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kligabalin
- Development stage
- Unknown
- Lead developer
- Haisco Pharmaceutical Group
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Kligabalin (HSK16149) is a novel gabapentinoid and a potent, high-affinity ligand for the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels (VGCCs). Developed by Haisco Pharmaceutical Group, it is designed to treat chronic neuropathic pain conditions, including diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN). By binding to the α2δ-1 and α2δ-2 subunits, kligabalin modulates the trafficking and function of calcium channels, thereby inhibiting the release of excitatory neurotransmitters such as glutamate, substance P, and norepinephrine in the central nervous system. This mechanism effectively reduces neuronal hyperexcitability associated with neuropathic pain. Kligabalin besylate capsules were approved by China's National Medical Products Administration (NMPA) in May 2024 for the treatment of DPNP, offering a therapeutic option with potentially improved potency and safety compared to earlier gabapentinoids like pregabalin.
- Brand names
- Simening
- Other names
- kligabalin besylateHSK16149 besylateHSK-16149 besylateHSK 16149 besylate克利加巴林
02
Targets
CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)CACNA2D2 (α2δ-2)
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