grisugabalin

Grisugabalin (JX-11502) is a novel small molecule gabapentinoid developed by Zhejiang Jingxin Pharmaceutical for the treatment of primary restless legs syndrome (RLS) and neuropathic pain. As a ligand for the $\alpha_2\delta$ subunits (specifically $\alpha_2\delta-1$ and $\alpha_2\delta-2$) of voltage-gated calcium channels, grisugabalin modulates the influx of calcium into neurons and subsequently inhibits the release of excitatory neurotransmitters such as glutamate and substance P. This mechanism is shared with other gabapentinoids like pregabalin and gabapentin, but grisugabalin is designed to offer improved efficacy or safety profiles. In 2025, it entered Phase 3 clinical trials in China, where it is being compared to pramipexole for the treatment of adults with primary RLS in a multicenter study sponsored by Shanghai General Hospital.

Other names

grisugabalin格瑞舒加巴林