Brain PET measurement of PDE10A occupancy by TAK‐063, a new PDE10A inhibitor, using [11C]T‐773 in nonhuman primates

In conclusion, this nonhuman primate PET study demonstrated that [11C]T‐773 is useful to estimate the PDE10A occupancy by TAK‐063 in the striatum although there is in vivo interaction of the uptake between [11C]T‐773 and TAK‐063 in the cerebellum. These results warrant further clinical occupancy study for TAK‐063. This article is protected by copyright. All rights reserved.

The target occupancy of a new PDE10A inhibitor, TAK‐063, was evaluated using [11C]T‐773. The authors show that the target occupancy was appropriately estimated even there was interaction between [11C]T‐773 and TAK‐063 in brain regions without PDE10A binding. The results would help further clinical applications of both TAK‐063 and [11C]T‐773.

Source: Synapse - February 16, 2016 Category: Neurology Authors: Akihiro Takano, Vladimir Stepanov, Ryuji Nakao, Nahid Amini, Balázs Gulyás, Haruhide Kimura, Christer Halldin Tags: Research Article Source Type: research