Jump to content

Elbasvir

From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by Espresso Addict (talk | contribs) at 23:48, 5 October 2016 (Starting See also; wikilink). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Elbasvir
Clinical data
Routes of
administration		Oral
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • Dimethyl N,N’-([(6S)-6H-indolo[1,2-c][1,3]benzoxazine-3,10-diyl]bis{1H-imidazole-5,2-diyl-(2S)-pyrrolidine-2,1-diyl[(2S)-1-oxo-3-methylbutane-1,2-diyl]})biscarbamate
CAS Number
ChemSpider
ChEBI
CompTox Dashboard (EPA)
ECHA InfoCard100.234.242 Edit this at Wikidata
Chemical and physical data
FormulaC49H55N9O7
Molar mass882.015 g/mol g·mol−1
3D model (JSmol)
  • CC(C)[C@@H](C(=O)N1CCC[C@H]1c2[nH]cc(n2)c3ccc4c(c3)cc-5n4[C@@H](Oc6c5ccc(c6)c7c[nH]c(n7)[C@@H]8CCCN8C(=O)[C@H](C(C)C)NC(=O)OC)c9ccccc9)NC(=O)OC
  • InChI=1S/C49H55N9O7/c1-27(2)41(54-48(61)63-5)45(59)56-20-10-14-37(56)43-50-25-34(52-43)30-17-19-36-32(22-30)23-39-33-18-16-31(24-40(33)65-47(58(36)39)29-12-8-7-9-13-29)35-26-51-44(53-35)38-15-11-21-57(38)46(60)42(28(3)4)55-49(62)64-6/h7-9,12-13,16-19,22-28,37-38,41-42,47H,10-11,14-15,20-21H2,1-6H3,(H,50,52)(H,51,53)(H,54,61)(H,55,62)/t37-,38-,41-,42-,47-/m0/s1
  • Key:BVAZQCUMNICBAQ-PZHYSIFUSA-N

Elbasvir (MK-8742) is a drug approved (FDA Jan 2016)[1] for the treatment of hepatitis C. It was developed by Merck and completed Phase III trials, following promising results in Phase II when used in combination with the NS3/4a protease inhibitor grazoprevir, either with or without ribavirin.[2]

Elbasvir is a highly potent and selective inhibitor of the hepatitis C virus NS5A replication complex.[3] It has only been investigated as a combination product with other complementary hepatitis C antiviral drugs such as grazoprevir and MK-3682, and it is unclear whether elbasvir would show robust antiviral activity if it was administered by itself. Nevertheless, combination products of this type represent the most successful approach yet developed for actually curing hepatitis C, rather than merely slowing the progression of the disease.[4]

See also

References

  1. ^ FDA approves Zepatier for treatment of chronic hepatitis C genotypes 1 and 4. January 28, 2016
  2. ^ Lawitz, E; Gane, E; Pearlman, B; Tam, E; Ghesquiere, W; Guyader, D; Alric, L; Bronowicki, JP; Lester, L; Sievert, W; Ghalib, R; Balart, L; Sund, F; Lagging, M; Dutko, F; Shaughnessy, M; Hwang, P; Howe, AY; Wahl, J; Robertson, M; Barr, E; Haber, B (2015). "Efficacy and safety of 12 weeks versus 18 weeks of treatment with grazoprevir (MK-5172) and elbasvir (MK-8742) with or without ribavirin for hepatitis C virus genotype 1 infection in previously untreated patients with cirrhosis and patients with previous null response with or without cirrhosis (C-WORTHY): a randomised, open-label phase 2 trial". Lancet. 385 (9973): 1075–86. doi:10.1016/S0140-6736(14)61795-5. PMID 25467591.
  3. ^ Coburn, CA; Meinke, PT; Chang, W; Fandozzi, CM; Graham, DJ; Hu, B; Huang, Q; Kargman, S; Kozlowski, J; Liu, R; McCauley, JA; Nomeir, AA; Soll, RM; Vacca, JP; Wang, D; Wu, H; Zhong, B; Olsen, DB; Ludmerer, SW (2013). "Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity". ChemMedChem. 8 (12): 1930–40. doi:10.1002/cmdc.201300343. PMID 24127258.
  4. ^ Gentile, I; Buonomo, AR; Zappulo, E; Borgia, G (Jul 2014). "Interferon-free therapies for chronic hepatitis C: toward a hepatitis C virus-free world?". Expert Review of Anti-Infective Therapy. 12 (7): 763–73. doi:10.1586/14787210.2014.929497. PMID 24918116.


Stub icon

This antiinfective drug article is a stub. You can help Wikipedia by expanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Elbasvir&oldid=742814450"