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UPJOHN ANNOUNCES NOVEL AIDS COMPOUND; MAY BE USEFUL AGAINST DRUG-RESISTANT STRAINS OF HIV

 UPJOHN ANNOUNCES NOVEL AIDS COMPOUND;
 MAY BE USEFUL AGAINST DRUG-RESISTANT STRAINS OF HIV
 KALAMAZOO, Mich., July 22 /PRNewswire/ -- Scientists from Upjohn Laboratories announced at the HIV Drug Resistance Meeting preceding the 8th International Conference on AIDS being held this week in the Netherlands that they have synthesized a compound that is considerably more potent in blocking growth of the HIV virus in human cells than the currently approved drugs AZT or ddI. Studies on the compound were done in collaboration with researchers at the University of California at Los Angeles Medical School and the University of Nebraska Medical Center.
 The compound, known as BHAP-E, works by blocking the activity of an essential viral enzyme known as reverse transcriptase (RT). BHAP-E is an analogue of U-87,201E, another Upjohn BHAP compound currently in clinical evaluation for treating AIDS.
 BHAP-E is the most potent RT inhibitor to date that has been reported, including other compounds currently on the market or in clinical trials.
 A major problem reported with the nonnucleoside RT inhibitors is that the HIV virus can mutate and acquire resistance to the compounds. Characterization of viruses resistant to BHAP compounds revealed novel mutations of the RT enzyme that were different from and not previously described with respect to other nonnucleoside RT inhibitors. Moreover, mutant RT enzymes resistant to other nonnucleoside RT inhibitors remain susceptible to inhibition by low concentrations of the potent BHAP-E.
 These data, in contrast to previous reports, indicate that cross- resistance among non-nucleoside RT inhibitors varies between compounds and raise the possibility that the BHAP compounds may be useful against drug resistant strains of HIV. Compound U-87,201E is currently in Phase II clinical trials. Phase I clinical trials with BHAP-E are scheduled to begin in September.
 "Drug resistance has been a major problem with the reverse transcriptase inhibitors that are currently available," said Jerry R. Mitchell, M.D., Ph.D., Corporate Executive Vice President and President of Upjohn Laboratories. "These laboratory studies on BHAP-E are important in that they show a potential use against drug resistant strains of HIV."
 The Upjohn Company (NYSE: UPJ) is a worldwide, research-based provider of human health care products, animal health products, agronomic and vegetable seeds and specialty chemicals. Headquartered in Kalamazoo, the company has been dedicated to improving health and nutrition for more than a century.
 -0- 7/22/92
 /CONTACT: Nancy H. Lassen of The Upjohn Company, 616-323-6902/
 (UPJ) CO: The Upjohn Company ST: Michigan IN: MTC SU: PDT


ML -- DE004 -- 1707 07/22/92 09:04 EDT
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Date:Jul 22, 1992
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