Maraviroc (Celsentri)

Maraviroc (known by the trade name Celsentri in Europe and Selzentry in the United States) is the first drug to be licensed from a new class of antiretrovirals called CCR5 inhibitors. Maraviroc prevents HIV from entering uninfected cells by blocking the predominant route of entry on the surface of some immune cells, the CCR5 receptor .

A majority of virus, particularly early on in infection, is macrophage-tropic (referred to as M-tropic or R5-tropic virus) and can only enter the CD4 cell by using the CCR5 receptor.  Between 50 and 60% of treatment-experienced patients have CCR5-tropic virus. The HIV population begins to switch to make use of both the CCR5 and CXCR4 receptors as the CD4 cell count falls. Faster CD4 cell decline is associated with the emergence of a predominantly CXCR4-tropic virus population. 

If the CCR5 receptor is unavailable, M-tropic HIV is unable to infect the cell. Maraviroc interferes with the interaction between the CD4 cell chemokine receptor CCR5 and HIV-1 gp120.

In 2007, the drug was approved for use in combination with other antiretrovirals, by treatment-experienced individuals with a confirmed CCR5-tropic virus in the US and marketing approval in Europe followed soon after. Maraviroc received licensing for use in antiretroviral-naive patients in the US in November 2009.1 2

References

  1. Gulick RM et al. Maraviroc for previously treated patients with R5 HIV-1 infection. N Engl J Med 359(14): 1429-1449, 2008
  2. Vandekerckhove L et al. Maraviroc: perspectives for use in antiretroviral-naive HIV-1-infected patients. J Antimicrob Chemother 63(6):1087-1096, 2009