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'''Leritrelvir''' ('''RAY1216''') is an [[antiviral]] drug which acts as a [[3C-like protease]] inhibitor. It was developed and approved<ref>{{cite journal | doi = 10.1038/s41392-024-01770-y | title = Targeted drug approvals in 2023: Breakthroughs by the FDA and NMPA | date = 2024 | journal = Signal Transduction and Targeted Therapy | volume = 9 | issue = 1 | page = 46 | pmid = 38378623 | pmc = 10879080 | vauthors = Zheng L, Wang W, Sun Q }}</ref> in China for treatment of [[COVID-19]].<ref>{{cite journal | vauthors = Chen X, Huang X, Ma Q, Kuzmic P, Zhou B, Zhang S, Chen J, Xu J, Liu B, Jiang H, Zhang W, Yang C, Wu S, Huang J, Li H, Long C, Zhao X, Xu H, Sheng Y, Guo Y, Niu C, Xue L, Xu Y, Liu J, Zhang T, Spencer J, Zhu Z, Deng W, Chen X, Chen SH, Zhong N, Xiong X, Yang Z | title = Preclinical evaluation of the SARS-CoV-2 Mpro inhibitor RAY1216 shows improved pharmacokinetics compared with nirmatrelvir | journal = Nature Microbiology | volume = 9 | issue = 4 | pages = 1075-1088 | date = April 2024 | doi = 10.1038/s41564-024-01618-9 | pmid = 38553607 | pmc = 10994847 }}</ref><ref>{{cite journal | vauthors = Janin YL | title = On the origins of SARS-CoV-2 main protease inhibitors | journal = RSC Medicinal Chemistry | volume = 15 | issue = 1 | pages = 81–118 | date = January 2024 | doi = 10.1039/d3md00493g | pmid = 38283212 | pmc = 10809347 }}</ref><ref>{{cite journal | vauthors = Chan CC, Guo Q, Chan JF, Tang K, Cai JP, Chik KK, Huang Y, Dai M, Qin B, Ong CP, Chu AW, Chan WM, Ip JD, Wen L, Tsang JO, Wang TY, Xie Y, Qin Z, Cao J, Ye ZW, Chu H, To KK, Ge XY, Ni T, Jin DY, Cui S, Yuen KY, Yuan S | title = Identification of novel small-molecule inhibitors of SARS-CoV-2 by chemical genetics | journal = Acta Pharmaceutica Sinica. B | volume = 14 | issue = 9 | pages = 4028–4044 | date = September 2024 | doi = 10.1016/j.apsb.2024年05月02日6 | pmid = 39309487 | pmc = 11413674 }}</ref><ref>{{cite journal | vauthors = Cao Q, Ding Y, Xu Y, Li M, Zheng R, Cao Z, Wang W, Bi Y, Ning G, Xu Y, Zhao R | title = Small-molecule anti-COVID-19 drugs and a focus on China's homegrown mindeudesivir (VV116) | journal = Frontiers of Medicine | volume = 17 | issue = 6 | pages = 1068–1079 | date = December 2023 | doi = 10.1007/s11684-023-1037-3 | pmid = 38165534 }}</ref><ref>{{cite journal | vauthors = Zheng B, Zhao Q, Yang W, Feng P, Xin C, Ying Y, Yang B, Han B, Zhu J, Zhang M, Li G | title = Small-molecule antiviral treatments for COVID-19: A systematic review and network meta-analysis | journal = International Journal of Antimicrobial Agents | volume = 63 | issue = 3 | (削除) pages (削除ここまで) = 107096 | date = March 2024 | doi = 10.1016/j.ijantimicag.2024.107096 | pmid = 38244811 | doi-access = free }}</ref>
'''Leritrelvir''' ('''RAY1216''') is an [[antiviral]] drug which acts as a [[3C-like protease]] inhibitor. It was developed and approved<ref>{{cite journal | doi = 10.1038/s41392-024-01770-y | title = Targeted drug approvals in 2023: Breakthroughs by the FDA and NMPA | date = 2024 | journal = Signal Transduction and Targeted Therapy | volume = 9 | issue = 1 | page = 46 | pmid = 38378623 | pmc = 10879080 | vauthors = Zheng L, Wang W, Sun Q }}</ref> in China for treatment of [[COVID-19]].<ref>{{cite journal | vauthors = Chen X, Huang X, Ma Q, Kuzmic P, Zhou B, Zhang S, Chen J, Xu J, Liu B, Jiang H, Zhang W, Yang C, Wu S, Huang J, Li H, Long C, Zhao X, Xu H, Sheng Y, Guo Y, Niu C, Xue L, Xu Y, Liu J, Zhang T, Spencer J, Zhu Z, Deng W, Chen X, Chen SH, Zhong N, Xiong X, Yang Z | title = Preclinical evaluation of the SARS-CoV-2 Mpro inhibitor RAY1216 shows improved pharmacokinetics compared with nirmatrelvir | journal = Nature Microbiology | volume = 9 | issue = 4 | pages = 1075-1088 | date = April 2024 | doi = 10.1038/s41564-024-01618-9 | pmid = 38553607 | pmc = 10994847 }}</ref><ref>{{cite journal | vauthors = Janin YL | title = On the origins of SARS-CoV-2 main protease inhibitors | journal = RSC Medicinal Chemistry | volume = 15 | issue = 1 | pages = 81–118 | date = January 2024 | doi = 10.1039/d3md00493g | pmid = 38283212 | pmc = 10809347 }}</ref><ref>{{cite journal | vauthors = Chan CC, Guo Q, Chan JF, Tang K, Cai JP, Chik KK, Huang Y, Dai M, Qin B, Ong CP, Chu AW, Chan WM, Ip JD, Wen L, Tsang JO, Wang TY, Xie Y, Qin Z, Cao J, Ye ZW, Chu H, To KK, Ge XY, Ni T, Jin DY, Cui S, Yuen KY, Yuan S | title = Identification of novel small-molecule inhibitors of SARS-CoV-2 by chemical genetics | journal = Acta Pharmaceutica Sinica. B | volume = 14 | issue = 9 | pages = 4028–4044 | date = September 2024 | doi = 10.1016/j.apsb.2024年05月02日6 | pmid = 39309487 | pmc = 11413674 }}</ref><ref>{{cite journal | vauthors = Cao Q, Ding Y, Xu Y, Li M, Zheng R, Cao Z, Wang W, Bi Y, Ning G, Xu Y, Zhao R | title = Small-molecule anti-COVID-19 drugs and a focus on China's homegrown mindeudesivir (VV116) | journal = Frontiers of Medicine | volume = 17 | issue = 6 | pages = 1068–1079 | date = December 2023 | doi = 10.1007/s11684-023-1037-3 | pmid = 38165534 }}</ref><ref>{{cite journal | vauthors = Zheng B, Zhao Q, Yang W, Feng P, Xin C, Ying Y, Yang B, Han B, Zhu J, Zhang M, Li G | title = Small-molecule antiviral treatments for COVID-19: A systematic review and network meta-analysis | journal = International Journal of Antimicrobial Agents | volume = 63 | issue = 3 | (追記) article-number (追記ここまで) = 107096 | date = March 2024 | doi = 10.1016/j.ijantimicag.2024.107096 | pmid = 38244811 | doi-access = free }}</ref>


== References ==
== References ==

Latest revision as of 04:37, 30 September 2025

Pharmaceutical compound
Leritrelvir
Legal status
Legal status
  • Rx in China
Identifiers
  • (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
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C31H44F3N5O6
Molar mass 639.717 g·mol−1
3D model (JSmol)
  • 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=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 ]
  1. ^ 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.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
RNA virus antivirals (primarily J05, also S01AD and D06BB)
Hepatitis C
NS3/4A protease inhibitors (–previr)
NS5A inhibitors (–asvir)
NS5B RNA polymerase inhibitors (–buvir)
Combination drugs
Hepatitis D
Picornavirus
Anti-influenza agents
Multiple/general
Interferon
3CL protease inhibitors (–trelvir)
RNA pol inhibitors
Multiple/Unknown/Other


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