Dosing Based on Receptor Occupancy

The use of PET for the evaluation of degree and duration of receptor occupancy in relation to dose has become standard for new antipsychotic and antidepressive drugs. Important information derived from such studies include the following:

(i) drug interaction with the assumed biochemical target and hence information that the drug reaches the target tissue, for example, passes through the blood-brain barrier,

(ii) degree of receptor occupancy reached for a given dose, i.e., the dose-occupancy relations,

(iii) duration of action on the target system and its relation to conventional plasma kinetics,

(iv) variability in a patient population with respect to receptor occupancy, and

(v) degree of receptor occupancy affected by other drugs.

Some of the above factors are essential for a decision on dose and dose interval in a clinical trial [37].

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