Grapefruit Juice and Saquinavir

Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

Grapefruit Juice and Saquinavir

AIDS Treatment News (11/17/95) No. 235, P. 5
James, John S.

Hoffmann-La Roche's saquinavir has very low bioavailability, in part, because it is poorly absorbed and because it is quickly destroyed by an enzyme called CYP3A4. A small study of the protease inhibitor in 12 HIV-negative subjects showed that chemicals in grapefruit juice inhibit that enzyme. Participants who drank one glass of grapefruit juice with the saquinavir, and then another glass an hour later saw their AUCs (areas under the curve, a measure of the total exposure of the drug) increase 50 percent to 150 percent. The AUC of saquinavir was increased to 220 percent when double-strength grapefruit juice was given. Despite such results, there could be some uncertainties or drawbacks in taking grapefruit juice saquinavir to increase the efficacy of a low dose. First, the effects of the juice--which can vary from batch to batch--can also vary from person to person. Also, there is no way to determine for oneself whether the juice is working because the test to measure saquinavir in the blood is not generally available. A third concern is that some other drugs are also metabolized by the same enzyme and large amounts of grapefruit juice could therefore increase their levels in the blood enough to cause toxicity. For these and other reasons, Hoffmann-La Roche will not pursue the grapefruit juice method, and is instead designing a new formulation of saquinavir which raises bioavailability by about 300 percent.

951218
AD952254

Copyright © 1995 - Information, Inc., Bethesda, MD. The CDC National Center for HIV, STD and TB Prevention provides the following information as a public service only. Providing synopses of key scientific articles and lay media reports on HIV/AIDS, other sexually transmitted diseases and tuberculosis does not constitute CDC endorsement. This daily update also includes information from CDC and other government agencies, such as background on Morbidity and Mortality Weekly Report (MMWR) articles, fact sheets, press releases and announcements. Reproduction of this text is encouraged; however, copies may not be sold, and the CDC HIV/STD/TB Prevention News Update should be cited as the source of the information. Contact the sources of the articles abstracted below for full texts of the articles.

AEGiS is a 501(c)3, not-for-profit, tax-exempt, educational corporation. AEGiS is made possible through unrestricted funding from Boehringer Ingelheim, Bridgestone/Firestone Charitable Trust, Elton John AIDS Foundation, the National Library of Medicine, AIDS Walk of Orange County, and donations from users like you.

Always watch for outdated information. This article first appeared in 1995. This material is designed to support, not replace, the relationship that exists between you and your doctor.

AEGiS presents published material, reprinted with permission and neither endorses nor opposes any material. All information contained on this website, including information relating to health conditions, products, and treatments, is for informational purposes only. It is often presented in summary or aggregate form. It is not meant to be a substitute for the advice provided by your own physician or other medical professionals. Always discuss treatment options with a doctor who specializes in treating HIV.

Copyright ©1980, 1995. AEGiS. All materials appearing on AEGiS are protected by copyright as a collective work or compilation under U.S. copyright and other laws and are the property of AEGiS, or the party credited as the provider of the content.