Tasisulam

Tasisulam is an anticancer agent that inhibits the growth of Calu-6 non-small cell lung carcinoma (NSCLC) and A-375 melanoma cell lines (EC₅₀s = 10 and 25 μM, respectively).¹ It arrests the cell cycle at the G₂/M phase and induces apoptosis of Calu-6 cells in a concentration-dependent manner. Tasisulam induces non-apoptotic growth arrest in human vascular endothelial cells (HUVECs) and inhibits VEGF-, FGF-, and EGF-induced endothelial cord formation in vitro (EC₅₀s = 47, 103, and 34 nM, respectively). In vivo, tasisulam (25 and 50 mg/kg) reduces hemoglobin content and blood vessel density in a Matrigel™ plug model of neoangiogenesis. It also reduces tumor growth in a dose-dependent manner in a Calu-6 mouse xenograft model via arrest of the cell cycle at the G₂/M phase, induction of apoptosis, and reduction of tumor blood vessel density. Formulations containing tasisulam are under clinical investigation for the treatment of advanced solid tumors.

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1. Meier, T., Uhlik, M., Chintharlapalli, S., et al. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Mol. Cancer. Ther. 10(11), 2168-2178 (2011).