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PSI-352938, A Novel Purine Nucleotide Analog, Exhibits Potent Antiviral Activity and No Evidence of Resistance in Patients with HCV Genotype 1 Over 7 Days
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Reported by Jules Levin EASL 2011 Berlin March 31-Apr 2
M Rodriguez-Torres1, E Lawitz2, J Denning3, M Cornpropst3, E Albanis3, WT Symonds3, MM Berrey3 1Fundacion de Investigacion de Diego, Santurce, PR, 2Alamo Medical Research, San Antonio, TX 3Pharmasset, Inc., Princeton, NJ
INTRODUCTION
PSI-352938 (PSI-938) is a novel purine nucleotide analog polymerase inhibitor in clinical development for the treatment of chronic HCV. PSI-938 demonstrates potent, broad-genotype antiviral activity in vitro, maintains activity against S282T mutants, achieves high liver:plasma ratios in preclinical studies and has low risk of drug interaction. PSI-938 was created as an optimal partner DAA for the pyrimidine nucleotide analog, PSI-7977. A first-in-human healthy subject study demonstrated that single doses up to 1600 mg were well tolerated. Pharmacokinetics supported QD dosing. These data, coupled with PSI-938's high barrier to resistance, supported progression to a 7-day, dose-ranging monotherapy study in HCV-infected subjects.
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