TAK-063 (Balipodect)

Description: Balipodect (formerly also known as TAK-063) is a novel, highly potent, orally bioavailable and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 0.30 nM. TAK-063 has also excellent selectivity (> 15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of TAK-063 to mice elevated striatal 3', 5'-cyclic adenosine monophosphate (cAMP) and 3', 5'-cyclic guanosine monophosphate (cGMP) levels at 0.3 mg/kg and showed potent suppression of phencyclidine (PCP)-induced hyperlocomotion at a minimum effective dose (MED) of 0.3 mg/kg.

References: J Med Chem. 2014 Nov 26; 57(22):9627-43.