Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.
PR Newswire - December 12, 1995
The Phase I/II trial announced today is a dose-ranging study designed to test the antiviral efficacy, tolerability and pharmacokinetics of VX-478 during four weeks of drug administration in HIV-positive individuals. The trial will initially investigate three dose levels: 300 mg twice daily; 300 mg three times daily and 450 mg twice daily. Higher doses may be explored based on the tolerability of VX-478 at the initial doses. VX-478 has been shown to be well-tolerated in Phase I clinical studies which evaluated single doses up to 1200 mg. To assess the anti-HIV activity of VX-478 at each dose level, the study will monitor CD4 counts and the viral load of the study participants. The data from this trial will be used by Glaxo Wellcome and Kissei to design advanced trials to assess the safety and anti-HIV efficacy of VX-478 alone and in combination with reverse transcriptase inhibitors.
"This Phase I/II trial builds on the strong tolerability, pharmacokinetics and bioavailability data generated for VX-478 in the Phase I trial completed earlier this year," commented Dr. Joshua Boger, President and Chief Executive Officer of Vertex. "This trial marks the beginning of an accelerated effort to move VX-478 through clinical development."
In July 1995, Glaxo Wellcome reported data from a Phase I trial of VX-478. In this study, VX-478 was well-tolerated and displayed excellent pharmacokinetics at the single doses tested, 150 mg, 300 mg, 600 mg, 900 mg and 1200 mg. The amount of VX-478 detected in the blood was directly proportional to the doses administered. At eight hours following administration, the level of VX-478 detected in the bloodstream for each of the doses was well above the IC90, the concentration of drug that eliminates 90 percent of HIV replication in vitro. The half-life of the compound ranged from approximately seven to ten hours, and oral bioavailability was calculated at greater than 70 percent.
HIV protease, a viral enzyme required by the virus for replication, is widely recognized as a promising therapeutic target for treatment of HIV infection and AIDS. The HIV protease is an alternative target to reverse transcriptase, the viral enzyme targeted by drugs such as Retrovir(R) (AZT), Videx(R) (ddI), Hivid(R) (ddC) and Epivir(TM) (3TC).
Vertex is engaged in the discovery, development and commercialization of novel, small molecule pharmaceuticals for the treatment of diseases for which there are currently limited or no effective treatments. The Company is a leader in the use of structure- based drug design, an approach to drug discovery that integrates advanced biology, biophysics and chemistry. The Company is concentrating on the discovery and development of drugs for the treatment of viral diseases, multidrug resistance in cancer, hemoglobin disorders, inflammation, autoimmune diseases and organ transplant rejection.
CONTACT: Lynne H. Brum, Director of Corporate Communications of Vertex, 617-499-2490, http://www.vpharm.com, or Gretchen L.P. Schweitzer of Feinstein Partners Inc., 617-577-8110/ 08:29 EST
Copyright (c) 1995/PR NewsWire. Reproduced with permission. Reproduction of this article (other than one copy for personal reference) must be cleared through the Permissions Desk, PR Newswire, 810 Seventh Avenue, New York, NY 10019.
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