Entry Inhibitors


Enfuvirtide An HIV-1 gp41 fusion inhibitor used in patients experiencing HIV-1 replication who are already being treated with other anti-retrovirals.
Maraviroc A CCR5 co-receptor antagonist used with other antiretroviral medications to treat CCR5-tropic HIV-1 infection.
Ibalizumab A CD4-specific antibody used to treat HIV infections.
Source: https://go.drugbank.com/categories/DBCAT000220

HIV entry into a CD4+ cell is a multi-step process. Entry begins when the HIV envelope glycoprotein gp-120 attaches to a CD4 receptor. The HIV glycoprotein gp-120 undergoes a confirmational change when it contacts the CD4 receptor allowing it to be secured to a coreceptor, CCR5 or CXCR4.

Maraviroc is the first of a new class of medications targeting the CCR5 co-receptor on a CD4+ cell. Maraviroc binds to the CCR5 co-receptor stopping CCR5 tropic HIV-1 from securely attaching to the CD4+ cell.

Co-receptor binding is believed to be essential for HIV-1 replication. Antiretroviral therapy that includes maraviroc is indicated only for treatment experienced adult patients who have evidence of viral replication of CCR5-tropic HIV-1. An HIV-1 tropism test such as a trofile assay must be done to verify that maraviroc will be effective.


Reference

CCR5 Antagonist: NIH. CCR5 Antagonist | NIH. (n.d.). https://clinicalinfo.hiv.gov/en/glossary/ccr5-antagonist.

HIV Fusion Inhibitors: Drug Bank. (n.d.). https://go.drugbank.com/categories/DBCAT000220

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