Late Stage Fluorination and its Applications to Drug Discovery



Taylor NJ et al 2017                                      Gao Z et al 2013                    Tresadern G 2017


All of modern medicine is dependent on advances in chemistry and the healthcare goalposts have moved as the century has progressed. We all face problems with the spreading of infectious diseases on an unprecedented scale. Poorer nations struggle to access and distribute modern drugs, and drug resistance is growing in all countries. In addition, the increasing prevalence of non-infectious diseases in an ageing population brings unforeseen and expensive challenges to healthcare.

The pressing need to shorten cycle times and reduce the costs of drug discovery has led pharma and the clinicians that
guide them to use positron emission tomography (PET) and magnetic resonance imaging (MRI) scanning techniques, enabling them to increase disease understanding, study target engagement with therapeutics and improve decision making, so that only the best candidate molecules progress to the later stages of drug development. Overcoming these challenges requires multidisciplinary knowledge, and can be facilitated through stronger links between academia and Pharma.

Fluorine chemistry plays a central role in drug discovery. Chemical entities substituted with fluorine or fluorine-containing groups are frequently used to design drugs with improved pharmacological and pharmacokinetic profiles that provide important benefits over existing therapies, such as superior safety, efficacy, dosing, and patient compliance. Over 20% of pharmaceuticals prescribed or administered in the clinic contain at least one fluorine atom, including about one third of the 30 leading blockbuster drugs by sales.

FLUDD ESRs will be centered in the Department of Chemistry of the University of Oxford (UOXF), and integrated into a highly productive chemistry training and research environment. The UOXF training component of all ESRs projects will take place in the Chemistry Research Laboratory (CRL), a worldclass facility that possesses state-of-the-art equipment, services and laboratory space. The ambitious scientific objectives are clear and within reach through dynamic interactions between FLUDD partners. FLUDD brings together leading experts in a range of disciplines from across Europe to work collaboratively on challenges beyond the scope of individual partners.