Author:

Patrick McConville, PhD, Chief Scientific Officer, Senior Vice President and Co-founder

Date:

March 1, 2016

The use of PET imaging to detect and quantify receptor occupancy (RO) has become a translational standard in CNS discovery and clinical trials. For example, 18F radiolabeling of targeted small molecules enables a PET tracer-based PD biomarker. The tracer can be used for dynamic, non-invasive quantification of percentage RO.

For relevant targets, rodent models can be used to quickly and efficiently:

  • Screen for specificity
  • Validate the target using a cold blocking compound
  • Generate a full dose-RO curve
  • Compare candidate molecules

Promising molecules can then be more confidently selected for NHP and/or first in human studies. This inherently also allows quantification of RO, and correlation with efficacy in future translational work.

CNS RO - graphic (EWM)

 

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