Small Molecule PET Tracers in Drug Discovery

18F-Fluorination: Challenge and Opportunity for Organic Chemists

“…The discovery of a drug begins with the validation of a target, synthesis, and testing of a series of molecules that bind efficiently to the target and, subsequently, optimization of chemical structures that interact with the target to improve the potential as a drug before commencing the actual clinical trials in human ( Figure 2 ). 10 Thousands of drug candidates are eliminated during this process before the optimal candidate is chosen to move forward into the clinic. Because the costs of clinical drug development increase from phase 1 to 3 so dramatically, early informed decisions in the process become crucial or at least can save hundreds of millions of dollars if molecules that would ultimately fail could be eliminated at the early stages of the development.…”

Copper‐mediated nucleophilic radiofluorination of [18F]β‐CFT for positron emission tomography imaging of dopamine transporter

“…[10][11][12] Due to the favorable properties of 18 F as a positron emitter and the prevalence of fluorine in drug design, [13][14][15] PET also has become a powerful and useful tool to facilitate drug discovery and development. [16][17][18] These utilizations and applications have created a large demand for new radiochemistry focusing on 18 F-radiofluorination. [19][20][21] In the past two decades, the number of methods for incorporating fluorine into aromatic hydrocarbons has continuously increased as these motifs are commonly found in pharmaceuticals to impact drug potency.…”

Kinfitr — an open-source tool for reproducible PET modelling: validation and evaluation of test-retest reliability

“…Positron emission tomography (PET) is an imaging modality with high sensitivity and specificity for biochemical markers and metabolic processes in vivo [ 1 ]. It is an important tool in the study of psychiatric and neurological diseases, as well as for evaluating novel and established pharmacological treatments [ 2 – 4 ].…”