This week in therapeutics




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Infectious disease

Influenza virus

Protease-activated receptor 1 (PAR1)

Mouse studies suggest inhibiting PAR1 could help treat influenza virus infection. In mouse models of influenza A virus infection, genetic deletion or pharmacological inhibition of Par1 attenuated inflammation and virus replication in the lung and protected against weight loss and death. The PAR1 inhibitor vorapaxar protected the mice from low pathogenic H1N1 and H3N2 infection as well as high pathogenic H5N1 or pandemic H1N1 infection. Next steps could include testing clinical-stage PAR1 inhibitors.
In 2011, Merck & Co. Inc. discontinued dosing of patients in two Phase III trials of vorapaxar to prevent cardiovascular events because intracranial hemorrhage occurred in a subset of patients. In 2012, the pharma announced plans to file regulatory applications for the compound in the same indication but in a restricted patient population.

SciBX 5(49); doi:10.1038/scibx.2012.1285
Published online Dec. 20, 2012

Patented by the French National Institute for Agricultural Research (INRA); available for licensing

Khoufache, K. et al. J. Clin. Invest.; published online Dec. 3, 2012;
Contact: Béatrice Riteau, University of Lyon and the French National Institute for Agricultural Research (INRA), Lyon, France