Call Today
1-800-238-7828
 |
|
  
Novel HIV-1 protease inhibitor well tolerated; shows antiretroviral activity
Last Updated: 2001-04-10 12:24:51 EDT (Reuters Health)
SEATTLE (Reuters Health) - A potent, selective inhibitor of the HIV-1 protease that belongs to a novel chemical class has shown good antiviral activity and tolerability at all dosages tested, according to results of a phase I/II trial presented here Monday at the 14th International Conference on Antiviral Research.
DMP450 (Mozenavir) is a nonpeptidomimetic, water-soluble cyclic urea. The phase I/II trial was a randomized, indinavir-controlled dose-escalation study, which looked at the antiretroviral activity and safety of escalated doses of DMP450, said Dr. Carey Moxam, who presented the data on behalf of Triangle Pharmaceuticals, of Durham, North Carolina, which has worldwide license rights to DMP450 through their acquisition of Avid Corporation.
The antiretroviral-naive patients were sequentially randomized to receive DMP450 in one of three doses (750 mg three times a day, 1250 mg twice a day or 1250 mg three times a day) or indinavir 800 mg three times a day. Stavudine and lamivudine were added to all of the treatment groups.
At baseline, all patients had a viral load greater than 10,000 copies/mL but less than 300,000 copies/mL. Viral loads across the cohorts were fairly similar, explained Dr. Moxam.
"There was a very rapid response to suppress viral load below the limit of detection in all four cohorts," Dr. Moxam said. At the end of the 48-week trial, the majority of patients experienced suppression of plasma HIV-1 RNA levels to less than 50 copies/mL in all treatment arms.
In general, most adverse events were mild. Among the study enrollees, there were only seven cases of serious adverse events, Dr. Moxam reported. The incidence of diarrhea was higher in patients taking indinavir, and nausea was about the same for both drugs. There was a significant increase in the incidence of rash with DMP450 dose escalation, suggesting that this event may be dosage related, Dr. Moxam said. DMP450 also appears to have less of an effect on total cholesterol levels compared with indinavir, he added.
DMP450 is currently on partial clinical hold here in the US because of concerns over a QVC prolongation that had been observed in animals exposed to high doses of the drug. This current trial was conducted at six sites in France, Mexico, Spain and Germany. There was no effect on QVC prolongation noted in this study, or any other similar abnormalities.
"Mozenavir is an attractive HIV protease inhibitor with a straightforward chemical synthesis, limited pharmacokinetic interactions and limited metabolism by CYP450," Dr. Moxam told the attendees. It produces antiretroviral activity similar to indinavir and is well tolerated through week 48.
-Westport Newsroom 203 319 2700
|
Copyright 2001 Reuters Limited. All rights reserved. Republication or redistribution of Reuters Limited content, including by framing or similar means, is expressly prohibited without prior written consent of Reuters Limited. Reuters Limited shall not be liable for any error or delays in the content, or for any actions taken in reliance thereon.
|
|
 Back To HIV Wellness Center
|
