Radiochemistry: A Useful Tool in the Ophthalmic Drug Discovery

Abstract

Positron Emission Tomography (PET) and Single Photon Emission Computerized Tomography (SPECT) are ultra-sensitive, fully translational and minimally invasive nuclear imaging techniques capable of tracing the spatiotemporal distribution of positron (PET) or gamma (SPECT) emitter-labeled molecules after administration into a living organism. Besides their impact in the clinical diagnostic, PET and SPECT are playing an increasing role in the process of drug development, both during the evaluation of the pharmacokinetic properties of new chemical entities as well as in the proof of concept, proof of mechanism and proof of efficacy studies. However, they have been scarcely applied in the context of ophthalmic drugs. In this paper, the basics of nuclear imaging and radiochemistry are briefly discussed, and the few examples of the use of these imaging modalities in ophthalmic drug development reported in the literature are presented and discussed. Finally, in a purely theoretical exercise, some labeling strategies that could be applied to the preparation of selected ophthalmic drugs are proposed and potential applications of nuclear imaging in ophthalmology are projected.

Keywords: Positron Emission Tomography (PET); Single Photon Emission Computerized Tomography (SPECT); drug development; nuclear imaging; ophthalmology; radiochemistry..