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Antiviral combination medication
Simnotrelvir Other names SIM0417, SSD8432
Routes of administration Oral
Drug class
SARS-CoV-2 3CLpro inhibitor
Legal status
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]
(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
Formula C 22 H 30 F 3 N 5 O 4 S 2
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 .
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
^
a
b
c
d 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 .
^ 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 .
^ 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 .
^
"China approves two oral drugs to treat COVID-19" . bioworld.com . January 30, 2023.
^ 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 .
^ 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