This excerpt taken from the MYGN 8-K filed Jun 22, 2009.
MPC-4326 (bevirimat dimeglumine) is a first-in-class, small molecule inhibitor of HIV-1 maturation we are developing for the oral treatment of HIV infection that we recently acquired from Panacos Pharmaceuticals, Inc. MPC-4326 interferes with a late step in the processing of the HIV-1 Gag protein. This inhibition leads to formation of noninfectious, immature virus particles, thus preventing subsequent rounds of HIV infection. It has demonstrated potent activity against a broad range of HIV strains, and laboratory studies have shown MPC-4326 to be an inhibitor of HIV isolates that are resistant to a large range of currently approved HIV drugs. To date, over 675 subjects, including over 180 HIV-infected patients, have been studied in clinical trials of MPC-4326. Results from these trials have shown MPC-4326 to be well tolerated and have demonstrated significant and clinically relevant reductions in
viral load in a large subset of HIV-infected patients representing approximately 60-70% of HIV-infected patients. These patients can be identified by a simple, rapid and inexpensive assay of the HIV virus.
In the most recent Phase 2 clinical trial of MPC-4326, designed to examine the oral bioavailability of a new tablet formulation, 32 treatment-naive and treatment-experienced HIV patients were recruited, MPC-4326 met its primary objective by demonstrating drug plasma levels to be in a target range for virologic reduction. After 14 days of treatment with MPC-4326 given twice daily at doses of 200 mg or 300 mg, all 32 patients had steady state MPC-4326 plasma concentrations well above the previously identified minimum drug level necessary to maintain anti-viral activity. In addition, MPC-4326s safety profile was comparable to earlier studies where it had been indistinguishable from placebo. Across all trials of MPC-4326 in which a total of 678 people had been treated with MPC-4326 through the end of 2008, there has been one serious adverse event involving an HIV-positive patient suffering a stroke, which was considered possibly related to treatment. Other reported adverse events of mild or moderate intensity that appear to be related to treatment with MPC-4326 include diarrhea, nausea, headache and dizziness. MPC-4326 has a very good oral bioavailability and a half life in humans in excess of 24 hours. We expect to initiate a Phase 2b clinical trial of MPC-4326 in treatment-experienced HIV patients in the second half of 2009.