PK/PD modeling of targeted protein degraders: Charting new waters and navigating the shallows

Abstract

The development of targeted protein degraders has picked up considerable steam recently, with interest stoked further by the first compounds entering Phase III studies. To keep up with leading biotech start-up firms, big pharma has been keen to venture into this new field, bringing along experienced crews of drug hunters. At their disposal, they find a burgeoning body of literature on pharmacokinetics/pharmacodynamics (PK/PD) models tailor-made for this new therapeutic modality. However, this ocean of opportunities might seem daunting even to veteran scientists. Here, we provide orientation and direction for researchers to find the approach best suited for their respective questions.