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FAK inhibitors in Cancer, a patent review

Peng-Cheng Lv1,2, Ai-Qin Jiang1,2, Wei-Ming Zhang1,2

  • 1a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing P. R. China.

Expert Opinion on Therapeutic Patents
|December 7, 2017
PubMed
Abstract

Insights

Small molecule inhibitors targeting focal adhesion kinase (FAK) show promise in cancer therapy. Recent research focuses on their design, synthesis, and clinical development for treating aggressive tumors.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase involved in cell adhesion and ECM signaling.
  • FAK regulates critical cell functions including survival, proliferation, and migration.
  • Elevated FAK expression is observed in numerous cancer types, correlating with tumor aggressiveness.

Purpose of the Study:

  • To review recent advancements in small molecule FAK inhibitors.
  • To analyze the design, synthesis, and structure-activity relationships (SAR) of FAK inhibitors from 2015 onwards.
  • To provide an update on FAK inhibitors in clinical development and future prospects.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Analysis of structure-activity relationships for small molecule FAK inhibitors.
  • Synthesis and characterization of novel FAK inhibitors (implied).

Main Results:

  • Small molecule FAK inhibitors induce tumor cell apoptosis.
  • FAK inhibitors effectively reduce metastasis and angiogenesis.
  • Several FAK inhibitors are progressing through clinical trials for cancer treatment.

Conclusions:

  • FAK is a validated therapeutic target for anticancer strategies.
  • Small molecule FAK inhibitors represent a promising class of anticancer agents.
  • Continued research and clinical development are crucial for FAK inhibitor-based therapies.
Keywords:
Anticancer agentscancer therapyfocal adhesion kinase (FAK)non-receptor tyrosine kinasesmall molecule FAK inhibitors

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