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DEFACTINIB
Avutometinib inhibits MEK1/2 and ERK1/2 phosphorylation, while defactinib inhibits FAK and Pyk2, enhancing anti-tumor effects when combined.
At a glance
| Generic name | DEFACTINIB |
|---|---|
| Target | MEK1/2, ERK1/2, FAK, Pyk2 |
| Modality | Small molecule |
| Phase | FDA-approved |
Mechanism of action
Avutometinib blocks the activation of MEK1/2 and ERK1/2, which are part of the MAPK pathway, reducing tumor cell growth. Defactinib targets FAK and Pyk2, further inhibiting cancer cell proliferation and enhancing the effect when used together.
Approved indications
- KRAS-mutated recurrent LGSOC
Common side effects
- nausea
- diarrhea
- vomiting
- abdominal pain
Drug interactions
- Strong and moderate CYP3A4 inhibitors
- Strong and moderate CYP3A4 inducers
- Warfarin
- Proton pump inhibitors (PPIs) or H2 receptor antagonists
Key clinical trials
- Testing VS-6063 (Defactinib) as a Potential Targeted Treatment in Cancers With NF2 Genetic Changes (MATCH-Subprotocol U) (PHASE2)
- A Study of Avutometinib and Defactinib in People With Thyroid Cancer (PHASE2)
- Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) (PHASE2)
- Stereotactic Body Radiotherapy and Focal Adhesion Kinase Inhibitor in Advanced Pancreas Adenocarcinoma (PHASE2)
- Stereotactic Body Radiotherapy Plus FAK and RAF/MEK Inhibition in Advanced Pancreatic Adenocarcinoma (PHASE2)
- Combined Evaluation of Epigenetic and Sensitising Therapy in AML and MDS (PHASE1)
- A Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer (PHASE3)
- A Study of Avutometinib (VS-6766) and Defactinib in People With Mesonephric Gynecologic Cancer (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- DEFACTINIB CI brief — competitive landscape report
- DEFACTINIB updates RSS · CI watch RSS