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Discovery and Basic Research
Speaker Spotlight

Speaker Spotlight: Assessment of Permeability: Bridging Traditional and Novel Compounds in Discovery

Monday, October 21, 2024
9:30 AM – 10:30 AM MT
Location:Spotlight Stage A, Aisle 1100, Exhibit Hall

Discovery and Basic Research

Optimizing in vitro ADME assays to Deliver Orally Bioavailable PROTACs
A significant challenge with oral bioavailability for large and complex molecules like PROTACs, lies in their propensity to experience poor intestinal absorption. Factors such as low membrane permeability, instability within the intestinal environment, and susceptibility to enzymatic degradation, all can hinder their ability to be orally bioavailable.

Learning objectives:
How useful are ADME properties for design and optimization of PROTACs
Opportunities of different analytical and in silico tools to advance drug design
Identify and resolve the challenges within in vitro ADME assays in drug discovery (DDI, PPB, Metabolic stability etc)

Learning Objectives:

  • Understand the importance of intestinal permability in oral delivery and the difficulties with Protein degraders.
  • Provide an explanation of permeability methods and their applications using protein degraders molecules.
  • Recognize that assay modification are needed to measure permeability for protein degraders and how innovative solutions can help improve prediction of drug permeability.
  • How useful are ADME properties for design and optimization of PROTACs, learn about opportunities of different analytical and in silico tools to advance drug design, and Identify and resolve the challenges within in vitro ADME assays in drug discovery (DDI, PPB, Metabolic stability etc).