Drug intelligence / Profile preview

tenofovir + lamivudine + darunavir + ritonavir + raltegravir

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

Overview

This is a combination antiretroviral regimen consisting of five agents used in the treatment of HIV infection. The components are: - **Tenofovir**: A nucleotide reverse transcriptase inhibitor (NRTI) that inhibits HIV reverse transcriptase, blocking viral DNA synthesis. - **Lamivudine**: Another NRTI that also inhibits HIV reverse transcriptase, preventing viral replication. - **Darunavir**: A protease inhibitor that blocks the activity of the HIV protease enzyme, leading to production of immature, noninfectious virus particles. - **Ritonavir**: Primarily used as a pharmacokinetic booster for other protease inhibitors like darunavir by inhibiting cytochrome P450 3A4 enzymes, increasing plasma concentrations and effectiveness of co-administered drugs. - **Raltegravir**: An integrase strand transfer inhibitor (INSTI) that prevents integration of viral DNA into the host genome. This combination targets multiple steps in the HIV life cycle and is typically reserved for patients with resistance or intolerance to standard regimens. Each component is FDA-approved for use in antiretroviral therapy; however, this specific five-drug combination does not have a fixed-dose co-formulation and must be prescribed as individual agents[3][4][5].

Brand names
Viread (tenofovir)Epivir (lamivudine)Prezista (darunavir)Norvir (ritonavir)Isentress (raltegravir)
02

Targets

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

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