This week in therapeutics




Licensing status

Publication and contact information



Orexin 1 receptor (HCRTR1; OX1R); HCRTR2 (OX2R)

Rat and nonhuman primate studies suggest antagonizing orexin receptors could help treat insomnia with fewer cognitive side effects than marketed drugs that modulate GABA receptors. In rats and nonhuman primates, an orexin receptor antagonist induced sleep at concentrations that did not significantly decrease cognition in object recognition tests, whereas a series of compounds that modulate GABA receptors did decrease cognition. Next steps include clinical studies to evaluate the effect of orexin antagonists on cognition.
An NDA for Merck & Co. Inc.'s suvorexant, a dual orexin receptor antagonist, will be discussed by an FDA advisory committee on May 22, 2013.

At least seven companies market GABA receptor modulators to treat insomnia.

SciBX 6(14); doi:10.1038/scibx.2013.342
Published online April 11, 2013  

Patents pending; licensing status unavailable

Uslaner, J.M. et al. Sci. Transl. Med.; published online April 3, 2013;
Contact: Jason M. Uslaner, Merck & Co. Inc., West Point, Pa.