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

Abstract

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 ¹⁸F-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 ¹⁸F-labelled molecules take their place alongside clinically established oncology biomarkers such as ¹⁸FDG and ¹⁸FLT.

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: ¹⁸F PET is a flourishing field with many applications in drug discovery and development, through radiolabelling of drug molecules or use of fluorinated disease biomarkers.

Keywords::

• ¹⁸F
• biomarkers
• in vivo imaging
• positron emission tomography

Notes

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