Drug intelligence / Profile preview

tipranavir + ritonavir + amprenavir

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **triple combination of the HIV-1 protease inhibitors tipranavir, ritonavir, and amprenavir**. - **Tipranavir** is a non-peptidic protease inhibitor designed for antiretroviral therapy, most frequently administered with low-dose ritonavir to boost its bioavailability and efficacy[1][2][3][4][5][7]. Tipranavir inhibits the proteolytic cleavage of the HIV-1 Gag and Gag-Pol polyproteins, preventing maturation of infectious virus particles[1][3]. Ritonavir is used at low dose to boost plasma concentrations of protease inhibitors such as tipranavir, acting as a **CYP3A4 inhibitor**. Amprenavir is also a protease inhibitor, with a mechanism similar to tipranavir, preventing cleavage of the gag-pol polyprotein and resulting in immature, noninfectious viral particles[6]. - This combination is not a standard or approved regimen. While tipranavir/ritonavir is widely used, the addition of amprenavir is not standard, and combination of these three drugs may have complex pharmacokinetic and toxicity profiles, and is not recommended in guidelines[7]. - Tipranavir is developed by **Boehringer Ingelheim**[2]. - **Primary indication**: treatment of HIV-1 infection in individuals with extensive prior antiretroviral treatment and virus resistant to multiple protease inhibitors[1][3][5].

02

Targets

CYP2C19 (Cytochrome P450 2C19)CYP1A2 (Cytochrome P450 1A2)ABCB1 (P-glycoprotein)UGT (UDP-glucuronosyltransferase family)CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)PR (Progesterone receptor)

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