Related Experiment Video

Updated: Jan 29, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

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TRK Inhibitors: Clinical Development of Larotrectinib

Munveer S Bhangoo1, Darren Sigal2

  • 1Scripps Clinic, Division of Hematology-Oncology, 10666 North Torrey Pines Road, La Jolla, CA, 92037, USA.

Current Oncology Reports
|February 5, 2019
PubMed
Abstract

Insights

Larotrectinib shows significant clinical activity in cancers with NTRK gene fusions. Screening for these fusions is crucial for identifying patients who can benefit from this targeted therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Genetics

Background:

  • Tropomyosin receptor kinases (TrkA, TrkB, TrkC) are key in neuronal development.
  • NTRK gene fusions are driver mutations in various cancers.
  • NTRK alterations are rare but significant in oncogenesis.

Purpose of the Study:

  • To review the pre-clinical development of larotrectinib.
  • To highlight recent clinical studies of larotrectinib.
  • To discuss future directions for larotrectinib in NTRK fusion-positive tumors.

Main Methods:

  • Review of pre-clinical data.
  • Analysis of recent clinical trial results.
  • Synthesis of current literature on NTRK fusions and larotrectinib.

Main Results:

  • Larotrectinib, a Trk inhibitor, demonstrates broad clinical activity.
  • NTRK fusion-positive tumors show exceptional response to larotrectinib.
  • NTRK alterations are identified as a predictive biomarker across diverse malignancies.

Conclusions:

  • Larotrectinib is a highly effective targeted therapy for NTRK fusion-positive cancers.
  • NTRK gene fusions represent an important actionable biomarker.
  • Screening for NTRK alterations is recommended for any cancer patient.
Keywords:
LarotrectinibNTRKPersonalized medicinePrecision medicineTRK inhibitorTargeted oncology

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