Contribution of SPECT Measurements of D₂and 5-HT_2AOccupancy to the Clinical Development of the Antipsychotic SB-773812

Abstract

In all subjects, SB-773812 showed penetration into the brain, reaching its target receptors. In patients with schizophrenia, D(2) occupancy levels induced by a single dose were maintained over time, indicating that once-daily dosing regimens are appropriate. Pharmacokinetics-receptor occupancy analysis provided guidance for the selection of a clinically effective dose, supporting progression in phase II.