Related Experiment Video

Updated: Mar 10, 2026

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down
08:59

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down

Published on: December 11, 2017

7.7K

Disarming cancer resistance: FAK as a therapeutic target

Terrance J Haanen1, David D Schlaepfer1

  • 1Department of Obstetrics, Gynecology, and Reproductive Sciences, Division of Gynecologic Oncology, University of California, San Diego, Moores Cancer Center, 3855 Health Sciences Drive, MC0803, La Jolla, CA 92093, USA.

Trends in Cancer
|March 9, 2026
PubMed

Insights

Focal adhesion kinase inhibitors (FAKi) show promise in combination therapies for ovarian cancer. Targeting FAK disarms tumor resistance, offering new avenues for treatment against KRAS-mutated cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Development

Background:

  • Focal adhesion kinase (FAK) plays a crucial role in tumor progression and resistance.
  • Recent FDA accelerated approval highlights advancements in FAK inhibitor (FAKi) therapy.
  • FAKi, like defactinib, are being explored in combination treatments for various cancers.

Purpose of the Study:

  • To review the history and development of FAK inhibitors.
  • To summarize ongoing clinical trials involving FAK inhibitors in combination therapies.
  • To discuss the mechanisms of action and potential of FAK targeting in overcoming tumor resistance.

Main Methods:

  • Literature review of FAK inhibitor development and clinical trials.
  • Analysis of studies investigating FAK activation as a signaling hub.
  • Discussion of FAK's role in tumor adaptive changes and resistance mechanisms.

Main Results:

  • FAK inhibitors have evolved from limited single-agent activity to sensitizing tumors to various treatments.
  • FAK activation is identified as a key signaling hub sensitive to chemotherapy and mechanical stress.
  • Targeting FAK demonstrates potential to disarm tumor resistance through multiple pathways.

Conclusions:

  • FAK inhibitors represent a significant advancement in cancer therapy, particularly in combination regimens.
  • Understanding FAK's role in chemo- and mechano-sensitivity provides new biological insights.
  • Future clinical combinations targeting FAK hold promise for improved cancer treatment outcomes.
Keywords:
FAKRAFRASadaptive resistanceavutometinibdefactinib

More Related Videos

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

11.2K
Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence10:09

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence

Published on: January 7, 2019

8.8K

Related Concept Videos

Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.9K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.0K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
6.3K
Adaptive Mechanisms in Cancer Cells02:53

Adaptive Mechanisms in Cancer Cells

Cancer cells accumulate genetic changes at an abnormally rapid rate due to the defects in the DNA repair mechanisms. From an evolutionary perspective, such genetic instability is advantageous for cancer development. Mutant cell lines accumulate a series of beneficial mutations that contribute to their progression into cancer.
Some of the advantages that cancer cells have on normal cells include - enhanced ability to divide without terminally differentiating, induce new blood vessel formation,...
7.3K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
8.3K
Tumor Immunotherapy01:27

Tumor Immunotherapy

Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
2.1K