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Fatty acid amide hydrolase (FAAH)

Mouse and in vitro studies identified a-ketooxazole-based covalent inhibitors of FAAH that could be useful for treating pain. In vitro, the lead inhibitor caused irreversible inhibition of FAAH by covalently binding to serine 241 and cysteine 269 in the enzyme's active site. In a mouse model for neuropathic pain, the lead inhibitor lowered allodynia with a longer duration of effect than a reversible FAAH inhibitor. Next steps include evaluating the compounds in additional animal models for pain.
Vernalis plc's V158866, a small molecule FAAH inhibitor, is in Phase II trials to treat pain.

SciBX 6(17); doi:10.1038/scibx.2013.419
Published online May 2, 2013

Unpatented; compounds available for licensing

Otrubova, K. et al. J. Am. Chem. Soc.;
published online April 12, 2013;
Contact: Dale L. Boger, The Scripps Research Institute, La Jolla, Calif.