Simnotrelvir/ritonavir

Last updated

Simnotrelvir/ritonavir
Simnotrelvir.svg
Ritonavir structure.svg
Chemical structures of simnotrelvir (top) and ritonavir (bottom)
Combination of
Simnotrelvir SARS-CoV-2 3CLpro inhibitor
Ritonavir Protease inhibitor
Clinical data
Trade names 先诺欣 (Xiannuoxin)
Pregnancy
category
  • Contraindicated (CN)
Routes of
administration 		Oral
Legal status
Legal status
  • Rx in China
Simnotrelvir
Clinical data
Other namesSIM0417, SSD8432
Routes of
administration 		Oral
Drug class SARS-CoV-2 3CLpro inhibitor
Legal status
Legal status
  • Not approved on its own
Pharmacokinetic data
Protein binding 72.5% [1]
Metabolism hepatic (CYP3A) [1]
Elimination half-life 3.1 h; 4.1 h with ritonavir [1]
Excretion urine (55.4%), feces (36.7%) [1]
Identifiers
  • (8S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-7-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxamide
PubChem CID
Chemical and physical data
Formula C22H30F3N5O4S2
Molar mass 549.63 g·mol−1
3D model (JSmol)
  • CC(C)(C)[C@@H](C(=O)N1CC2(C[C@H]1C(=O)N[C@@H](C[C@@H]3CCNC3=O)C#N)SCCS2)NC(=O)C(F)(F)F
  • InChI=InChI=1S/C22H30F3N5O4S2/c1-20(2,3)15(29-19(34)22(23,24)25)18(33)30-11-21(35-6-7-36-21)9-14(30)17(32)28-13(10-26)8-12-4-5-27-16(12)31/h12-15H,4-9,11H2,1-3H3,(H,27,31)(H,28,32)(H,29,34)/t12-,13-,14-,15+/m0/s1
  • Key:LQBRGTAIBBFUJJ-ZQDZILKHSA-N

Simnotrelvir/ritonavir (trade name Xiannuoxin) is a pharmaceutical drug used for the treatment of COVID-19. [2] Simnotrelvir/ritonavir is a combination drug of simnotrelvir, an inhibitor of SARS-CoV-2 3CLpro, and ritonavir, [3] a CYP3A inhibitor.

Contents

It was developed by Simcere Pharmaceutical and conditionally approved in China by the National Medical Products Administration (NMPA) in January 2023. [4] Results for the phase Ib trial are available. [5] In a phase II/III trial, it reduced the duration of symptoms by a median of 36 hours compared to placebo. [6]

See also

References

  1. 1 2 3 4 Simcere (January 28, 2023). "先诺欣 [先诺特韦片/利托那韦片组合包装 Simnotrelvir Tablets/Ritonavir Tablets（co-packaged）]". Dxy.cn package insert database (in Chinese (China)). Retrieved 2 October 2023.
  2. ↑ Zhu KW (September 2023). "Deuremidevir and Simnotrelvir-Ritonavir for the Treatment of COVID-19". ACS Pharmacology & Translational Science. 6 (9): 1306–1309. doi:10.1021/acsptsci.3c00134. PMC   10496140 . PMID   37705591.
  3. ↑ Wang Q, Chen G, He J, Li J, Xiong M, Su H, et al. (May 2023). "Structure-Based Design of Potent Peptidomimetic Inhibitors Covalently Targeting SARS-CoV-2 Papain-like Protease". International Journal of Molecular Sciences. 24 (10): 8633. doi: 10.3390/ijms24108633 . PMC   10218254 . PMID   37239980.
  4. ↑ "China approves two oral drugs to treat COVID-19". bioworld.com. January 30, 2023.
  5. ↑ Wang F, Xiao W, Tang Y, Cao M, Shu D, Asakawa T, et al. (September 2023). "Efficacy and safety of SIM0417 (SSD8432) plus ritonavir for COVID-19 treatment: a randomised, double-blind, placebo-controlled, phase 1b trial". The Lancet Regional Health. Western Pacific. 38 100835. doi:10.1016/j.lanwpc.2023.100835. PMC   10362366 . PMID   37484496.
  6. ↑ Cao B, Wang Y, Lu H, Huang C, Yang Y, Shang L, et al. (2024-01-18). "Oral Simnotrelvir for Adult Patients with Mild-to-Moderate Covid-19". New England Journal of Medicine. 390 (3): 230–241. doi:10.1056/NEJMoa2301425. PMC   11156186 . PMID   38231624. S2CID   267030019.
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