Drug intelligence / Profile preview

etravirine + lopinavir + ritonavir

Development stage
Phase 1
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

Etravirine + lopinavir + ritonavir is a combination of three antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV) infection. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that blocks HIV-1 reverse transcriptase, thereby inhibiting viral replication. Lopinavir and ritonavir are protease inhibitors; lopinavir inhibits the HIV-1 protease enzyme, preventing maturation of infectious virus particles, while ritonavir acts primarily as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A-mediated metabolism of lopinavir, increasing its plasma concentration. This combination is typically used in patients with prior antiretroviral therapy experience or resistance to other regimens. The coadministration has been shown to be generally well tolerated but can result in reduced exposure to etravirine due to metabolic induction by lopinavir/ritonavir[4][6][8].

Brand names
Kaletra + Intelence
Other names
lopinavir/ritonavir + etravirineLPV/r + ETR
02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)Human immunodeficiency virus type 1 reverse transcriptaseCYP3A (CYP3A family)

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