Drug intelligence / Profile preview

raltegravir + darunavir + ritonavir

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

Overview

This is an investigational nucleoside reverse transcriptase inhibitor (NRTI)-sparing antiretroviral regimen consisting of the integrase strand transfer inhibitor raltegravir and the protease inhibitor darunavir, boosted with ritonavir. It was evaluated by the National Center for Global Health and Medicine in Japan in the SPARE (Switching to Darunavir/r and Raltegravir for Renal Function in HIV) trial. The regimen was designed to assess whether switching from a tenofovir-based regimen to this combination could improve renal function (specifically eGFR and urinary biomarkers) while maintaining virological suppression in HIV-infected patients. Raltegravir blocks the HIV integrase enzyme, preventing viral DNA integration into the host genome, while darunavir inhibits the HIV protease enzyme to prevent viral maturation. Ritonavir is included as a pharmacokinetic booster to increase darunavir plasma concentrations by inhibiting the CYP3A4 enzyme.

Other names
DRV/r + RALdarunavir/ritonavir + raltegravirNRTI-sparing regimen
02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP3A5 (Cytochrome P450 family 3 subfamily A member 5)Integrase allosteric pocket (HIV)PR (Progesterone receptor)

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