Avutometinib + defactinib

Avutometinib + defactinib is an investigational, oral combination therapy for the treatment of recurrent low-grade serous ovarian cancer (LGSOC), particularly in patients with KRAS mutations who have received at least one prior systemic therapy. Avutometinib is a first-in-class RAF/MEK clamp that inhibits MEK kinase activity and blocks compensatory reactivation by upstream RAF kinases (ARAF, BRAF, CRAF), resulting in maximal inhibition of the RAS/MAPK pathway. Defactinib is a selective inhibitor of focal adhesion kinase (FAK) and proline-rich kinase 2 (Pyk2), which are involved in cell proliferation, survival, migration, and invasion; FAK inhibition may also overcome resistance to other anticancer agents. The combination has demonstrated synergistic anti-tumor activity and improved outcomes compared to monotherapy in clinical trials. Developed by Verastem Oncology, this regimen has received FDA Breakthrough Therapy Designation and Orphan Drug Designation for LGSOC[3][4][5][6].

Brand names

Avmapki Fakzynja Co-pack

Other names

RAF/MEK clamp + FAK inhibitor