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The Upjohn Protease Inhibitor (1/96)
Upjohn (now called Pharmacia & Upjohn, after the merger) has been in the process of developing, what we hope, will be a unique protease inhibitor. They have been trying to develop this product for a while; the first 2 generation inhibitors failed, but they are now trying again with the 3rd generation.
Unlike all of the current protease inhibitors in clinical development (which are peptide based protease inhibitors), the Upjohn product is a non-peptidic inhibitor with a lower molelcular weight. It is different structurally; it binds differently, because of being non-peptidic and structurally different; it binds to different amino acids. Therefore, Upjohn says, its major mutations are different. The promise of this is it may not have the same measure of cross-resistance problems as the current group of inhibitors in clinical development.
They are currently developing their 3rd generation protease inhibitor. The first (U-96,988) had sufficient absorption and safety but was not potent enough. The 2nd generation (U-103,017) was highly protein bound, rendering it ineffectual; the 3rd generation is less protein bound and much more potent than the other two generations.
They are currently conducting pre-clinical studies of several 3rd generation protease inhibitors. They are testing in vitro and in animals for potency, absorption and toxicity. They hope to be able to develop either 1 or possibly 2 of these compounds.
If all goes well, they are planning a human, single-dose phase I study in the 2nd half of 1996.
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About the author: Jules Levin is the Executive Director of NATAP, based in New York City.
The National AIDS Treatment Advocacy Project (NATAP) is a New York State non-profit corporation dedicated to facilitating the effort for development of effective treatment for HIV.
Last modified 1/27/96
by Jules Levin
copyright © 1996 natap
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