Drug intelligence / Profile preview

raltegravir + maraviroc + darunavir + ritonavir + tenofovir + emtricitabine

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

This is a six-drug antiretroviral combination regimen used in the treatment of HIV infection, particularly in patients with multidrug-resistant virus or those requiring salvage therapy. The regimen includes: *Raltegravir*: an integrase strand transfer inhibitor that blocks the integration of viral DNA into the host genome. *Maraviroc*: a CCR5 antagonist that prevents HIV from entering CD4+ cells by blocking the CCR5 co-receptor. *Darunavir*: a protease inhibitor, administered with *ritonavir* as a pharmacokinetic booster to increase its plasma levels; it inhibits HIV protease, preventing viral maturation. *Tenofovir disoproxil fumarate* and *emtricitabine*: both are nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) that inhibit reverse transcription of viral RNA into DNA. This combination targets multiple steps in the HIV replication cycle and is typically reserved for complex cases due to pill burden and potential drug-drug interactions[1][3][5][6][8].

Other names
Truvada (tenofovir + emtricitabine)
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCCR5 (C-C chemokine receptor type 5)CYP3A7 (Cytochrome P450 3A7)Integrase allosteric pocket (HIV)PR (Progesterone receptor)

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