CYP3A4. Larotrectinib also decreases the metabolism of other antineoplastic agents.

Contraindications

  • Pregnancy
  • Breastfeeding

Side effects

Common
AnaemiaArthralgiaConstipationCoughDiarrhoeaDizzinessFatigueGait abnormalLeucopeniaMuscle weaknessMyalgiaNauseaNeutropeniaParaesthesiaTaste alteredVomitingWeight increased
Serious
  • Liver dysfunction (monitoring advised)
  • neurotoxicity
  • hepatotoxicity

Pregnancy & lactation

Pregnancy

Manufacturer advises avoid—limited information available.

Lactation

Manufacturer advises avoid during treatment and for 3 days after last treatment—no information available.

Drug interactions

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Clarithromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Conivaptan
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Delavirdine
Severe
Database

Clinical effect not specified

Source: DDInter

Enzalutamide
Severe
Database

Clinical effect not specified

Source: DDInter

Fosamprenavir
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Tyrosine Kinase Inhibitor drugs

Ask House about Larotrectinib

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