In early discovery, an increasing number of small molecule drug candidates are challenging to deliver orally due to poor solubility and/or low permeability. Additionally, there are a number of research fields where small molecules have broken through 500 molecular weight (i.e. - protein degraders, molecules that address protein-protein interactions, etc.), and there is opportunity to design in amphiphilicity into molecules without sacrificing potency and selectivity. This talk will focus on the question: Is there opportunity to take advantage of amphiphilicity in small molecules to boost their absorption potential?
The question will be addressed by examining a case study of a poorly soluble, small molecule drug candidate. The talk will include an explanation of in vitro and in vivo data that enabled the identification and characterization of molecular amphiphilicity.
Learning Objectives:
Explain the biopharmaceutic advantages that an amphiphilic drug molecule can present
Recognize discrepancies in physiochemical property measurements, absorption potential models and in vivo data that may indicate molecular amphiphilicity
Design in vitro tests to identify and characterize molecular assembly of an amphiphilic molecule
