Ensitrelvir

Ensitrelvir[1] (code name S-217622, brand name Xocova)[2] is an antiviral drug developed by Shionogi in partnership with Hokkaido University, which acts as an orally active 3C-like protease inhibitor for the treatment of COVID-19 infection.[3][4] It is taken by mouth, and has been successfully tested against the recently emerged Omicron variant.[5][6]

Ensitrelvir
Clinical data
Other namesS-217622
Identifiers
IUPAC name
  • 1-(2,4,5-trifluorobenzyl)-3-[(1-methyl-1H-1,2,4-triazol-3-yl)methyl]-(6E)-6-[(6-chloro-2-methyl-2H-indazol-5-yl)imino]-1,3,5-triazinane-2,4-dione
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC22H17ClF3N9O2
Molar mass531.88 g·mol−1
3D model (JSmol)
SMILES
  • Cn1cnc(CN2C(=O)N(Cc3cc(F)c(F)cc3F)C(=N\c3cc4cn(C)nc4cc3Cl)\NC2=O)n1
InChI
  • InChI=1S/C22H17ClF3N9O2/c1-32-7-12-4-18(13(23)5-17(12)30-32)28-20-29-21(36)35(9-19-27-10-33(2)31-19)22(37)34(20)8-11-3-15(25)16(26)6-14(11)24/h3-7,10H,8-9H2,1-2H3,(H,28,29,36)
  • Key:QMPBBNUOBOFBFS-UHFFFAOYSA-N

History

It has reached Phase III clinical trials.[7] The Japanese government is reportedly considering allowing Shionogi permission to apply for approval for medical use before the final steps of trials are completed, potentially speeding up the release for sale. This conditional early approval system has previously been used in Japan to accelerate the progression to market of other antiviral drugs targeting COVID-19, including remdesivir and molnupiravir.[8] In a study of 428 patients, viral load was reduced, but symptoms were not significantly reduced.[9]

If approved it would become the first Japanese domestic pill to treat COVID-19 and the third to be approved in Japan. In February 2022, the company sought emergency approval from regulators in Japan.[9]

Shionogi announced they had reached a preliminary agreement to supply 1 million doses to the Japanese government once the drug is approved. The CEO said they could have capacity to make 10 million doses a year. [10]

See also

References
  1. World Health Organization (2021). "International Nonproprietary Names for Pharmaceutical Substances. Proposed INN: List 126" (PDF). WHO Drug Information. 35 (4): 1135.
  2. "Xocova: Powerful New Japanese Pill for Coronavirus Treatment". BioPharma Media. February 2022.
  3. Unoh Y, Uehara S, Nakahara K, Nobori H, Yamatsu Y, Yamamoto S, et al. (May 2022). "Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19". Journal of Medicinal Chemistry. 65 (9): 6499–6512. doi:10.1021/acs.jmedchem.2c00117. PMC 8982737. PMID 35352927.
  4. "Shionogi presents positive Ph II/III results for COVID-19 antiviral S-217622". thepharmaletter.com. 31 January 2022.
  5. "Shionogi's new COVID pill appears to ease omicron symptoms". Nikkei Asia. 21 December 2021.
  6. Uraki R, Kiso M, Iida S, Imai M, Takashita E, Kuroda M, et al. (IASO study team) (May 2022). "Characterization and antiviral susceptibility of SARS-CoV-2 Omicron/BA.2". Nature. 607: 119–127. doi:10.1038/s41586-022-04856-1. PMID 35576972.
  7. Tyndall JD (May 2022). "S-217622, a 3CL Protease Inhibitor and Clinical Candidate for SARS-CoV-2". Journal of Medicinal Chemistry. 65 (9): 6496–6498. doi:10.1021/acs.jmedchem.2c00624. PMID 35507419.
  8. "Japan to consider early approval for Shionogi COVID-19 pill". Japan Times. 8 February 2022.
  9. "Japan's Shionogi seeks approval for COVID-19 pill". Reuters. 25 February 2022.
  10. "Japan's Shionogi signs government supply pact for pill to fight COVID". Reuters. 25 March 2022.
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