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Updated: Feb 5, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

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Published on: September 18, 2013

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Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application

Wei Yan1, Naga Rajiv Lakkaniga1, Francesca Carlomagno2,3

  • 1Department of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.

Journal of Medicinal Chemistry
|September 7, 2018
PubMed

Insights

Tropomyosin receptor kinase (TRK) precision medicine targets cancers with TRK genomic rearrangements. This perspective reviews TRK biology, inhibitors, clinical trials, and future drug development for TRK-driven cancers.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Kinase-directed precision medicine, exemplified by imatinib, has transformed cancer therapy.
  • Tropomyosin receptor kinase (TRK) gene rearrangements are found in approximately 20,000 cancer cases annually.
  • TRK alterations represent a significant target for precision oncology.

Purpose of the Study:

  • To provide a comprehensive overview of TRK precision medicine.
  • To discuss the biological significance of the TRK kinase family.
  • To outline current and future directions in TRK inhibitor development.

Main Methods:

  • Review of existing literature on TRK biology and inhibitors.
  • Analysis of cocrystal structures of TRK inhibitors.
  • Compilation and summary of ongoing TRK clinical trials.

Main Results:

  • The TRK kinase family plays a crucial role in various cancers driven by genomic rearrangements.
  • Multiple TRK inhibitors are in development, with structural insights guiding their design.
  • Clinical trials demonstrate the efficacy of TRK inhibitors in relevant patient populations.

Conclusions:

  • TRK inhibitors represent a successful example of kinase-directed precision medicine.
  • Continued research into TRK biology and inhibitor development is essential for advancing cancer treatment.
  • Future drug discovery efforts will focus on overcoming resistance and expanding therapeutic applications.

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