novel ccr5 antagonist reduces hiv viral load

Inpharma 1504 - 10 Sep 2005

Novel CCR5 antagonist reducesHIV viral load

GW 873140,* a spirodiketopiperazine CCR5antagonist, produced significant reductions in HIV RNAlevels in a short-term monotherapy study involving40 patients, 21 of whom were treatment-experienced.Patients were randomised to receive oral GW 873140 ata dose of 200mg or 400mg once daily, or 200mg or600mg twice daily, for 10 days, followed by a 14-daypost-treatment period; each cohort included10 patients, two of whom received placebo.

Mean reductions from baseline in HIV RNA levels atnadir** ranged from 0.46 log10copies/mL in the groupreceiving the 200mg once daily dose of GW 873140 to1.66 log10copies/mL in patients receiving the 600mgtwice daily dose; the proportions of patients achievingreductions in viral load of > 1 log10copies/mL in thesetwo groups were 17% and 100%, respectively. Incontrast, the mean reduction in viral load in placeborecipients was 0.12 log10copies/mL, and a reduction of> 1 log10copies/mL was not achieved in any of thesepatients. There was no difference in response betweentreatment-experienced and -naive patients.* Ono Pharmaceutical, GlaxoSmithKline; phase III for HIV infections inthe US** Nadir usually occurred on day 12 (range day 5–24).

Lalezari J, et al. Antiviral activity and safety of 873140, a novel CCR5 antagonist,during short-term monotherapy in HIV-infected adults. AIDS 19: 1443-1448, No.14, 23 Sep 2005 801017283

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Inpharma 10 Sep 2005 No. 15041173-8324/10/1504-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved