Drug intelligence / Profile preview

tipranavir + ritonavir + lopinavir

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

Overview

Tipranavir + ritonavir + lopinavir is a non-standard, three-drug combination consisting of three HIV protease inhibitors. Tipranavir and lopinavir are both direct inhibitors of the HIV-1 protease enzyme, which is necessary for viral replication. Ritonavir acts both as a weak direct protease inhibitor and, more importantly, as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A4 (CYP3A4)-mediated metabolism, substantially increasing plasma levels of the other protease inhibitors. The combination would have a markedly complex drug interaction profile, a high risk of hepatotoxicity, and significant potential for overlapping toxicities and reduced efficacy due to drug-drug interactions. While tipranavir + ritonavir and lopinavir + ritonavir are well-studied and sometimes used sequentially, co-administration of all three in a single regimen is not standard and may be associated with reduced or unpredictable plasma concentrations[6]. It is not marketed under a unique brand name and not approved as a fixed combination. Used components individually are indicated for the treatment of HIV-1 infection in combination with other antiretroviral agents.

02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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