PROTAC ADCs: Incorporating Historical Learnings to Navigate Novel Payload Development Beyond Blind Potency

  • Highlighting rationale for developing the first reported degrader payloads versus a known oncology target in light of lack of efficacy from small molecule inhibitors
  • Laying out medicinal chemistry approaches to optimize PROTAC payload properties and exploring variety of conjugation approaches
  • Showcasing potent data generated in preclinical models and highlighting next steps in novel payload development