2009 Safety and Antiviral Activity of Ana598 in Combination With Pegylated Interferon Α2a Plus Ribavirin in Treatment-Naive Genotype-1 Chronic HCV Patients

Rapid and strong antiviral activity of the non-nucleosidic NS5B polymerase inhibitor BI 207127 in combination with peginterferon alfa 2a and ribavirin

“…The palm pocket 1 NS5B polymerase inhibitor ANA598 was dosed at either 200 mg (n = 29) or 400 mg (n = 34) BID in combination with PegIFN/RBV in GT-1 TN patients [20,21]. In total 56% and 42% of patients in the 200 and 400 mg arms, respectively, demonstrated RVR, compared with 13% of patients receiving Peg-IFN/RBV plus placebo.…”

An Objective Assessment of Conformational Variability in Complexes of Hepatitis C Virus Polymerase with Non-Nucleoside Inhibitors

“…However, mutations far from the binding sites have not been specifically characterized and are in fact usually not reported at all. Still, a careful search of the available literature indicates that mutations that are not in (first sphere) or near (second sphere) the binding pockets have been reported under antiviral pressure with NNIs binding to sites III, [15][16][17][18][19]21 and II. [22][23][24][25] Strikingly, off-site mutations are consistently found for these three classes of NNIs in the hinges we defined in the detailed mapping of the moving parts of NS5B (Table 4).…”

New developments in small molecular compounds for anti-hepatitis C virus (HCV) therapy

“…Twelve-week results for the first cohort (200 mg BID) reported no serious adverse events except for those associated with SOC. The combination of ANA598 with SOC was well tolerated; ANA598 accelerated the rate of achieving undetectable virus in HCV-1 subjects (Lawitz et al, 2010a).…”