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A Single Monotherapy Dose of MK-8591,a Novel NRTI, Suppresses HIV for Ten Days
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Reported by Jules Levin
CROI 2016 Feb 22-24 Boston
"MK-8591 administered once-weekly in an SIV rhesus macaque model demonstrated potent antiviral efficacy. Clinically, MK-8591-TP exhibited a half-life of ∼150-160 hrs in human PBMCs with C168hr exceeding projected efficacious concentrations at doses of >10 mg.....In an open-label study in HIV-1–infected subjects naÏve to antiretroviral treatment (ART), subjects are being administered a single dose of MK-8591 across a range of doses. ....A single 10-mg dose of MK-8591 was associated with a rapid and robust reduction in VL. At 168 hours postdose, a mean (95% CI) VL reduction of 1.67 log10 (1.47, 1.87) was observed. .....MK-8591 suppressed HIV replication for at least ten days when administered as a single 10-mg dose. The low dose and potent antiviral effect of MK8591 provide a platform for extended duration oral and parenteral formulations....."
Evan J. Friedman1; Dirk Schurmann2; Deanne Jackson Rudd1; Sabrina Fox-Bosetti1; Sandra Zhang1;Martine Robberechts1; Andreas Huser2; Daria Hazuda1; Marian Iwamoto1; Jay A. Grobler1 on behalf of the HIV Early Development Team
1Merck & Co., Inc., Kenilworth, NJ, USA; 2Charite Universitatsmedizin Berlin, Research Hospital, Berlin, Germany
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