Drug intelligence / Profile preview

maraviroc + raltegravir + dolutegravir

Development stage
Unknown
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three antiretroviral drugs used in the treatment of HIV infection. Each drug targets a different stage in the HIV life cycle: - **Maraviroc** is a CCR5 antagonist that blocks the CCR5 co-receptor on host cells, preventing entry of CCR5-tropic HIV into CD4+ T cells[6][2]. - **Raltegravir** is an integrase strand transfer inhibitor (INSTI) that inhibits the catalytic activity of HIV integrase, thereby blocking integration of viral DNA into the host genome[6]. - **Dolutegravir** is also an integrase strand transfer inhibitor (INSTI), binding to and inhibiting HIV integrase at a different site than raltegravir, thus preventing viral DNA integration as well[8]. These agents are typically used in combination with other antiretrovirals but may be considered together for salvage therapy or complex resistance patterns. All three are small molecule drugs and are not available as a fixed-dose single-tablet regimen; they must be taken as separate pills.

02

Targets

CCR5 (C-C chemokine receptor type 5)Integrase allosteric pocket (HIV)SLC47A1 (Multidrug and toxin extrusion transporter 1)OCT2 (Organic cation transporter 2)

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