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Last Updated: 01/25/17

Information below provided by the Pharmaceutical Company.

Larotrectinib (LOXO-101)

Agent Description

Larotrectinib is a potent, oral and selective investigational agent in clinical development for the treatment of patients with cancers that harbor abnormalities involving the tropomyosin receptor kinases (TRKs).

Mechanism of Action

ATP-competitive kinase inhibitor of TrkA/B/C

Classification

small molecule, tyrosine kinase inhibitor

Molecular Targets

NTRK-1, NTRK-2, NTRK-3 fusion proteins; TrkA/B/C proteins

Monograph

Larotrectinib (LOXO-101) is currently being studied in both adults and pediatrics (aged >1 month of age) in on-going phase 1 and phase 2 trials. Larotrectinib will also be studied in the ECOG-ACRIN NCI Adult MATCH and the COG-NCI Pediatric MATCH phase 2 trials. Larotrectinib has received FDA Breakthrough Therapy Designation for the treatment of unresectable or metastatic solid tumors with NTRK-fusion proteins in adult and pediatric patients who require systemic therapy and who have either progressed following prior treatment or who have no acceptable alternative treatments. Larotrectinib has low nanomolar potency against TrkA (NTRK1), TrkB (NTRK2), and TrkC (NTRK3) with no other kinase inhibition at physiologically achievable doses. Larotrectinib is available in both capsule and liquid formulations.

Studies of Interest

N/A

Information collaborator would like included in investigator proposals

N/A