Elbasvir
 | |
| Systematic (IUPAC) name | |
|---|---|
| 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 | |
| Clinical data | |
| |
| Oral | |
| Identifiers | |
| 1370468-36-2 | |
| Chemical data | |
| Formula | C49H55N9O7 |
| 882.015 g/mol | |
|
SMILES
| |
Elbasvir (MK-8742) is an experimental drug for the treatment of hepatitis C. It is being developed by Merck and is currently in 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.[1]
Elbasvir is a highly potent and selective inhibitor of the hepatitis C virus NS5a replication complex.[2] 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.[3]
References
- ↑ 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. 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. 2015;385(9973):1075-86. doi: 10.1016/S0140-6736(14)61795-5. PMID 25467591
- ↑ 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. Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity. ChemMedChem. 2013;8(12):1930-40. doi: 10.1002/cmdc.201300343. PMID 24127258
- ↑ Gentile I, Buonomo AR, Zappulo E, Borgia G. Interferon-free therapies for chronic hepatitis C: toward a hepatitis C virus-free world? Expert Review of Anti-Infective Therapy. 2014 Jul;12(7):763-73. doi: 10.1586/14787210.2014.929497. PMID 24918116
| ||||||||||||||||||||||||||||||||||||||||||