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Pharmacokinetics of VM-1500 20 mg and 40 mg in
Healthy and HIV-Infected Patients
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Reported by Jules Levin
IAC Melbourne 2014
Winai Ratanasuwan1, Peerawong Werarak1, Angela Koryakova4, Baiba Berzins5, Vadim Bichko2,3, *Robert Murphy5
1Siriraj Hospital/Mahidol University, Bangkok, Thailand, 2ChemDiv,Inc., San Diego,USA, 3Viriom Ltd, San Diego, CA, USA,
4Chemical Diversity Research Institute, Moscow, Russia, 5Northwestern University, Chicago, USA
potentially, once per week.....metabolite half life is really long.
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program abstract
Background: VM-1500 is the prodrug of the active compound VM-1500A, a highly active and selective HIV non-nucleoside reverse transcriptase inhibitor which demonstrated a 1.73 to 1.8 log10 decrease in HIV viral load after 7 days of therapy in treatment-naïve HIV-infected patients.
Methods: Uninfected healthy volunteers were randomized (7:1) to receive a single oral dose of VM-1500 20 mg, 40 mg or placebo. In the second part of the study, HIV-infected treatment-naive patients were randomized to VM-1500 20 mg, 40 mg or placebo once daily for 7 days. Plasma samples were collected over 24 hours after the Day 1 and Day 7 doses and at 14, 21, and 36 days of follow-up. VM-1500 and VM-1500A plasma concentrations were measured using LC-MS/MS method, and PK parameters were calculated.
Results: 7 patients in each cohort received VM-1500. The mean half-life (T1/2) of a single 20 mg dose of VM-1500 in HIV-infected patients was 1.7 hours, and 2.6 hours for the 40 mg dose. T1/2 of the metabolite VM-1500A was 8.9 and 8.8 days for the 20 and 40 mg doses, respectively. The Table shows the PK parameters for 7 days of dosing in HIV-infected patients and the Figure plots the VM-1500A concentrations.
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