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Safety and Pharmacokinetics of BMS-650032 Following Multiple Ascending Doses for 14 Days in Healthy Subjects
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Reported by Jules Levin
ICAAC Sept 14 2010 Boston
T. ELEY1, C. PASQUINELLI1, P. WENDELBURG1, C. VILLEGAS1 , B. HE1, S. LIAO1, H. JIANG1, T. MARBURY2, R. BERTZ1, D. GRASELA1
1Bristol-Myers Squibb, Princeton, NJ, 2Orlando Clinical Res. Ctr., Orlando, FL
Introduction
The HCV NS3/4A protease is an essential enzyme for viral replication and
has been validated as a target for anti-HCV therapy in clinical trials
BMS-650032 is a potent and selective HCV NS3 protease inhibitor with
in vitro picomolar potency vs. NS3/4A protease complexes in genotype
1a/1b
- Replicon EC50: Genotype 1a (4 nM); Genotype 1b (1 nM)
- In vitro: synergistic with IFN-α and other HCV inhibitors
BMS-650032 was generally well tolerated at single doses up to 1200 mg in
healthy subjects and 600 mg in HCV-infected subjects
Antiviral activity observed following three days of dosing in HCV-infected
subjects suggests that doses of 200-600 mg twice daily may be
therapeutic1
Objectives
Primary Objective:
To assess the safety and tolerability of multiple doses of BMS-650032 in
the range of 10 to 600 mg twice daily in healthy subjects
Secondary Objectives:
To assess the effect of multiple oral doses of BMS-650032 on
electrocardiographic (ECG) parameters including heart rate, PR, QRS, QT,
QTc intervals
To assess the pharmacokinetics of BMS-650032 following single and
multiple oral doses, including accumulation index, time to steady-state,
and diurnal variation in healthy subjects
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