Clinical Development of PROTACs

PROTACs have gained significant attention in recent years due to their capability to target and degrade disease-causing proteins. It is looked upon as a therapeutic that would address resistance mechanisms thus expanding treatment opportunities. The deployment of PROTACs as therapeutic modalities depends upon their translational efficacy from being confined as a lab success to patient utility. Results of the clinical trials done recently heighten the anticipation of integration of PROTACs into treatment regimens. In this chapter, we delve into the cutting-edge realm of targeted protein degradation, specifically focusing on PROTACs. Our exploration encompasses a multifaceted analysis, beginning with pharmacology of PROTACs and examination of biomarkers crucial for monitoring the efficacy and response to PROTAC therapies. Moving forward, we present an overview of ongoing clinical trials, shedding light on their trial designs and the potential these trials hold for the future of anticancer treatments. Moreover, our discussion encompasses dosing strategies for PROTACs, emphasizing the approaches employed in optimizing therapeutic outcomes. Addressing safety concerns and considerations is paramount in our examination, offering a comprehensive understanding of the challenges and advancements in ensuring the well-being of patients undergoing PROTAC-based therapies. Lastly, we explore the frontier of combining PROTACs with other anticancer molecules.