PET for in vivo pharmacokinetic and pharmacodynamic measurements

Positron emission tomography (PET) scanning is evolving as a unique tool for drug development in oncology for improving both the efficacy of established treatment and in evaluating novel anticancer agents. As a non-invasive functional imaging modality, PET has an unrivalled sensitivity when monitoring the pharmacokinetics and pharmacodynamics of drugs and biochemicals when radiolabelled with short living positron-emitting radioisotopes. This is of particular relevance in assessing newer molecular-targeted therapy where conventional evaluation criteria (maximum tolerated dose and tumour shrinkage for example) may be inappropriate. PET has already been applied to a wide number of drugs to demonstrate activity in vivo from standard chemotherapy such as 5-fluorouracil (5-FU) [J Clin Oncol 17 (1999) 1580], to novel molecular agents such as those involved in tumour angiogenesis [Br J Cancer 83 (2000) P6] and antivascular therapy [Proc Annu Meet Am Soc Clin Oncol 19 (2000) 179a]. This review will evaluate the achievements of PET in the drug development process, an approach that promises to facilitate the rapid translation of scientific research into current clinical practice. (C) 2002 Elsevier Science Ltd. All rights reserved.