Finding a needle in the haystack: ADME and pharmacokinetics/pharmacodynamics characterization and optimization towards orally available bifunctional protein degraders

Despite many recent advances in the field, continued research will further our understanding of rational design regarding degrader optimization. Machine-learning and computational approaches will become increasingly important once larger, more robust datasets become available. Furthermore, tissue-targeting approaches (particularly regarding the Central Nervous System will be increasingly studied to elucidate efficacious drug regimens that capitalize on the catalytic mode of action. Finally, additional specialized approaches (e.g. covalent degraders, LOVdegs) can enrich the field further and offer interesting alternative approaches.