Second International Congress Drug Therapy in HIV Infection 18-22 November 1994 Glasgow, UK

NEW ANTI-VIRALS

Mark A. Wainberg
McGill University AIDS Centre Jewish General Hospital 3755 Cote-Ste-Catherine Road Montreal, Canada H3T lE2

Int Cong Drug Therapy HIV 1994 Nov 18-22;2:Abstract No. 11.1
AIDS 1994, Vol. 8 (Suppl. 4);S9

New anti-HIV compounds have been developed to antagonize each of the viral reverse transcriptase (RT) and protease activities. It is hoped that certain of these drugs will not be prone to problems of HIV resistance associated with earlier generations of both nucleoside and non-nucleoside inhibitors of RT and peptide inhibitors of protease.

Although tissue culture selection protocols with non-nucleoside antagonists of RT gave rise to rapid emergence of drug resistance, there is evidence that these drugs may act synergistically with nucleosides and that, in some cases, they may help to overcome resistance against the latter drugs. With regard to nucleosides, novel heterosubstituted compounds, that contain O and S atoms in their sugar moiety, have been generated that can inhibit viral RT activity at concentrations of 0.01 - 0.05 μM. Interestingly, selection for resistance against these drugs has been difficult to achieve and phase I trials are currently being planned.

The HIV protease represents a highly attractive target for anti-viral chemotherapy, in spite of the fact that selection of viruses resistant to peptide inhibitors of this enzyme has been easy to achieve in culture - New generations of protease antagonists include cyclic urea compounds, against which selection for resistance may be relatively difficult to achieve. The advent of these new compounds creates grounds for renewed optimism in the treatment of HIV-associated disease.

Presenting author: Mark A. Wainberg

1994-11-18
11.1

Originally published in AIDS Volume 8, Supplement 4 and hosted with permission of the publisher Lippincott Williams & Wilkins, 250 Waterloo Road, London, SE1 8RD, UK. Tel: +44 (0)20 7981 0700 Fax: +44 (0) 7981 0701

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