Drug intelligence / Profile preview

raltegravir + etravirine + darunavir + ritonavir

Development stage
Phase 4
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Raltegravir + etravirine + darunavir + ritonavir is a combination antiretroviral therapy (ART) regimen used as a salvage therapy for heavily treatment-experienced patients with multidrug-resistant HIV-1 infection. This regimen is not a single fixed-dose product but a combination of four separate small molecule drugs: raltegravir (an integrase strand transfer inhibitor), etravirine (a non-nucleoside reverse transcriptase inhibitor), and darunavir (a protease inhibitor) boosted by ritonavir (a pharmacokinetic enhancer). By targeting three distinct stages of the HIV replication cycle—integration, reverse transcription, and proteolytic processing—the regimen provides a high genetic barrier to resistance. It was notably evaluated in the ANRS 139 TRIO trial, which demonstrated significant viral suppression in patients who had failed multiple prior lines of therapy.

Other names
TRIO regimenANRS 139 TRIO regimenANRS139 TRIO regimenANRS-139 TRIO regimen
02

Targets

CYP3A4 (Cytochrome P450 3A4)Integrase allosteric pocket (HIV)PR (Progesterone receptor)Human immunodeficiency virus type 1 reverse transcriptase

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