The role of imaging in proof of concept for CNS drug discovery and development

Dean F. Wong, Johannes Tauscher, Gerhard Gründer

Research output: Contribution to journalReview articlepeer-review

145 Scopus citations


Neuroimaging, particularly that of neuroreceptor radioisotope and functional magnetic resonance imaging (fMRI), has played a fundamental role in neuropharmacology and neurophysiology. Because of the unique and pioneering role, especially of the radiolabeling of central nervous system (CNS) drugs for receptor and neurotransmitter system imaging, there is an increasingly major role to aid in CNS drug development. One component is providing evidence for proof of concept of the target for which candidate drugs are being tested for receptor occupancy mechanism of action and ultimately rational drug dosing. There is also a role for other areas of neuroimaging, including fMRI and magnetic resonance spectroscopy in other magnetic resonance-based techniques that, together with radioisotope imaging, represent 'CNS molecular imaging.' The role of these approaches and a review of the recent advances in such neuroimaging for proof-of-concept studies is the subject for this paper. Moreover, hypothetical examples and possible algorithms for early discovery/phase I development using neuroimaging provide specific working approaches. In summary, this article reviews the vital biomarker approach of neuroimaging in proof of concept studies.

Original languageEnglish
Pages (from-to)187-203
Number of pages17
Issue number1
StatePublished - Jan 2009


  • Dose finding
  • Magnetic resorance imaging
  • Occupancy
  • Positron emission tomography
  • Proof of mechanism
  • Proof-of-concept


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