The role and future potential of fluorinated biomarkers in positron emission tomography

Importance of the field: Positron emission tomography (PET) is rapidly emerging as the functional imaging method of choice for in vivo imaging applications in a number of key areas of drug discovery and clinical pathology, but especially in oncology. One key limitation of PET is the requirement for rapid synthesis and purification of biomarker/drug molecules regiospecifically labelled with short-lived positron-emitting isotopes. Areas covered in this review: In this review, we focus on the role of F-18-labelled molecules in PET, presenting a perspective on the challenges associated with the synthesis and future clinical utility of a range of labelled small molecules and macromolecular structures. Further preclinical method development for the regiospecific synthesis of fluorinated biomarkers under mild conditions is required before a wide range of F-18-labelled molecules take their place alongside clinically established oncology biomarkers such as (18)FDG and (FLT)-F-18. What the reader will gain: In this review, we offer insights into current and future chemical methods for the efficient synthesis of fluorinated PET biomarkers, featuring modern technologies such as microwave-promoted chemistries and microfluidic reactors, both of which possess the capability to routinely and rapidly produce the small quantities of PET-labelled molecules under the mild and efficient conditions that are required for PET tracer synthesis. Take home message: F-18 PET is a flourishing field with many applications in drug discovery and development, through radiolabelling of drug molecules or use of fluorinated disease biomarkers.