Applying model-informed drug discovery and development (MID3) early in development can reduce late-stage risk by determining feasibility of drugging a given target, prioritizing between targets, or defining optimal drug properties for a target product profile. However, the lack of pharmacokinetic (PK) and pharmacodynamic (PD) data available at early stages can make modeling a challenge. For this reason, we developed Early Feasibility Assessment (EFA): a method for making effective dose predictions using mechanistic PK/PD models built from general biophysical principles and parameterized by data that is readily available early in drug discovery.
Applied BioMath Assess™ is a point-and-click, MID3 software for performing EFA across various modalities. This webinar series will discuss scientific case studies demonstrating how you can quickly inform target selection, project clinical dose requirements, design a lead optimization funnel, and identify areas of program risk.
This webinar will demonstrate how to use Applied BioMath's PROTAC Assess model to:
- Explore PROTAC binding parameters to optimize its potency
- Evaluate the dependence of target expression and turnover on its degradation profile
The model is a cellular model of a targeted protein degrader (TPD). The TPD modeled is a proteolysis targeting chimeric (PROTAC), a heterobifunctional molecule that can bind to E3 ligase, target of interest, or both (forming a ternary complex). Formation of a ternary complex leads to target degradation. Model output is target expression over time. Additional targets of interest (up to 2) can be added to explore selectivity of TPD.