Drug intelligence / Profile preview

darunavir + etravirine + ritonavir + emtricitabine + tenofovir disoproxil fumarate

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination antiretroviral regimen used in the treatment of human immunodeficiency virus (HIV) infection. Each component has a distinct mechanism of action targeting different stages of the HIV life cycle: - Darunavir is a protease inhibitor that prevents viral replication by inhibiting the HIV-1 protease enzyme. - Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to and inhibits reverse transcriptase, an enzyme crucial for viral RNA conversion to DNA. - Ritonavir acts primarily as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A4, thereby increasing plasma concentrations of other protease inhibitors like darunavir. - Emtricitabine and tenofovir disoproxil fumarate are nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase activity, preventing viral DNA synthesis. This combination is typically reserved for patients with drug-resistant HIV or those requiring complex regimens due to prior treatment failure. The regimen works synergistically to reduce HIV viral load and delay progression to acquired immunodeficiency syndrome (AIDS). It does not cure HIV but helps manage the infection and improve immune function[7][1][2].

02

Targets

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

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