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Updated: Oct 26, 2025

Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
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Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment

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FAK inhibitors as promising anticancer targets: present and future directions

Muhamad Mustafa1,2, Amer Ali Abd El-Hafeez3,4, Dalia A Abdelhafeez5

  • 1Department of Medicinal Chemistry, Minia University, Minia, 61519, Egypt.

Future Medicinal Chemistry
|August 3, 2021
PubMed

Insights

Focal adhesion kinase (FAK) inhibitors are promising anticancer agents targeting solid tumors and metastases. This review details synthetic FAK inhibitors developed over 30 years and discusses future smart drugs to combat resistance.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Focal adhesion kinase (FAK) is a nonreceptor tyrosine kinase.
  • FAK overexpression is common in solid tumors and promotes metastasis.
  • Targeting FAK is a key strategy for developing novel anticancer drugs.

Purpose of the Study:

  • To comprehensively review synthetic compounds developed as FAK inhibitors over the past three decades.
  • To discuss the future of FAK-targeting smart drugs for cancer therapy.

Main Methods:

  • Literature review of synthetically derived FAK inhibitors.
  • Analysis of FAK's role in cancer progression and metastasis.
  • Discussion of emerging drug resistance mechanisms and future therapeutic strategies.

Main Results:

  • Multiple classes of potent synthetic FAK inhibitors have been identified.
  • FAK inhibitors show promise as therapeutic agents for various cancers.
  • The development of FAK inhibitors has advanced significantly over the last 30 years.

Conclusions:

  • FAK inhibitors represent a promising class of targeted anticancer agents.
  • Continued research into FAK inhibitors is crucial for advancing cancer treatment.
  • Future strategies will focus on smart drugs to overcome drug resistance.
Keywords:
FAK inhibitorsPROTACscancerfocal adhesion kinase

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