rigosertib

Rigosertib is a synthetic small molecule, classified as a styryl benzyl sulfone analogue and Ras mimetic, with investigational antineoplastic activity. It acts as a multi-targeted kinase inhibitor, primarily inhibiting the Ras signal transduction pathway by binding to the Ras-binding domain (RBD) of various effector proteins such as Raf kinase and phosphatidylinositol 3‑kinase (PI3K). This disrupts downstream signaling through pathways including Ras/Raf/Erk, PI3K/Akt, and polo-like kinase 1 (PLK1), leading to cell cycle arrest and apoptosis in tumor cells. Rigosertib also functions as a non‑ATP competitive inhibitor of PLK1 and has microtubule-destabilizing properties. It is being developed for both oral and intravenous administration for hematologic malignancies such as myelodysplastic syndromes (MDS), chronic myelomonocytic leukemia (CMML), acute myeloid leukemia (AML), solid tumors, among others[1][2][3][4].

Brand names

EstybonNovonex

Other names

rigosertib sodium