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New AIDS drug discoveries to battle drug-resistant HIV strains

NEW BRUNSWICK/PISCATAWAY, N.J. Belgian and American scientists have collaborated in discovering several new potential anti-AIDS drugs, including compounds that can block all known drug-resistant strains of the virus. While current anti-HIV therapies have saved lives, the emergence of drug-resistant strains of the rapidly mutating virus has been a major obstacle to successful long-term treatment.

Two of the new drugs, Dapivirine (also called R147681 or TMC120) and R165335 (also called TMC125), are derived from the dianilinopyrimidine (DAPY) family of highly potent compounds. Both have shown great promise in Phase I and Phase II clinical trials.

Dapivirine, based on its ease of manufacture and low cost, is a viable candidate for treating AIDS in the developing world, home to 95 percent of all HIV-infected patients, the researchers said. It is also being tested as a microbicide to prevent the transmission of HIV.

A third compound (R278474), scheduled for Phase I trials, is even more active against common HIV strains and all the mutants tested, according to the researchers.

The team developing the drugs includes scientists from Rutgers, The State University of New Jersey, and the National Institutes of Health (NIH) in the United States; and from Janssen Pharmaceutica in the United States and Belgium and Tibotec-Virco, N.V. in Belgium, both subsidiaries of Johnson & Johnson.

In a presentation at the 224th American Chemical Society (ACS) national meeting in Boston (MEDI 206), Bart De Corte of Janssen Pharmaceutica described the drugs and Paul Lewi of the Center for Molecular Design (CMD) at Janssen Pharmaceutica in Belgium discussed the strategies used to design the drug molecules.

The research effort, which has been conducted under the overall guidance of Dr. Paul Janssen, began more than 10 years ago. Janssen, founder of Janssen Pharmaceutica, has been a leader in drug discovery and has developed drugs u
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Contact: Joseph Blumberg
blumberg@ur.rutgers.edu
732-932-7084 x652
Rutgers, the State University of New Jersey
19-Aug-2002


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