Big physics, small doses: the use of AMS and PET in human microdosing of development drugs

Early clinical drug development has seen little change in 20 years despite a 40% failure rate due to poor drug metabolism and pharmacokinetics. A new method called microdosing allows investigational drugs to be tested in humans earlier, enabling smarter candidate selection. Microdosing relies on two ultrasensitive techniques: positron emission tomography (PET) for pharmacodynamic information and accelerator mass spectrometry (AMS) for pharmacokinetic information. This approach permits safer human studies and reduces the use of animals in preclinical toxicology.

Study at a glance

Abstract

The process of early clinical drug development has changed little over the past 20 years despite an up to 40% failure rate associated with inappropriate drug metabolism and pharmacokinetics of candidate molecules. A new method of obtaining human metabolism data known as microdosing has been developed which will permit smarter candidate selection by taking investigational drugs into humans earlier. Microdosing depends on the availability of two ultrasensitive 'big-physics' techniques: positron emission tomography (PET) can provide pharmacodynamic information, whereas accelerator mass spectrometry (AMS) provides pharmacokinetic information. Microdosing allows safer human studies as well as reducing the use of animals in preclinical toxicology.