Drug intelligence / Profile preview

etravirine + darunavir + ritonavir

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination antiretroviral regimen used in the treatment of HIV-1 infection. It consists of three agents: - **Etravirine (TMC125)** is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that inhibits HIV-1 reverse transcriptase by binding to an allosteric site on the enzyme and blocking RNA-dependent and DNA-dependent DNA polymerase activities. - **Darunavir** is a protease inhibitor that prevents HIV replication by binding to the active site of the HIV-1 protease enzyme and inhibiting cleavage of viral Gag-Pol polyproteins. This action halts viral maturation and leads to production of immature, non-infectious virus particles[3]. - **Ritonavir** acts primarily as a pharmacokinetic enhancer ("booster") for other protease inhibitors like darunavir by inhibiting cytochrome P450 3A4-mediated metabolism. Ritonavir itself also inhibits HIV protease but at lower doses its main role is boosting plasma concentrations of co-administered drugs[6]. This combination is indicated for use in adults and pediatric patients with HIV-1 infection who are treatment-experienced or have resistance to other regimens. Etravirine (TMC125) was developed by Tibotec (now part of Johnson & Johnson), while darunavir was also developed by Tibotec/Johnson & Johnson; ritonavir was developed by AbbVie.

Brand names
Intelence
Other names
etravirine + darunavir + ritonavirTMC125 + darunavir + ritonavir
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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