Title:Radiochemistry: A Useful Tool in the Ophthalmic Drug Discovery
Volume: 27
Issue: 4
关键词:
正电子发射断层扫描（PET），单光子发射计算机断层扫描（SPECT），放射化学，核成像，眼科，药物开发。
摘要: 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.
