Novel 18F-Labeled PET-Tracers for Use in Treatment of Neurological Disorders

Background

Dysregulation of Glycogen Synthase Kinase 3β (GSK3β) is associated with several neurodegenerative diseases, such as Parkinson’s, Alzheimer’s and Huntington’s. Therefore, development of a selective GSK3β PET tracer would enable both, early detection of its aberrant activity and facilitate therapeutic drug discovery. However, efforts to develop a potent tracer has remained unsuccessful due to either poor penetration of the blood-brain-barrier (BBB) and/ or short half life of traditional radio-label conjugate, 11C, used as a radio-label.

Technology

Researchers at Stony Brook University have developed novel 18F radiolabeled GSK3β inhibitors. 18F radiolabeling offer several advantages to these inhibitors:-Long half life (t1/2 = 109.7m) which eliminates the reliance on in-house cyclotron thus facilitating wide spread use.-Better spatial resolution and image quality due to short range positron emission. Additionally, these compounds are highly potent (IC50 = 1.7nM) and have been demonstrated to cross BBB in rodents (Figure 1.).Further Details: Hu et al. ACS Medicinal Chemistry Letters, 8, 287-292, 2017

Advantages

Longer t1/2 of 18F ( vs traditional 11C) labeled tracers-Demonstrated brain penetration-Improved spatial resolution and image quality-High potency

Application

- Medical Imaging- Diagnostics- Therapeutics

Patent Status

Patent application submitted

Stage Of Development

PCT application covering compositions and methods of use (PCT/US18/13446).

Licensing Potential

Licensing Status

Additional Info

https://stonybrook.technologypublisher.com/files/sites/sxmoen3syqdlibhcld3q_mstat1.png Please note, header image is purely illustrative. Source: SciBiograph, Wikimedia Commons, CC BY-SA 4.0, edited.