TY - JOUR
T1 - Tipranavir
T2 - A new option for the treatment of drug-resistant HIV infection
AU - Temesgen, Zelalem
AU - Feinberg, Judith
N1 - Funding Information:
Potential conflicts of interest. J.F. has received recent research funding from Bristol Myers Squibb, GlaxoSmithKline, Boehringer-Ingelheim, Ti-botec Therapeutics, Achillion, Theratechnology, Pfizer, and Neurogesx; is a consultant for Bristol Myers Squibb, GlaxoSmithKline, Koronls, Immtech, Boehringer-Ingelheim, Tibotec Therapeutics, and Pfizer; and serves on the speakers’ bureau for Gilead Science, Bristol Myers Squibb, Abbott, GlaxoSmithKline, Merck, Boehringer-Ingelheim, and Tibotec Therapeutics. Z.T.: no conflicts.
PY - 2007/9/15
Y1 - 2007/9/15
N2 - Tipranavir is a recently approved nonpeptidic protease inhibitor specifically developed for the management of human immunodeficiency virus (HIV) infection in treatment-experienced patients with protease inhibitor-resistant infection. It is active against a wide range of drug-resistant laboratory- and patient-derived isolates. Tipranavir requires pharmacokinetic boosting by ritonavir (200 mg) to achieve therapeutic levels with twice-daily dosing and must be administered with food for optimal absorption. It is a potent protease inhibitor with a unique drug-resistance profile that offers advantages in the management of cases of multidrug-resistant HIV infection. Tipranavir (in combination with ritonavir) is both an inhibitor and inducer of cytochrome p450, with significant potential for drug-drug interactions, and therefore, it must be used cautiously when administered to patients who are receiving other drugs. Evolution of drug resistance after treatment failure with tipranavir is complex and is not yet fully understood. There is limited overlap in the resistance mutations that predict response to tipranavir and another new protease inhibitor, darunavir, which is active against drug-resistant isolates. Tipranavir is associated with elevations in alanine aminotransferase and aspartate aminotransferase levels, as well as elevated cholesterol and triglyceride levels, and can cause the typical gastrointestinal adverse effects associated with all protease inhibitors.
AB - Tipranavir is a recently approved nonpeptidic protease inhibitor specifically developed for the management of human immunodeficiency virus (HIV) infection in treatment-experienced patients with protease inhibitor-resistant infection. It is active against a wide range of drug-resistant laboratory- and patient-derived isolates. Tipranavir requires pharmacokinetic boosting by ritonavir (200 mg) to achieve therapeutic levels with twice-daily dosing and must be administered with food for optimal absorption. It is a potent protease inhibitor with a unique drug-resistance profile that offers advantages in the management of cases of multidrug-resistant HIV infection. Tipranavir (in combination with ritonavir) is both an inhibitor and inducer of cytochrome p450, with significant potential for drug-drug interactions, and therefore, it must be used cautiously when administered to patients who are receiving other drugs. Evolution of drug resistance after treatment failure with tipranavir is complex and is not yet fully understood. There is limited overlap in the resistance mutations that predict response to tipranavir and another new protease inhibitor, darunavir, which is active against drug-resistant isolates. Tipranavir is associated with elevations in alanine aminotransferase and aspartate aminotransferase levels, as well as elevated cholesterol and triglyceride levels, and can cause the typical gastrointestinal adverse effects associated with all protease inhibitors.
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U2 - 10.1086/520847
DO - 10.1086/520847
M3 - Review article
C2 - 17712762
AN - SCOPUS:34548534109
SN - 1058-4838
VL - 45
SP - 761
EP - 769
JO - Clinical Infectious Diseases
JF - Clinical Infectious Diseases
IS - 6
ER -