Kinetic models for estimating occupancy from single-scan PET displacement studies.

The traditional design of PET target engagement studies is based on a baseline scan and one or more scans after drug administration. We here evaluate an alternative design in which the drug is administered during an on-going scan (i.e.

Designing drug occupancy studies with PET neuroimaging: Sample size, occupancy ranges and analytical methods.

Molecular neuroimaging is today considered essential for evaluation of novel CNS drugs; it is used to quantify blood-brain barrier permeability, verify interaction with key target and determine the drug dose resulting in 50% occupancy, IC. In spite of this, there has been limited data available to inform on how to optimize study designs. Through simulations, we here evaluate how IC estimation is affected by the (i) range of drug doses administered, (ii) number of subjects included, and (iii) level of noise in the plasma drug concentration measurements.