Drug intelligence / Profile preview

crisugabalin + metformin

Development stage
Unknown
Lead developer
Haisco Pharmaceutical Group
Modality
Small Molecules
Administration
Oral
01

Overview

Crisugabalin (HSK16149) is a novel, potent oral γ-aminobutyric acid (GABA) analogue developed by Haisco Pharmaceutical Group. It acts as a selective ligand for the α2δ subunit of voltage-gated calcium channels in the central nervous system, reducing calcium influx and thereby decreasing the release of excitatory neurotransmitters such as glutamate and norepinephrine. This mechanism provides analgesic, antiepileptic, and antianxiety effects. Crisugabalin has demonstrated greater potency and a wider therapeutic index than pregabalin in preclinical studies and clinical trials for neuropathic pain conditions such as diabetic peripheral neuropathic pain (DPNP). Metformin is an established oral antihyperglycemic agent widely used to treat type 2 diabetes mellitus; it works primarily by inhibiting hepatic gluconeogenesis and improving insulin sensitivity. The combination of crisugabalin with metformin may be considered for patients with diabetic neuropathy who also require glycemic control[1][2][4][5][7].

Other names
HSK16149 + metformincrisugabalin + metformin hydrochloride
02

Targets

ND1 (Mitochondrial electron transport chain complex I)CACNA2D2 (α2δ-2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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