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Professor of Clinical Pharmacy, Department of Clinical Pharmacy, School of Pharmacy, University of California at San Francisco, San Francisco, CA
Assistant Clinical Professor, Department of Clinical Pharmacy, School of Pharmacy, University of California at San Francisco
Reprints: Dr. Dong, Department of Clinical Pharmacy, School of Pharmacy, University of California at San Francisco, 521 Parnassus Ave., C-152, Box 0622, San Francisco, CA 94143-0622, fax 415/476-6632, dongb{at}pharmacy.ucsf.edu
OBJECTIVE: To review the efficacy, safety, pharmacology, virology, pharmacokinetics, and resistance of the nonpeptidic protease inhibitor (PI) tipranavir.
DATA SOURCES AND STUDY SELECTION: A PubMed search (1966-February 2006) was conducted using the key words tipranavir or PNU-140690, with the limitation of English-language reports. Pharmacokinetic and randomized clinical trials originating from major HIV conferences, such as the Conference on Retroviruses and Opportunistic Infections, International AIDS Society, European AIDS Conference, and Interscience Conference on Antimicrobial Agents and Chemotherapy, published only in abstract form, from 2000 to February 2006, were reviewed for relevance and included in this review.
DATA SYNTHESIS: Phase III studies have shown that tipranavir is effective in the treatment of PI-resistant HIV compared with other PI-containing regimens. Adverse effects associated with tipranavir/ritonavir therapy include gastrointestinal reactions, hepatotoxicity, and elevations in cholesterol and triglyceride levels. Resistance data suggest that tipranavir/ritonavir should be reserved for salvage therapy in antiretroviral-experienced patients who have previously failed standard PI therapies. The potential for hepatotoxicity and drug interactions and the expense of tipranavir due to required ritonavir boosting may limit its widespread use.
CONCLUSIONS: Tipranavir/ritonavir is an essential addition to the antiretroviral armamentarium for HIV-infected patients with limited treatment options.
Key Words: antiretroviral, HIV, protease inhibitor, tipranavir
Published Online, June 20, 2006. www.theannals.com, DOI 10.1345/aph.1G598
THIS ARTICLE IS APPROVED FOR CONTINUING EDUCATION CREDIT
ACPE UNIVERSAL PROGRAM NUMBER: 407-000-06-016-H02