Raltegravir is a potent inhibitor of XMRV

January 01, 0001

Raltegravir is a potent inhibitor of XMRV

Xenotropic murine leukemia-related retrovirus (XMRV) is a recently discovered retrovirus that has been linked to human prostate cancer and chronic fatigue syndrome (CFS). Both diseases affect a large fraction of the world population, with prostate cancer affecting one in six men, and CFS affecting an estimated 0.4 to 1% of the population. Forty-five compounds, including twenty-eight drugs approved for use in humans, were evaluated against XMRV replication in vitro. The researchers from the US found that the retroviral integrase inhibitor, raltegravir, was potent and selective against XMRV at submicromolar concentrations, in MCF-7 and LNCaP cells, a breast cancer and prostate cancer cell line, respectively.

Another integrase inhibitor, L-000870812, and two nucleoside reverse transcriptase inhibitors, zidovudine (ZDV), and tenofovir disoproxil fumarate (TDF) also inhibited XMRV replication. When combined, these drugs displayed mostly synergistic effects against this virus, suggesting that combination therapy may delay or prevent the selection of resistant viruses.

The researchers concluded: "If XMRV proves to be a causal factor in prostate cancer or CFS, these discoveries may allow for rational design of clinical trials."

A virus to watch and an area of research to watch.

For the full abstract, click here.

PLoS ONE 5(4):e9948, 1 April 2010
© 2010 Singh et al
Raltegravir Is a Potent Inhibitor of XMRV, a Virus Implicated in Prostate Cancer and Chronic Fatigue Syndrome. Singh IR, Gorzynski JE, Drobysheva D, Bassit L and Schinazi RF. Correspondence to IR Singh: [email protected]

Category: A. General/Unspecified. Keywords: raltegravir, inhibitor, XMRV, prostate cancer, chronic fatigue syndrome, in vitro study, journal watch.
Synopsis edited by Dr Stephen Wilkinson, Melbourne, Australia. Posted on Global Family Doctor 14 May 2010

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