Danoprevir

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Danoprevir
Clinical data
Other namesITMN-191, RG-7227
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
  • (2R,6S,12Z,13aS,14aR,16aS)-6-[(tert-Butoxycarbonyl)amino]-14a-[N-(cyclopropanesulfonyl)carbamoyl]-5,16-dioxo- 1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a] [1,4]diazacyclopentadecin-2-yl 4-fluoro-1,3-dihydro-2H-isoindole-2-carboxylate
JSmol
)
  • CC(C)(C)OC(=O)N[C@@H]1CCCCC\C=C/[C@@H]2C[C@]2(NC(=O)[C@@H]3C[C@H](CN3C1=O)OC(=O)N4Cc5cccc(F)c5C4)C(=O)NS(=O)(=O)C6CC6
  • InChI=1S/C35H46FN5O9S/c1-34(2,3)50-32(45)37-27-13-8-6-4-5-7-11-22-17-35(22,31(44)39-51(47,48)24-14-15-24)38-29(42)28-16-23(19-41(28)30(27)43)49-33(46)40-18-21-10-9-12-26(36)25(21)20-40/h7,9-12,22-24,27-28H,4-6,8,13-20H2,1-3H3,(H,37,45)(H,38,42)(H,39,44)/b11-7-/t22-,23-,27-,28+,35-/m1/s1
  • Key:ZVTDLPBHTSMEJZ-UPZRXNBOSA-N

Danoprevir (

4A HCV protease.[3] It contains acylsulfonamide, fluoroisoindole and tert-butyl carbamate moieties. Danoprevir is a clinical candidate based on its favorable potency profile against multiple HCV genotypes 1–6 and key mutants (GT1b, IC50 = 0.2–0.4 nM; replicon GT1b, EC50 = 1.6 nM).[4]
Danoprevir has been evaluated in an open-label, single arm clinical trial in combination with ritonavir for treating COVID-19[5] and favourably compared to lopinavir/ritonavir in a second trial.[6]

History

Danaoprevir was initially developed by

Roche for development and production in China under the tradename Ganovo.[7][8]

References

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 64" (PDF). World Health Organization. p. 265. Retrieved 25 February 2017.
  2. PMID 20721837
    .
  3. PMID 23672640
    .
  4. ISBN 978-1-84973-701-2
    .
  5. PMID 33235105.{{cite journal}}: CS1 maint: multiple names: authors list (link
    )
  6. PMID 32501538.{{cite journal}}: CS1 maint: multiple names: authors list (link
    )
  7. ^ Ng E (17 July 2018). "Singapore sovereign wealth fund GIC to invest US$75 million in Chinese drug maker Ascletis' Hong Kong IPO". South China Morning Post. Retrieved 10 Aug 2018.
  8. ^ Speights K (21 February 2017). "How High Can Array BioPharma Inc. Stock Go?". The Motley Fool. Retrieved 13 August 2018.

Further reading

Seiwert SD, Andrews SW, Jiang Y, Serebryany V, Tan H, Kossen K, et al. (December 2008). "Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227)". Antimicrobial Agents and Chemotherapy. 52 (12): 4432–41.

PMID 18824605
.


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