tasisulam + gemcitabine

**Tasisulam + gemcitabine** is an investigational combination therapy for advanced solid tumors comprising tasisulam (a synthetic benzamide-sulfonamide derivative) and gemcitabine (a nucleoside analog). Tasisulam is a small molecule antineoplastic agent with complex pharmacology, believed to induce apoptosis and cell cycle arrest, although its precise molecular targets are not fully elucidated. In combination, gemcitabine is incorporated into DNA via its active metabolite gemcitabine triphosphate, leading to “masked chain termination,” DNA fragmentation, S-phase cell cycle arrest, and apoptosis of malignant cells. The combination leverages distinct cytotoxic mechanisms to enhance antitumor activity, and its main dose-limiting toxicities are hematologic, especially thrombocytopenia and neutropenia. This combination has been administered intravenously in Phase Ib trials targeting advanced solid tumors, including specific tumor subtypes.

Other names

tasisulam-sodiumgemcitabine hydrochloride