Simnotrelvir/ritonavir explained

Width:200px
Width2:180px
Type:combo
Component1:Simnotrelvir
Class1:SARS-CoV-2 3CLpro inhibitor
Component2:Ritonavir
Class2:Protease inhibitor
Tradename:先诺欣 (Xiannuoxin)
Pregnancy Category:Contraindicated (CN)
Routes Of Administration:Oral
Legal Status:Rx in China
Drug Name:Simnotrelvir
Routes Of Administration:Oral
Class:SARS-CoV-2 3CLpro inhibitor
Legal Status:Not approved on its own
Protein Bound:72.5%
Metabolism:hepatic (CYP3A)
Elimination Half-Life:3.1 h; 4.1 h with ritonavir[1]
Excretion:urine (55.4%), feces (36.7%)
Pubchem:168476146
Synonyms:SIM0417, SSD8432
Iupac Name:(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
C:22
H:30
F:3
N:5
O:4
S:2
Smiles: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
Stdinchi: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
Stdinchikey: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.

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

External links

Notes and References

  1. Web site: Simcere . 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 . 2 October 2023 . zh-cn . January 28, 2023.
  2. Zhu KW . Deuremidevir and Simnotrelvir-Ritonavir for the Treatment of COVID-19 . ACS Pharmacology & Translational Science . 6 . 9 . 1306–1309 . September 2023 . 37705591 . 10496140 . 10.1021/acsptsci.3c00134 .
  3. Wang Q, Chen G, He J, Li J, Xiong M, Su H, Li M, Hu H, Xu Y . 6 . Structure-Based Design of Potent Peptidomimetic Inhibitors Covalently Targeting SARS-CoV-2 Papain-like Protease . International Journal of Molecular Sciences . 24 . 10 . 8633 . May 2023 . 37239980 . 10218254 . 10.3390/ijms24108633 . free .
  4. News: China approves two oral drugs to treat COVID-19 . January 30, 2023 . bioworld.com .
  5. Wang F, Xiao W, Tang Y, Cao M, Shu D, Asakawa T, Xu Y, Jiang X, Zhang L, Wang W, Tang J, Huang Y, Yang Y, Yang Y, Tang R, Shen J, Lu H . 6 . 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 . September 2023 . 37484496 . 10362366 . 10.1016/j.lanwpc.2023.100835 .
  6. Cao B, Wang Y, Lu H, Huang C, Yang Y, Shang L, Chen Z, Jiang R, Liu Y, Lin L, Peng P, Wang F, Gong F, Hu H, Cheng C, Yao X, Ye X, Zhou H, Shen Y, Liu C, Wang C, Yi Z, Hu B, Xu J, Gu X, Shen J, Xu Y, Zhang L, Fan J, Tang R, Wang C . 6 . Oral Simnotrelvir for Adult Patients with Mild-to-Moderate Covid-19 . New England Journal of Medicine . 390 . 3 . 2024-01-18 . 10.1056/NEJMoa2301425 . 230–241. 38231624 . 267030019 . 11156186 .