ArticlePharmaceutical research2026
Preclinical Pharmacokinetic and Pharmacological Profiling of B339, a Novel SARM1 Inhibitor for the Treatment of Vincristine-induced Peripheral Neuropathy.
Article in Pharmaceutical research, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
purposeDespite the extensive knowledge about the role of Sterile α and TIR motif-containing protein-1 (SARM1) inhibition in the prevention of axonal degeneration, very few pharmacological inhibitors of SARM1 have been discovered and tested in preclinical models, with limited knowledge about their pharmacokinetic properties.
methodsIn this study, a thioamide small-molecule library was screened against SARM1 via structure-guided molecular docking and the inhibitory activity of the resulting hits was further evaluated using High Performance Liquid Chromatography (HPLC) based in vitro NADase assay. In vitro drug metabolism and in vivo pharmacokinetic studies were performed for the best candidate, and the compound was tested in a preclinical mouse model of vincristine-induced peripheral neuropathy (VIPN).
resultsA benzothioamide derivative, B339, emerged as a potent SARM1 inhibitor (IC
conclusionsThe study provided discovery and in-depth pharmacokinetic characterization of a novel SARM1 inhibitor, B339, and demonstrated its pharmacological potential for the treatment of VIPN.
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