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At a glance

Larotrectinib is indicated for the treatment of patients with solid tumors that have an NTRK gene fusion, are metastatic or where surgical resection is likely to result in severe morbidity, and have no alternative treatments or have progressed following treatment.

Indications
  • Solid tumors with NTRK gene fusion (metastatic or where surgical resection would cause severe morbidity, no alternative treatments or progressed following treatment)
Pharmacology

Larotrectinib is a highly selective inhibitor of TRKA, TRKB, and TRKC (IC50 5-11 nM). It inhibits chimeric TRK fusion proteins resulting from NTRK gene fusions, which act as oncogenic drivers promoting tumor cell proliferation and survival.

Dosage

Adult and Pediatric (BSA ≥1 m²):

  • 100 mg PO twice daily
  • With or without food
  • Continue until disease progression or unacceptable toxicity

Pediatric (BSA <1 m²):

  • 100 mg/m² PO twice daily

Hepatic Impairment: Moderate to severe (Child-Pugh B/C): Reduce starting dose by 50%

Side effects

Common Side Effects (>10%):

  • Increased AST/ALT (45%)
  • Anemia (42%)
  • Fatigue (37%)
  • Hypoalbuminemia (35%)
  • Increased alkaline phosphatase (30%)
  • Nausea (29%), Dizziness (28%), Vomiting (26%)
  • Cough (26%), Constipation (23%), Neutropenia (23%)
  • Diarrhea (22%), Pyrexia (18%), Dyspnea (18%)
  • Peripheral edema (15%), Increased weight (15%), Headache (14%)
  • Arthralgia (14%), Myalgia (14%), Muscular weakness (13%)
  • Decreased appetite (13%), Abdominal pain (13%), Back pain (12%)
  • Pain in extremity (12%), Hypertension (11%)
Use in pregnancy

Use in Pregnancy: Can cause embryo-fetal harm when administered to pregnant women. Verify pregnancy status and use effective contraception (for 1 week after the last dose).

Precautions & warnings
  • Monitor for neurologic adverse reactions (occur in 53% of patients; most within first 3 months)
  • Do not drive or operate hazardous machinery if experiencing neurologic reactions
  • Monitor liver tests for hepatotoxicity (every 2 weeks during first month, then monthly)
  • Can cause fetal harm in pregnant women
Overdose effects

No specific overdose information available; symptomatic and supportive measures should be employed.

Storage conditions

Store below 30°C in a cool and dry place, away from sunlight; keep out of reach of children.

Larotrectinib — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.