MEDICAL UPDATE: The Status of Protease Inhibitors


MEDICAL UPDATE: The Status of Protease Inhibitors

Being Alive; February 1994
Mark Katz MD and reported by Jim Stoecker

At last count, at least 18 companies have some sort of protease inhibitor in some stage of development. There is hope that out of all this activity will come a drug that works and that will make a significant contribution to the fight against HIV.

One big issue is that of bioavailability. You need a product that delivers enough drug to be effective. The protease inhibitor developed by Abbott required continuous intravenous infusion to deliver enough drug. This was obviously not practical, and this product development has been stopped. Roche developed an oral form that has been tested in Europe and soon begins Phase III testing at 40 sites in this country.

Meanwhile, Merck developed a protease inhibitor that has a longer half life than the Roche product. This means that it may only need to be taken twice daily, as opposed to three or four times daily for some of the other oral formulations. So, the bioavailability issue is being actively worked on.

In addition to the bioavailability issue, there is the question of how many steps it takes to synthesize the drug. The number of steps determines how costly the drug is to manufacture and thus how expensive it will be for the consumer to purchase.

Dupont-Merck has a protease inhibitor that takes only 12 steps to synthesize. Early studies, however, show that the drug may be poorly absorbed. In contrast, the better absorbed Merck product mentioned above takes 33 steps to synthesize and thus is far more costly to produce.

So, the race is on to develop a protease inhibitor that works, that is easy to administer, and that is relatively simple to make. With so many manufacturers involved in this effort, the hope is that we will have a winner in the not too distant future.


940201
BA940203

AEGiS is made possible through unrestricted grants from Roxane Laboratories, the National Library of Medicine, and donations from users like you. Always watch for outdated information. Always watch for outdated information. This article first appeared in 1994. This material is designed to support, not replace, the relationship that exists between you and your doctor.

Copyright © 1994 - Beings Alive. Permission granted for noncommercial reproduction, provided that our address and phone number are included if more than short quotations are used. Subscription lists are kept confidential. Being Alive, 621 N. San Vicente Blvd., West Hollywood, CA 90069, Tel - 310.289.2551; FAX - 310.289.9866; Email: BeiAlive@aol.com  http://www.beingalivela.org/

This information is designed to support, not replace, the relationship that exists between you and your doctor.
©1994. AEGIS.