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Radiosynthesis of 1-2-[18F]Fluoroethyl-L-Tryptophan using a One-pot, Two-step Protocol
Published on: September 21, 2021
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PET Tracers To Study Clinically Relevant Hepatic Transporters
Andrea Testa1, Matteo Zanda1, Charles S Elmore
1†Kosterlitz Centre for Therapeutics, School of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen AB25 2ZD, U.K.
Molecular Pharmaceutics
|June 3, 2015
Summary
Positron emission tomography (PET) imaging visualizes hepatic transporter activity, crucial for drug clearance and preventing toxicity. This review highlights PET
Area of Science:
- Pharmacology
- Biochemistry
- Medical Imaging
Background:
- Hepatic transporter proteins regulate drug and metabolite clearance from the bloodstream into bile.
- Reduced transporter activity can lead to increased exposure to toxic compounds and adverse drug effects.
- Inhibition of hepatic transporters by drugs is a significant factor in drug-drug interactions (DDIs).
Purpose of the Study:
- To review the clinical relevance of hepatic transporters.
- To explore the application of positron emission tomography (PET) imaging in assessing transporter activity.
- To discuss the development and application of radiotracers for hepatic transporter studies.
Main Methods:
- Review of existing literature on hepatic transporters and PET imaging.
- Analysis of pharmacokinetic parameters determined by PET imaging.
- Evaluation of the design, accessibility, and applications of current radiotracers.
Main Results:
- PET imaging with radiolabeled substrates can demonstrate inhibition of hepatic transporters.
- PET allows for the determination of pharmacokinetic parameters related to transporter activity.
- Various radiotracers have been developed for preclinical and clinical applications.
Conclusions:
- PET imaging is a valuable tool for studying hepatic transporter function and drug interactions.
- Further development of novel PET probes is needed for comprehensive analysis.
- Understanding transporter activity through PET can improve drug safety and efficacy.
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