Lufotrelvir

Last updated
Lufotrelvir
Lufotrelvir.svg
Legal status
Legal status
  • US:Investigational drug
Identifiers
  • [(3S)-3-[(2S)-2-[(4-methoxy-1H-indol-2-yl)formamido]-4-methylpentanamido]-2-oxo-4-[(3S)-2-oxopyrrolidin-3-yl]butoxy]phosphonic acid
CAS Number
PubChem CID
DrugBank
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
Formula C24H33N4O9P
Molar mass 552.521 g·mol−1
3D model (JSmol)
  • CC(C)C[C@@H](C(=O)N[C@@H](C[C@@H]1CCNC1=O)C(=O)COP(=O)(O)O)NC(=O)C2=CC3=C(N2)C=CC=C3OC
  • InChI=1S/C24H33N4O9P/c1-13(2)9-18(28-24(32)19-11-15-16(26-19)5-4-6-21(15)36-3)23(31)27-17(10-14-7-8-25-22(14)30)20(29)12-37-38(33,34)35/h4-6,11,13-14,17-18,26H,7-10,12H2,1-3H3,(H,25,30)(H,27,31)(H,28,32)(H2,33,34,35)/t14-,17-,18-/m0/s1
  • Key:FQKALOFOWPDTED-WBAXXEDZSA-N

Lufotrelvir (PF-07304814) is an antiviral drug developed by Pfizer which acts as a 3CL protease inhibitor. [1] It is a prodrug with the phosphate group being cleaved in vivo to yield the active agent PF-00835231. [2] Lufotrelvir is in human clinical trials for the treatment of COVID-19, and shows good activity against COVID-19 including several variant strains, but unlike the related drug nirmatrelvir it is not orally active and must be administered by intravenous infusion, and so has been the less favoured candidate for clinical development overall. [3] [4] [5]

See also

References

  1. ↑ Hoffman RL, Kania RS, Brothers MA, Davies JF, Ferre RA, Gajiwala KS, et al. (November 2020). "Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19". Journal of Medicinal Chemistry. 63 (21): 12725–12747. doi:10.1021/acs.jmedchem.0c01063. PMC   7571312 . PMID   33054210.
  2. ↑ Boras B, Jones RM, Anson BJ, Arenson D, Aschenbrenner L, Bakowski MA, et al. (October 2021). "Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19". Nature Communications. 12 (1) 6055. Bibcode:2021NatCo..12.6055B. doi:10.1038/s41467-021-26239-2. PMC   8523698 . PMID   34663813.
  3. ↑ de Vries M, Mohamed AS, Prescott RA, Valero-Jimenez AM, Desvignes L, O'Connor R, et al. (March 2021). "A comparative analysis of SARS-CoV-2 antivirals characterizes 3CLpro inhibitor PF-00835231 as a potential new treatment for COVID-19". Journal of Virology. 95 (7). doi:10.1128/JVI.01819-20. PMC   8139662 . PMID   33622961.
  4. ↑ Baig MH, Sharma T, Ahmad I, Abohashrh M, Alam MM, Dong JJ (March 2021). "Is PF-00835231 a Pan-SARS-CoV-2 Mpro Inhibitor? A Comparative Study". Molecules. 26 (6): 1678. doi: 10.3390/molecules26061678 . PMC   8002701 . PMID   33802860.
  5. ↑ Vandyck K, Deval J (August 2021). "Considerations for the discovery and development of 3-chymotrypsin-like cysteine protease inhibitors targeting SARS-CoV-2 infection". Current Opinion in Virology. 49: 36–40. doi:10.1016/j.coviro.2021.04.006. PMC   8075814 . PMID   34029993.
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