BW813U

BW813U is a small molecule inhibitor of choline acetyltransferase (ChAT), the enzyme responsible for the biosynthesis of acetylcholine. It is being investigated as a novel therapeutic approach for lung adenocarcinoma (LUAD), particularly in patients with a history of tobacco smoke or nicotine exposure. Nicotine is known to accelerate the growth of human LUADs by stimulating nicotinic acetylcholine receptors (nAChRs). By inhibiting ChAT, BW813U reduces the availability of endogenous acetylcholine, thereby suppressing tumor growth and angiogenesis. Preclinical studies have demonstrated that BW813U robustly suppresses angiogenesis in Matrigel and CAM models and potently decreases the growth rate of LUAD tumor xenografts. Its anti-angiogenic activity is mediated through the alpha7-nAChR and nitric oxide signaling pathways, as evidenced by the reduction of the angiogenic biomarker CD31 in tumor sections.