1. Academic Validation
  2. Current race in the development of DAAs (direct-acting antivirals) against HCV

Current race in the development of DAAs (direct-acting antivirals) against HCV

  • Biochem Pharmacol. 2014 Jun 15;89(4):441-52. doi: 10.1016/j.bcp.2014.04.005.
Erik De Clercq 1
Affiliations

Affiliation

  • 1 Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium. Electronic address: erik.declercq@rega.kuleuven.be.
Abstract

The direct-acting antivirals (DAAs) currently in development for treatment of hepatitis C fall into four categories: (i) NS3/4A protease inhibitors: ABT-450/r, faldaprevir, asunaprevir, GS-9256, vedroprevir (GS-9451), danoprevir, MK-5172, vaniprevir, sovaprevir, ACH-2684, narlaprevir and simeprevir, in addition to those that are already developed [telaprevir (Incivek®) and boceprevir (Victrelis®)], (ii) NS5A protein inhibitors: ABT-267, daclatasvir, ledipasvir, ACH-2928, ACH-3102, PPI-668, AZD-7295, MK-8742, and GSK 2336805; (iii) NS5B (nucleoside-type) polymerase inhibitors: sofosbuvir (now approved by the FDA since 6 December 2013), GS-0938, mericitabine, VX-135, ALS 2158 and TMC 649128; (iv) NS5B (non-nucleoside-type) polymerase inhibitors: VX-222, ABT-072, ABT-333, deleobuvir, tegobuvir, setrobuvir, VCH-916, VCH-759, BMS-791325 and TMC-647055. Future drug combinations will likely exist of two or more DAAs belonging to any of the 4 categories, with the aim to achieve (i) pan-genotypic hepatitis C virus (HCV) activity, (ii) little or no risk for resistance; (iii) short duration (i.e. 12 weeks) of treatment, and (iv) a sustained viral response (SVR) and definite cure of the disease.

Keywords

Asunaprevir (PubChem CID: 16076883); Boceprevir (PubChem CID: 10324367); Daclatasvir (PubChem CID: 25154714); Danoprevir (PubChem CID: 71301228); Deleobuvir (PubChem CID: 56948249); Direct-acting antivirals; Faldaprevir (PubChem CID: 71300931); Hepatitis C virus (HCV); Ledipasvir (PubChem CID: 67505836); Mericitabine (PubChem CID: 16122663); NS3/4A protease inhibitors; NS5A protein inhibitors; NS5B (non-nucleoside-type) polymerase inhibitors; NS5B (nucleoside-type) polymerase inhibitors; Narlaprevir (PubChem CID: 11857239); Neceprevir (PubChem CID: 71301413); Setrobuvir (PubChem CID: 45136829); Simeprevir (PubChem CID: 24873435); Sofosbuvir (PubChem CID: 45375808); Sovaprevir (PubChem CID: 53362096); Tegobuvir (PubChem CID: 23649154); Telaprevir (PubChem CID: 3010818); Vaniprevir (PubChem CID: 24765256); Vedroprevir (PubChem CID: 25167947).

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