crisugabalin besilate

Crisugabalin besilate (HSK16149) is a novel, potent, and selective gabapentinoid developed by Haisco Pharmaceutical Group as a next-generation treatment for neuropathic pain. It acts as a ligand for the $\alpha_2\delta$ subunit of voltage-gated calcium channels (VGCCs), specifically targeting the $\alpha_2\delta-1$ and $\alpha_2\delta-2$ isoforms. By binding to these subunits, crisugabalin modulates the influx of calcium into presynaptic neurons, thereby reducing the release of excitatory neurotransmitters such as glutamate and substance P, which are involved in pain signaling. Developed to offer improved potency and a more favorable safety profile compared to pregabalin, crisugabalin besilate has received regulatory approval in China for the treatment of diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN). Hangzhou Third People's Hospital served as a key clinical development partner, particularly in trials focusing on herpes zoster-related pain.

Brand names

Simeining

Other names

crisugabalin besylate(S)-3-(aminomethyl)-5-methylhexanoic acid benzenesulfonate