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Updated: Jun 22, 2025

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
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FAK inhibitors in cancer, a patent review - an update on progress

Ya-Xi Ye1, Yu-Yao Cao2, Li-Sheng Xu1

  • 1Institute of Pharmaceutical Biotechnology, School of Biology and Food Engineering, Suzhou University, Suzhou, PR China.

Expert Opinion on Therapeutic Patents
|July 1, 2024
PubMed
Abstract

Insights

Focal adhesion kinase (FAK) inhibitors show promise for cancer treatment. Recent research focuses on the design, synthesis, and structure-activity relationships of these chemotherapeutic agents for improved cancer therapy.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Biochemistry

Background:

  • Focal adhesion kinase (FAK) is a cytoplasmic non-receptor tyrosine kinase.
  • FAK is over-expressed in various malignancies, influencing cell adhesion, metastasis, and proliferation.
  • FAK is recognized as a promising therapeutic target for cancer treatment.

Purpose of the Study:

  • To provide an updated overview of chemotherapeutic FAK inhibitors (FAKIs).
  • To summarize the design, synthesis, and structure-activity relationships of FAKIs from 2017 to the present.
  • To offer insights for future cancer treatment strategies from a medicinal chemistry perspective.

Main Methods:

  • Review of recent patents and literature on FAKIs.
  • Analysis of design and synthesis strategies for FAKIs.
  • Evaluation of structure-activity relationships of identified FAKIs.

Main Results:

  • A variety of FAKIs have been patented recently.
  • FAK inhibitors are progressing into clinical research phases.
  • Understanding FAKI design and SAR is crucial for drug development.

Conclusions:

  • FAK is a viable target for medicinal chemistry research in oncology.
  • Continued development of FAKIs holds potential for novel cancer therapies.
  • This review aims to broaden the understanding and inspire future research in FAKI development.
Keywords:
Focal adhesion kinase (FAK)cancer treatmentchemotherapeutic FAK inhibitorsnon-receptor tyrosine kinasetherapeutic target

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