Measuring receptor occupancy with PET

Authors
Citation
A. Van Waarde, Measuring receptor occupancy with PET, CUR PHARM D, 6(16), 2000, pp. 1593-1610
Citations number
135
Categorie Soggetti
Pharmacology & Toxicology
Journal title
CURRENT PHARMACEUTICAL DESIGN
ISSN journal
13816128 → ACNP
Volume
6
Issue
16
Year of publication
2000
Pages
1593 - 1610
Database
ISI
SICI code
1381-6128(200011)6:16<1593:MROWP>2.0.ZU;2-1
Abstract
Many physiological and biochemical measurements can be performed noninvasiv ely in humans with modern imaging techniques like magnetic resonance imagin g (MRI), positron emission tomography (PET) or single-photon emission compu ted tomography (SPECT). This review focuses on the monitoring of drug-recep tor interactions in patients and healthy volunteers with PET. Such studies depend on the availability of a suitable radioligand; they are already poss ible for classical and atypical neuroleptics, anxiolytics, antidepressants, anticholinergics, antihistamines, antiepileptics, beta-blockers and hypnot ic drugs. In Phase I-II human studies, measurements of plasma pharmacokinet ics can be combined with images of receptor occupancy and be quantitatively related to pharmacologic effects which are induced in the same subjects. O ptimal dosing schedules can be defined and valuable information for the des ign of Phase III studies can be acquired. Moreover, the effect of intervent ions (e.g. change of dose, additional medication) can be predicted. Medical imaging techniques will play an increasing role in clinical pharmacology a nd allow well-informed go/no-go decisions in future drug development.