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BMS-790052 is a First-in-class Potent Hepatitis C Virus (HCV) NS5A Inhibitor for Patients with Chronic HCV Infection: Results from a Proof-of-concept Study
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Reported by Jules Levin
20th Conference of the APASL, China National Convention Center, 25 - 28 March 2010, Beijing, China. Poster #321
Richard E Nettles1, Caly Chien1, Ellen Chung1, Anna Persson1, Min Gao1, Makonen Belema1, Nicholas Meanwell1, Michael DeMicco2, Thomas Marbury3, Ronald Goldwater4, Patrick G Northup5, John Coumbis1, Walter K Kraft6, Michael Charlton7, Juan Carlos Lopez-Talavera1, Dennis M Grasela1.
1Bristol-Myers Squibb, Research and Development, Princeton, NJ; 2Advanced Clinical Research Institute, Anaheim, CA; 3Orlando Clinical Research Center, Orlando, FL; 4PAREXEL International, Baltimore, MD;
5University of Virginia, Charlottesville, VA; 6Thomas Jefferson University, Philadelphia, PA; 7Mayo Clinic, Rochester, MN
BACKGROUND
NS5A is an essential component of the hepatitis C virus (HCV) replication complex
BMS-790052 is a first-in-class, highly selective, oral HCV NS5A inhibitor
BMS-790052 has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a and 1b
BMS-790052 has additive to synergistic effects in combination with interferon and other HCV inhibitors in vitro
In a single ascending dose study in healthy non-HCV infected patients (Protocol AI444-001), BMS-790052:
- was safe and well tolerated
- had a pharmacokinetic (PK) profile suggesting the possibility of once-daily dosing
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