molecules of the month


oral, brain-penetrant VGCC inhibitor

Ph. II/III for diabetic neuropathic pain in China


J. Pharmacol. Exp. Ther., Mar. 1, 2021

Haisco Pharmaceutical, Chengdu, CN

1 min read

10. The Haisco voltage-gated calcium channel (VGCC) alpha-2-delta subunit inhibitor, HSK16149, is a potent and potentially longer-acting gabapentinoid drug candidate for chronic pain over pregabalin, with a potentially wider therapeutic index for the central nervous system (CNS). The molecule is planned for a Ph. II/III trial in China for diabetic peripheral neuropathic pain. Identifying novel chemical matter around small ligands like pregabalin is challenging, but the Haisco team appears to have found a nice niche in this brain-penetrant molecule’s interesting bridged cyclobutane structure. Chemists here may enjoy the structure of a recently approved-in-Japan competitor molecule from Daiichi Sankyo, mirogabalin as well.

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