Phosphodiesterase 10A inhibitors: analysis of US/EP patents granted since 2012.

Research paper by José-Manuel JM Bartolomé-Nebreda, Susana S Conde-Ceide, María M García

Indexed on: 02 Jun '15Published on: 02 Jun '15Published in: Pharmaceutical patent analyst


Phosphodiesterases are enzymes that metabolically inactivate the intracellular second messengers 3',5'-cyclic adenosine and guanosine monophosphate contributing to the control of multiple biological processes. Among them, PDE10A has the most restricted distribution with high expression in striatal medium spiny neurons. Dysfunction of this key brain circuit has been associated with different psychiatric and neurodegenerative disorders. The unique role of PDE10A, together with its increased pharmacological characterization, have prompted enormous interest in investigating the potential of inhibitors of this enzyme as potential novel therapeutic agents This article reviews PDE10A related patents issued in the period 2012-2014 in the USA and Europe offering also a perspective on potential avenues for the future clinical development of phosphodiesterase 10A inhibitors.