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Defactinib

Defactinib, also known as VS-6063, is an investigational drug being studied in clinical trials for its potential to treat various types of cancer. As a focal adhesion kinase (FAK) inhibitor, defactinib targets a protein involved in cancer cell growth and survival. This article summarizes key information about ongoing clinical trials evaluating defactinib alone or in combination with other therapies for conditions including ovarian cancer, lung cancer, mesothelioma, and other advanced solid tumors.

Table of Contents

What is Defactinib?

Defactinib, also known as VS-6063 or PF-04554878, is an investigational drug being studied for the treatment of various types of cancer[1][2]. It is taken orally, usually in the form of tablets[8]. Defactinib is not yet approved by the U.S. Food and Drug Administration (FDA) for general use, but it is being tested in clinical trials to determine its effectiveness and safety[5].

How Defactinib Works

Defactinib is a type of drug called a focal adhesion kinase (FAK) inhibitor. FAK is a protein that plays a role in cancer cell growth and survival. By blocking FAK, defactinib may help to slow down or stop the growth of cancer cells[2].

Research suggests that defactinib may also have effects on the immune system. It might help to change the environment around tumors, making it easier for the body’s immune system to fight cancer cells[9].

Cancers Treated with Defactinib

Defactinib is being studied in several types of cancer, including:

  • Non-small cell lung cancer (NSCLC): This is a common type of lung cancer[10].
  • Ovarian cancer: A type of cancer that begins in the ovaries[8].
  • Mesothelioma: A rare cancer that affects the lining of the lungs, chest wall, or abdomen[5].
  • Pancreatic cancer: A cancer that starts in the pancreas[9].
  • Thyroid cancer: Including both differentiated thyroid cancer and anaplastic thyroid cancer[7].

Clinical Trials and Research

Defactinib is currently being studied in various clinical trials. These trials are designed to test how well the drug works, what dose is best, and how safe it is. Some key areas of research include:

  • Testing defactinib in combination with other cancer drugs[4].
  • Studying how the body absorbs and processes defactinib[1].
  • Investigating defactinib’s effects in specific types of cancer, such as KRAS mutant non-small cell lung cancer[10].
  • Exploring defactinib’s potential in cancers with certain genetic changes, like NF2 mutations[6].

Combination Therapies

Researchers are particularly interested in how defactinib works when combined with other cancer treatments. Some combinations being studied include:

  • Defactinib with pembrolizumab (a type of immunotherapy)[9].
  • Defactinib with paclitaxel (a chemotherapy drug)[8].
  • Defactinib with avutometinib (another targeted therapy)[3].

These combinations are being tested to see if they can improve the effectiveness of cancer treatment compared to using single drugs alone.

Side Effects and Safety

As with all medications, defactinib can cause side effects. The full range of side effects is still being studied in clinical trials. Common side effects observed in studies include:

  • Nausea
  • Fatigue
  • Diarrhea
  • Vomiting

More serious side effects may also occur. In clinical trials, doctors closely monitor patients for any unexpected or severe side effects[2]. It’s important to note that the safety profile of defactinib is still being established through ongoing research.

If you’re considering participating in a clinical trial involving defactinib, it’s crucial to discuss potential risks and benefits with your healthcare team. They can provide the most up-to-date information about the drug and help you make an informed decision about your treatment options.

Aspect Details
Drug Name Defactinib (VS-6063)
Drug Class Focal Adhesion Kinase (FAK) Inhibitor
Administration Oral, typically twice daily
Cancer Types Studied Ovarian, Non-Small Cell Lung Cancer, Mesothelioma, Advanced Solid Tumors
Combination Therapies Paclitaxel, Pembrolizumab, Avutometinib
Key Outcomes Measured Safety, Tolerability, Pharmacokinetics, Tumor Response, Progression-Free Survival
Notable Trial Designs Dose Escalation, Expansion Cohorts, Biomarker Analysis

FAQ

  • What is defactinib and how does it work? Defactinib (VS-6063) is an investigational drug that inhibits focal adhesion kinase (FAK), a protein involved in cancer cell growth and survival. By blocking FAK, defactinib may help slow or stop the growth of certain types of cancer cells.
  • What types of cancer is defactinib being studied for? Clinical trials are evaluating defactinib for various cancers including ovarian cancer, non-small cell lung cancer, mesothelioma, and other advanced solid tumors. It is being studied both as a single agent and in combination with other cancer therapies.
  • How is defactinib administered in clinical trials? In most trials, defactinib is given as an oral medication, typically taken twice daily. The dosage and schedule may vary between studies. Some trials use a 3 weeks on, 1 week off dosing schedule.
  • What are some of the potential side effects of defactinib? As with any investigational drug, the full side effect profile is still being determined. Clinical trials are carefully monitoring for adverse events. Common side effects of cancer therapies may include fatigue, nausea, and changes in blood cell counts. Your study doctor can provide more information on potential risks.
  • How can I find out if I'm eligible for a defactinib clinical trial? Eligibility criteria vary between trials but may include factors like cancer type, stage, prior treatments, and overall health status. You can discuss clinical trial options with your oncologist or search for trials on clinicaltrials.gov using the term 'defactinib' or 'VS-6063'.

Ongoing Clinical Trials on Defactinib

  • Study Comparing Avutometinib and Defactinib with Other Treatments for Patients with Recurrent Low-Grade Serous Ovarian Cancer

    Recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    Belgium Denmark France Germany Ireland Italy +3

  • Study of Avutometinib and Defactinib for Patients with Recurrent Low-Grade Serous Ovarian Cancer

    Not recruiting

    1 1
    Investigated diseases:
    Investigated drugs:
    Belgium France Italy Spain

  • Study of Avutometinib, Sotorasib, and Defactinib for Patients with KRAS G12C Mutant Non-Small Cell Lung Cancer

    Not recruiting

    1 1 1
    Investigated diseases:
    Investigated drugs:
    Belgium France The Netherlands Spain

Glossary

  • Focal Adhesion Kinase (FAK): A protein involved in cellular processes like growth, survival, and movement. FAK is often overactive in cancer cells and is the target of defactinib.
  • KRAS Mutation: A change in the KRAS gene that can drive cancer growth. Some defactinib trials are specifically studying patients with KRAS mutant cancers.
  • Pharmacokinetics: The study of how a drug moves through the body, including how it's absorbed, distributed, metabolized, and excreted.
  • Progression-Free Survival (PFS): The length of time during and after treatment that a patient lives without the cancer growing or spreading.
  • RECIST Criteria: Response Evaluation Criteria in Solid Tumors – a standard way to measure how well a cancer patient responds to treatment.
  • Dose-Limiting Toxicity (DLT): Side effects severe enough to prevent further dose increases of a drug in a clinical trial.
  • Maximum Tolerated Dose (MTD): The highest dose of a drug that can be given without causing unacceptable side effects.
  • Biomarker: A measurable substance in the body that may indicate disease, infection, or environmental exposure. In cancer trials, biomarkers may help predict response to treatment.

References

  1. https://clinicaltrials.gov/study/NCT02913716
  2. https://clinicaltrials.gov/study/NCT01943292
  3. https://clinicaltrials.gov/study/NCT06487221
  4. https://clinicaltrials.gov/study/NCT03875820
  5. https://clinicaltrials.gov/study/NCT04201145
  6. https://clinicaltrials.gov/study/NCT04439331
  7. https://clinicaltrials.gov/study/NCT06007924
  8. https://clinicaltrials.gov/study/NCT01778803
  9. https://clinicaltrials.gov/study/NCT02758587
  10. https://clinicaltrials.gov/study/NCT01951690