Crisugabalin

Last updated
Crisugabalin
Crisugabalin.svg
Legal status
Legal status
Identifiers
  • 2-[(1S,2S,3R,6S,8S)-2-(aminomethyl)-2-tricyclo[4.2.1.03,8]nonanyl]acetic acid
CAS Number
PubChem CID
UNII
Chemical and physical data
Formula C12H19NO2
Molar mass 209.289 g·mol−1
3D model (JSmol)
  • C1C[C@@H]2[C@@H]3C[C@H]1C[C@@H]3[C@@]2(CC(=O)O)CN
  • InChI=1S/C12H19NO2/c13-6-12(5-11(14)15)9-2-1-7-3-8(9)10(12)4-7/h7-10H,1-6,13H2,(H,14,15)/t7-,8-,9+,10-,12-/m0/s1
  • Key:WCEFMBSFXJUREW-LIJGXYGRSA-N

Crisugabalin (HSK16149) is a selective GABA analog in development for the treatment of chronic pain. It has a wider therapeutic index than pregabalin, which has a similar mechanism of action. In China, it was approved in May 2024 for the treatment of diabetic peripheral neuropathic pain [1] and approved in July 2024 for the treatment of postherpetic neuralgia. [2] In the United States, it is in Phase III trials as of 2023. [3] [4] The drug can be administered with or without food. [5]

See also

References

  1. ↑ "Monthly Report: New Drug Approval in China, May 2024".
  2. ↑ "海思科苯磺酸克利加巴林胶囊获批新适应症". PhIRDA. 19 July 2024. Retrieved 26 April 2025.
  3. ↑ Gou, Xiaoli; Yu, Xiaojuan; Bai, Dongdong; Tan, Bowei; Cao, Pingfeng; Qian, Meilin; Zheng, Xiaoxiao; Chen, Lei; Shi, Zongjun; Li, Yao; Ye, Fei; Liang, Yong; Ni, Jia (March 2021). "Pharmacology and Mechanism of Action of HSK16149, a Selective Ligand of α2δ Subunit of Voltage-Gated Calcium Channel with Analgesic Activity in Animal Models of Chronic Pain". The Journal of Pharmacology and Experimental Therapeutics. 376 (3): 330–337. doi: 10.1124/jpet.120.000315 . ISSN   1521-0103. PMID   33293377.
  4. ↑ Guo, Xiaohui; Zhang, Tingting; Yuan, Geheng; Yukun, LI; Hua Ma, Jian; Hong-Mei, LI (2023). "224-OR: The Efficacy and Safety of HSK 16149 in Chinese with Diabetic Peripheral Neuropathic Pain—A Randomized, Double-Blinded, Placebo and Pregabalin-Controlled Phase II/III Study". Diabetes. 72 224-OR. doi:10.2337/db23-224-OR.
  5. ↑ Wu, Qingqing; Zhu, Huijuan; Song, Rong; Zhang, Mengqi; Li, Fangqiong; Zeng, Weifang; Wang, Wei; Jia, Jingying; Yu, Chen; Liu, Yanmei (June 2023). "Effect of a high-fat and high-calorie food on the pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy subjects". Pharmacology Research & Perspectives. 11 (3): e01102. doi: 10.1002/prp2.1102 . PMC   10199234 . PMID   37208866.
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