Leritrelvir

Pharmaceutical compound

Leritrelvir
Legal status

Legal status	Rx in China
Identifiers
IUPAC name (3S,3aS,6aR)-2-[(2S)-2-cyclohexyl-2-[(2,2,2-trifluoroacetyl)amino]acetyl]-N-[(2S)-4-(cyclopentylamino)-3,4-dioxo-1-[(3S)-2-oxopyrrolidin-3-yl]butan-2-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamide
CAS Number	2923310-64-7
PubChem CID	167713195
ChemSpider	128922060
ChEMBL	ChEMBL5422898
Chemical and physical data
Formula	C₃₁H₄₄F₃N₅O₆
Molar mass	639.717 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C1CCC(CC1)[C@@H](C(=O)N2C[C@@H]3CCC[C@@H]3[C@H]2C(=O)N[C@@H](C[C@@H]4CCNC4=O)C(=O)C(=O)NC5CCCC5)NC(=O)C(F)(F)F
InChI InChI=1S/C31H44F3N5O6/c32-31(33,34)30(45)38-23(17-7-2-1-3-8-17)29(44)39-16-19-9-6-12-21(19)24(39)27(42)37-22(15-18-13-14-35-26(18)41)25(40)28(43)36-20-10-4-5-11-20/h17-24H,1-16H2,(H,35,41)(H,36,43)(H,37,42)(H,38,45)/t18-,19-,21-,22-,23-,24-/m0/s1 Key:ICGMMLTUQDVAST-HEZDJTGRSA-N

Leritrelvir (RAY1216) is an antiviral drug which acts as a 3C-like protease inhibitor. It was developed and approved^[1] in China for treatment of COVID-19.^[2]^[3]^[4]^[5]^[6]

References

[edit ]

^ Zheng L, Wang W, Sun Q (2024). "Targeted drug approvals in 2023: Breakthroughs by the FDA and NMPA". Signal Transduction and Targeted Therapy. 9 (1): 46. doi:10.1038/s41392-024-01770-y. PMC 10879080 . PMID 38378623.
^ Chen X, Huang X, Ma Q, Kuzmic P, Zhou B, Zhang S, et al. (April 2024). "Preclinical evaluation of the SARS-CoV-2 Mpro inhibitor RAY1216 shows improved pharmacokinetics compared with nirmatrelvir". Nature Microbiology. 9 (4): 1075–1088. doi:10.1038/s41564-024-01618-9. PMC 10994847 . PMID 38553607.
^ Janin YL (January 2024). "On the origins of SARS-CoV-2 main protease inhibitors". RSC Medicinal Chemistry. 15 (1): 81–118. doi:10.1039/d3md00493g. PMC 10809347 . PMID 38283212.
^ Chan CC, Guo Q, Chan JF, Tang K, Cai JP, Chik KK, et al. (September 2024). "Identification of novel small-molecule inhibitors of SARS-CoV-2 by chemical genetics". Acta Pharmaceutica Sinica. B. 14 (9): 4028–4044. doi:10.1016/j.apsb.2024年05月02日6. PMC 11413674 . PMID 39309487.
^ Cao Q, Ding Y, Xu Y, Li M, Zheng R, Cao Z, et al. (December 2023). "Small-molecule anti-COVID-19 drugs and a focus on China's homegrown mindeudesivir (VV116)". Frontiers of Medicine. 17 (6): 1068–1079. doi:10.1007/s11684-023-1037-3. PMID 38165534.
^ Zheng B, Zhao Q, Yang W, Feng P, Xin C, Ying Y, et al. (March 2024). "Small-molecule antiviral treatments for COVID-19: A systematic review and network meta-analysis". International Journal of Antimicrobial Agents. 63 (3) 107096. doi:10.1016/j.ijantimicag.2024.107096 . PMID 38244811.

v
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RNA virus antivirals (primarily J05, also S01AD and D06BB)

Hepatitis C

NS3/4A protease inhibitors (–previr)	Asunaprevir Boceprevir ^‡ Ciluprevir ^§ Danoprevir ^† Faldaprevir ^‡ Glecaprevir Grazoprevir Narlaprevir Paritaprevir Simeprevir Sovaprevir ^† Telaprevir ^‡ Vaniprevir Vedroprevir ^§ Voxilaprevir
NS5A inhibitors (–asvir)	Coblopasvir Daclatasvir ^# Elbasvir Ledipasvir Odalasvir ^† Ombitasvir Pibrentasvir Ravidasvir ^† Ruzasvir ^† Samatasvir ^† Velpatasvir
NS5B RNA polymerase inhibitors (–buvir)	Beclabuvir ^† Bemnifosbuvir ^† Dasabuvir ^# Deleobuvir ^§ Filibuvir ^§ GS-6620 ^§ IDX-184 ^§ Setrobuvir ^§ Sofosbuvir ^# Tegobuvir ^§ TMC-647055 ^§ Radalbuvir ^† Uprifosbuvir ^†
Combination drugs	Elbasvir/grazoprevir Glecaprevir/pibrentasvir Ledipasvir/sofosbuvir ^# Ombitasvir/paritaprevir/ritonavir ^# Sofosbuvir/daclatasvir Sofosbuvir/velpatasvir ^# Sofosbuvir/velpatasvir/voxilaprevir

Hepatitis D

Bulevirtide

Picornavirus

viral entry: Pleconaril ^†

Anti-influenza agents

neuraminidase inhibitors/release phase (Oseltamivir ^#
Zanamivir
Peramivir, Laninamivir ^†)

Multiple/general

Interferon	Interferon alfa 2b Peginterferon alfa-2a ^# Peginterferon alfa-2b ^#
3CL protease inhibitors (–trelvir)	Atilotrelvir Ensitrelvir ^† Ibuzatrelvir Leritrelvir Lufotrelvir Nirmatrelvir ^† (+ritonavir)^† Rupintrivir Simnotrelvir (+ritonavir ^†)
RNA pol inhibitors	CMX521 ^§ Deuremidevir ^† Favipiravir Galidesivir ^† GS-441524 ^§ Remdesivir MK-608 ^§ Mericitabine ^† Molnupiravir NITD008 ^§ Ribavirin ^# Taribavirin ^† Triazavirin Valopicitabine ^†
Multiple/Unknown/Other	EICAR ^§ Merimepodib ^§ Moroxydine Presatovir ^†

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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