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Biotech / Medical : Agouron Pharmaceuticals (AGPH)

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To: Izzy who wrote (2785)11/14/1997 5:04:00 PM
From: JOHN W.  Read Replies (1) of 6136
 
Subject: Pharmacology
Date: Fri, Nov 14, 1997 09:33 EST
From: LMoss
Message-id: <19971114143300.JAA16195@ladder01.news.aol.com>

Contrary to a statement posted recently, Fortovase is indeed saquinavir, but in a soft gel formulation. The purpose of the new formulation is to slow down its release in the body, where it is quickly metabolized by the liver.

In its original formulation, only about 4% of ingested saquinavir was biologically effective, and rapid metabolization reduced serum concentrations below those thought to be necessary during part of the day. Accordingly, saquinavir was not one of the protease inhibitors recommended by the NIH panel for HAART treatment of HIV.

The soft gel formulation will increase bioavailability to about 14%, and moderate the sharp peak-and-valley concentration produced by the original formulation.

Another approach is to slow down the rate of metabolization of saquinavir. One of the drugs that happens to do this is Viracept. Taken with saquinavir, it increases the bioavailability of the latter to about 20%. Taken with saq's soft-gel formulation (Fortovase) it should do even better. That is one reason this combination may prove to be the PI treatment of choice.

LMoss

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