defactinib

Defactinib is an orally bioavailable small molecule inhibitor of focal adhesion kinase (FAK), a cytoplasmic tyrosine kinase involved in integrin-mediated signal transduction. By inhibiting FAK activity, defactinib disrupts downstream signaling pathways such as RAS/MEK/ERK and PI3K/Akt that are critical for tumor cell migration, proliferation, survival, and angiogenesis. This mechanism imparts both antiangiogenic and antineoplastic effects. Defactinib is primarily developed for use in combination with avutometinib (a RAF/MEK clamp) for the treatment of recurrent KRAS-mutant low-grade serous ovarian cancer (LGSOC) in adults who have received at least one prior systemic therapy. It has also been investigated in other cancers including malignant pleural mesothelioma, non-small cell lung cancer (NSCLC), pancreatic cancer, thyroid cancer (including anaplastic and differentiated types), uveal melanoma, lymphoma, multiple myeloma, glioblastoma, solid tumors and gynaecological cancers[1][2][3][5][7][9].

Brand names

FAKZYNJA

Other names

defactinib hydrochlorideAVMAPKI FAKZYNJA CO-PACK1073154-85-41345713-71-4