AIDS TREATMENT NEWS No. 117 - December 21, 1990
John S. James
The antiviral, named BI-RG-587, was found by a systematic strategy for synthesizing and screening chemicals likely to be active against HIV-1 reverse transcriptase (RT), but without the toxicity of the nucleoside analog RT inhibitors such as AZT, ddC, and ddI. BI-RG-587 inhibited several strains of HIV-1 at low concentrations (under 50 nM) in cell cultures. Over 8,000 times the concentration was needed to be toxic to human cells. The chemical was so specific to HIV-1 that it had no effect on HIV-2, or on any other virus tested; this great specificity may help to reduce side effects. BI-RG-587 was also effective against HIV-1 strains obtained from four patients using AZT; we do not know the concentration used in these tests.
In animals, BI-RG-587 could be given orally. In monkeys, a single dose produced plasma levels 35 to 140 times the concentration needed to inhibit HIV-1 in the cell-culture tests, and these levels were maintained during an eight-hour period. In chimpanzees, 600 times the required concentration was achieved. The drug did cross the blood-brain barrier very well in the animal tests.
BI-RG-587 is a simple molecule which appears not difficult to synthesize -- important so that if it proves effective, there will not be delays due to manufacturing problems.
The developer of BI-RG-587 -- Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut -- was not previously known to be working on AIDS. However, rumors were furiously circulating shortly before the December 7 announcement, suggesting that the German parent company was starting tests of an AIDS drug.
AIDS TREATMENT NEWS has learned that the U. S. company has plans to file an IND (Investigational New Drug application) in January 1991, and has hopes of starting a U. S. trial by March.
Despite encouraging laboratory results, only human trials can tell if the drug will work. Another non-nucleoside RT inhibitor -- a TIBO derivative, the first one tested in humans -- showed similar promise in laboratory and animal tests, but seems not to be effective in patients. Other companies also are developing their own lines of non-nucleoside RT inhibitors. No one knows in advance which ones will be successful. But what can be done is to make sure that there are no unnecessary obstacles or delays in finding out.
References
1. Merluzzi VJ, Hargrave KD, Labadia M, and others. Inhibition of HIV-1 Replication by a Nonnucleoside Reverse Transcriptase Inhibitor. Science. December 7, 1990; volume 250, pages 1411-1413.
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