Gay Men's Health Crisis: Treatment Issues, Volume 7 no. 7 July/August, 1993

GEM 91: GEM (gene expression modulation) 91 is an antisense oligonucleotide produced by Hybridon, Inc. of Worcester, Massachusetts. Antisense oligonucleotides inhibit genes which are necessary for viral replication. Hybridon has submitted an application to both the FDA and the Clinical Trial Committee in France to begin phase I clinical studies. Most analysts predict that clinical studies of the drug will first begin in France.

Topotecan: Topotecan is an analog of camptothecin, a toxic anticancer drug made from the wood of the Chinese tree Camptotheca acuminata. Dr. Clyde Crumpacker from Boston's Beth Israel Hospital presented preliminary test tube data which shows that topotecan inhibited p24 antigen production and mRNA production in transfected human epithelial cells. Topotecan's mechanism of anti-HIV action is not yet known.

SC-49483: SC-49483 is the prodrug of N-butyl DNJ, a glucosidase inhibitor. Glucosidase inhibitors block the addition of sugar molecules to HIV's outer envelope. Sugar molecules are a necessary component of HIV's structure; without them, the virus becomes noninfectious. An earlier clinical study of N-butyl DNJ demonstrated that the drug is toxic. It inhibited normal intestinal functioning, resulting in improper carbohydrate absorption and intense diarrhea. Scientists from Monsanto Searle, the drug's manufacturer, hope that SC-49483 will be converted into N-butyl DNJ after it passes through the intestines, avoiding the diarrhea.

PIC 024-4 and PRO-189: Procepts, Inc, a Massachusetts company, presented preliminary data on their two lead anti-binding compounds PIC 024-4 and PRO-189. These compounds block the interaction of the CD4 receptor and HIV gp120, HIV's main gateway into human cells. Procept scientists hope that these compounds will prevent HIV from infecting new cells.

Synthetic Humates: A research team from the Institute of Medical Microbiology in Freiburg, Germany presented data on the ability of synthetically produced humates to block the CD4-gp120 interaction. Humates come from the decaying organic matter found in coal, soil, and peat. Melanins, another proposed anti-HIV agent, are related compounds.

Triterpine Derivatives: Rhone Poulenc Rorer, the French drugs giant, presented data on RPR 103611, a triterpine derivative. RPR 103611 does not inhibit integrase, protease, or reverse transcriptase, three common targets for new anti-HIV drugs. Although its exact mechanism of action is still unknown, Rhone Poulenc scientists believe that the compound inhibits HIV at an early point in its life cycle. Triterpines are a class of substances isolated from plants, particularly the root of Tripterygium wilfordii.

New Reverse Transcriptase Inhibitors: Eli Lilly, an Indianapolis- based drug company, and Hoescht AG-Bayer, a collaboration of two German drug companies, each presented preliminary data on their new reverse transcriptase inhibitors. Lilly's drug LY73497 and Hoescht-Bayer's quinoxaline derivative both inhibit HIV reverse transcriptase in vitro, but are not nucleoside analogs like other RT inhibitors, such as AZT.

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