VS-5584 + VS-6063

VS-5584 + VS-6063 is an investigational combination therapy for cancer, particularly being studied in relapsed malignant mesothelioma and other solid tumors. VS-5584 is a novel, orally available small molecule that acts as a dual inhibitor of phosphoinositide 3‑kinase (PI3K) and mammalian target of rapamycin (mTOR), showing potent activity against all class I PI3K isoforms and mTOR. It inhibits the PI3K/mTOR signaling pathway, which is frequently dysregulated in cancers and associated with tumor growth, survival, resistance to therapies, and poor prognosis[5][6][8]. VS-6063 (defactinib) is an orally available small molecule inhibitor targeting focal adhesion kinase (FAK), a protein involved in cancer cell survival, proliferation, metastasis, and maintenance of cancer stem cells[1][2]. Preclinical studies have shown that combining these agents results in superior anti-tumor efficacy compared to either agent alone. The combination preferentially targets cancer stem-like cells and has demonstrated promising activity in preclinical models[8]. Clinical trials are ongoing to evaluate safety and efficacy for patients with relapsed malignant mesothelioma who have failed prior chemotherapy[2][4].

Other names

defactinib