A new anti-HIV "entry inhibitor" drug called PRO 542 (Progenics Pharmaceuticals) has been well tolerated and shows anti-HIV benefits in phase I studies. Expanded phase II testing will be pursued, according to J. Jacobson, MD, from Mount Sinai Medical Center in New York City. A new CCR5 receptor antagonist drug called TAK-779 (Takeda Chemical Industries) was also described. In addition, an update on the new CXCR4 receptor antagonist drug called AMD3100 (AnorMED) was presented.
A new anti-HIV drug class-transcription inhibitors, or TIs-and its prototype were described. The TI temacrazine was presented by J.A. Turpin, MD, and colleagues from Serquest and Achillion Pharmaceuticals in Frederick, MD. Temacrazine blocks DNA transcription into RNA by using HIV's long terminal repeat region. Only nanomolar concentrations were necessary to inhibit HIV growth in the laboratory.
New non-nucleoside reverse transcriptase inhibitors (NNRTIs) described at the 39th ICAAC include PNU-142721 (Pharmacia & Upjohn), GW420867X (Glaxo Wellcome), UC781 (Bristol-Myers Squibb and Uniroyal), SJ-3366 (Samjin Pharmaceuticals), and Calanolide A (Sarawak MediChem Pharmaceuticals). The latter drug shows activity against the common NNRTI-associated mutations Y181C and K103N.
Two new nucleoside analogs (NRTIs) were described at the 39th ICAAC: dOTC, or BCH-10652 (BioChem Pharma) and DAPD (Triangle Pharmaceuticals), which displays activity against HIV and hepatitis B virus (HBV). According to R. Wood, MD, from Somerset Hospital in Cape Town, South Africa, dOTC showed anti-HIV effects and was well tolerated in a phase I/II clinical trial.
Two new PIs were also reported on: VX-175/GW433908 (Vertex and Glaxo Wellcome), a prodrug of amprenavir (Agenerase), and UIC-94-003.