For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Ombitasvir (ABT-267) is an inhibitor of HCV NS5A. ABT-267 inhibits replication of HCV subgenomic replicons in cell culture assays with EC50 values of 14 pM and 5 pM against genotype 1a-H77 and 1b-Con1, respectively.<br>IC50 value: 14 pM and 5 pM (EC50, for genotype 1a-H77 and 1b-Con1) [2]<br>Target: HCV NS5A<br>in vitro: Ombitasvir is a NS5A inhibitor. [1] The EC50 value of ABT-267 against stable cell line replicons containing NS5A from HCV genotypes 2a, 2b, 3a, 4a, 5a or 6a was 12.4, 4.3, 19.3, 1.7, 3.2 or 366 pM, respectively. The relatively similar EC50 values for all major HCV genotypes are noted. It is likely that ABT-267 might have been a valuable drug for the treatment of genotype 3; however, it will only be available co-formulated with a NS3/4A inhibitor with significantly reduced activity against this genotype. Also, the lower activity against genotype 6a is noted. The molecular background for this has not been clarified. ABT-267 had a TD50 of > 32,000,000 pM in an MTT cytotoxicity assay, producing a therapeutic index that exceeded 2 million-fold. [2]</p>
| Catalog Number | I001034 |
| CAS Number | 1258226-87-7 |
| Molecular Formula | C50H67N7O8 |
| Purity | ≥95% |
| Target | HCV NS5A |
| Solubility | DMSO: ≥ 33 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 14 pM and 5 pM (EC50, for genotype 1a-H77 and 1b-Con1) [2] |
| Reference | </br>1:Ombitasvir, paritaprevir, and ritonavir, with or without dasabuvir, plus ribavirin for patients with hepatitis C virus genotype 1 or 4 infection with cirrhosis (ABACUS): a prospective observational study. Petta S, Marzioni M, Russo P, Aghemo A, Alberti A, Ascione A, Antinori A, Bruno R, Bruno S, Chirianni A, Gaeta GB, Giannini EG, Merli M, Messina V, Montilla S, Perno CF, Puoti M, Raimondo G, Rendina M, Silberstein FC, Villa E, Zignego AL, Pani L, Craxì A; ABACUS study group.; AIFA team..Lancet Gastroenterol Hepatol. 2017 Jun;2(6):427-434. doi: 10.1016/S2468-1253(17)30048-1. Epub 2017 Apr 10. PMID: 28497758 </br>2:Mechanisms and Predictions of Drug-Drug Interactions of the Hepatitis C Virus 3-Direct Acting Antiviral (3D) Regimen: Paritaprevir/Ritonavir, Ombitasvir and Dasabuvir. Shebley M, Liu J, Kavetskaia O, Sydor J, de Morais SM, Fischer V, Nijsen MJ, Bow DA.Drug Metab Dispos. 2017 May 8. pii: dmd.116.074518. doi: 10.1124/dmd.116.074518. [Epub ahead of print] PMID: 28483778 </br>3:Real-World Effectiveness of Ombitasvir/Paritaprevir/Ritonavir ± Dasabuvir ± Ribavirin in Patients with HCV Genotype 1 or 4 Infection: a Meta-Analysis. Wedemeyer H, Craxí A, Zuckerman E, Dieterich D, Flisiak R, Roberts SK, Pangerl A, Zhang Z, Martinez M, Bao Y, Calleja JL.J Viral Hepat. 2017 May 8. doi: 10.1111/jvh.12722. [Epub ahead of print] PMID: 28480525 </br>4:Efficacy and safety of ombitasvir/paritaprevir/ritonavir in dialysis patients with genotype 1b chronic hepatitis C. Atsukawa M, Tsubota A, Koushima Y, Ikegami T, Watanabe K, Shimada N, Sato S, Kato K, Abe H, Okubo T, Arai T, Itokawa N, Kondo C, Mikami S, Asano T, Chuganji Y, Matsuzaki Y, Iwakiri K.Hepatol Res. 2017 Apr 29. doi: 10.1111/hepr.12910. [Epub ahead of print] PMID: 28457003 </br>5:Real-world efficacy and safety of ritonavir-boosted paritaprevir, ombitasvir, dasabuvir ± ribavirin for hepatitis C genotype 1 – final results of the REV1TAL study. Lubel J, Strasser S, Stuart KA, Dore G, Thompson A, Pianko S, Bollipo S, Mitchell JL, Fragomeli V, Jones T, Chivers S, Gow P, Iser D, Levy M, Tse E, Gazzola A, Cheng W, Nazareth S, Galhenage S, Wade A, Weltman M, Wigg A, MacQuillan G, Sasadeusz J, George J, Zekry A, Roberts SK; Australian Liver Association Clinical Research Network (ALA CRN)..Antivir Ther. 2017 Apr 19. doi: 10.3851/IMP3168. [Epub ahead of print] PMID: 28422043 </br>6:Ombitasvir, paritaprevir, and ritonavir plus dasabuvir for 8 weeks in previously untreated patients with hepatitis C virus genotype 1b infection without cirrhosis (GARNET): a single-arm, open-label, phase 3b trial. Welzel TM, Asselah T, Dumas EO, Zeuzem S, Shaw D, Hazzan R, Forns X, Pilot-Matias T, Lu W, Cohen DE, Feld JJ.Lancet Gastroenterol Hepatol. 2017 Apr 13. pii: S2468-1253(17)30071-7. doi: 10.1016/S2468-1253(17)30071-7. [Epub ahead of print] PMID: 28416221 </br>7:Drug Induced Pneumonitis Secondary to Treatment with Paritaprevir/Ritonavir/Ombitasvir and Dasabuvir (VIEKIRA PAK®) for Chronic Hepatitis C: Case Report of an Unexpected Life-Threatening Adverse Reaction. Wu SY, Faire B, Gane E.Case Rep Med. 2017;2017:4895736. doi: 10.1155/2017/4895736. Epub 2017 Mar 20. PMID: 28408931 Free PMC Article</br>8:Ombitasvir, paritaprevir, and ritonavir plus ribavirin for chronic hepatitis C virus genotype 4 infection in Egyptian patients with or without compensated cirrhosis (AGATE-II): a multicentre, phase 3, partly randomised open-label trial. Waked I, Shiha G, Qaqish RB, Esmat G, Yosry A, Hassany M, Soliman R, Mohey MA, Allam N, Zayed N, Asselah T, Hall C, Redman R, Mobashery N, Doss W.Lancet Gastroenterol Hepatol. 2016 Sep;1(1):36-44. doi: 10.1016/S2468-1253(16)30002-4. Epub 2016 Jun 16. PMID: 28404110 </br>9:Ombitasvir, paritaprevir, and ritonavir plus ribavirin in adults with hepatitis C virus genotype 4 infection and cirrhosis (AGATE-I): a multicentre, phase 3, randomised open-label trial. Asselah T, Hézode C, Qaqish RB, ElKhashab M, Hassanein T, Papatheodoridis G, Feld JJ, Moreno C, Zeuzem S, Ferenci P, Yu Y, Redman R, Pilot-Matias T, Mobashery N.Lancet Gastroenterol Hepatol. 2016 Sep;1(1):25-35. doi: 10.1016/S2468-1253(16)30001-2. Epub 2016 Jun 16. PMID: 28404108 </br>10:Real-World Safety and Efficacy of Ombitasvir/Paritaprevir/Ritonavir/+Dasabuvir±Ribavirin (OBV/PTV/r/+DSV±RBV) Therapy in Recurrent Hepatitis C Virus (HCV) Genotype 1 Infection Post-Liver Transplant: AMBER-CEE Study. Tronina O, Durlik M, Wawrzynowicz-Syczewska M, Buivydiene A, Katzarov K, Kupcinskas L, Tolmane I, Karpińska E, Pisula A, Karwowska KM, Bolewska B, Jabłkowski M, Rostkowska K, Jakutiene J, Simonova M, Flisiak R.Ann Transplant. 2017 Apr 7;22:199-207. PMID: 28386057 Free Article |
