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Simnotrelvir/ritonavir

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(Redirected fromSimnotrelvir)
Antiviral combination medication

Pharmaceutical compound
Simnotrelvir/ritonavir
Chemical structures of simnotrelvir (top) and ritonavir (bottom)
Combination of
SimnotrelvirSARS-CoV-2 3CLpro inhibitor
RitonavirProtease inhibitor
Clinical data
Trade names先诺欣 (Xiannuoxin)
Pregnancy
category
  • Contraindicated (CN)
Routes of
administration
Oral
Legal status
Legal status
  • Rx in China
Pharmaceutical compound
Simnotrelvir
Clinical data
Other namesSIM0417, SSD8432
Routes of
administration
Oral
Drug classSARS-CoV-2 3CLpro inhibitor
Legal status
Legal status
  • Not approved on its own
Pharmacokinetic data
Protein binding72.5%[1]
Metabolismhepatic (CYP3A)[1]
Eliminationhalf-life3.1 h; 4.1 h with ritonavir[1]
Excretionurine (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
PubChemCID
Chemical and physical data
FormulaC22H30F3N5O4S2
Molar mass549.63 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 nameXiannuoxin) is a pharmaceutical drug used for the treatment ofCOVID-19.[2] Simnotrelvir/ritonavir is acombination drug of simnotrelvir, aninhibitor ofSARS-CoV-2 3CLpro, andritonavir,[3] aCYP3A inhibitor.

It was developed by Simcere Pharmaceutical and conditionally approved in China by theNational 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 amedian of 36 hours compared to placebo.[6]

See also

[edit]

References

[edit]
  1. ^abcdSimcere (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)). Retrieved2 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.

External links

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