Columbia Technology Ventures

An improved tracer for serotonin receptor 5HT1A suitable for clinical trials of central nervous system diseases

The neurotransmitter serotonin is studied because of its role in a variety of diseases such as anxiety, depression, schizophrenia, and Parkinson’s disease. One of the most widespread receptors for serotonin is the 5HT1A receptor. Because of its integral role in several pathologies, the ability to study the effects of drugs and other treatments on the binding of serotonin to its receptors is an important area of study. Receptor specific radio-labeled ligands, which can be imaged via positron emission tomography (PET), are currently employed to assess serotonin/receptor interactions, receptor binding and target occupancy by therapeutic medication candidates. There exist, however, a limited number of 5HT1A tracers suitable for studies in a living brain. Further, there is a need for improvement in both the selectivity, ease of radio-labeling and isotope half-life of these tracers. This technology, which describes a 5HT1A tracer with high selectivity and longer half-life isotopes, addresses both of these needs, allowing for multi-center clinical trials and an improved understanding of the impact of drugs on central nervous system diseases.

By using an F-18 labeled tracer instead of C-11, the half-life of the tracer is extended making it suitable for off-site distribution

Currently, C-11 tracers for the 5HT1A receptor exist and are used for research studies. However, because of its short half-life (20 minutes), the C-11 tracer can only be used at high-tech facilities that can produce it in a local cyclotron. F-18 tracers, on which this technology is based on, have an extended half-life (120 minutes) that allows the tracer to be distributed up to 200 miles from the production facility. Widespread distribution is necessary for multi-center clinical trials making the F-18 tracer an ideal candidate for further studies of the 5HT1A receptor.

The effectiveness of these new tracers have been demonstrated in the laboratory and in animal testing with two Papio Anubis.

Lead Inventor:

J. John Mann, M.D.

Applications:

  • Clinical trial study of the neuropathology of several brain disorders
  • Evaluate target occupancy of new treatments for brain disorders and evaluation of pharmacodynamics effects of new drugs or treatments for a variety of CNS related diseases
  • Pre-clinical research on the serotonin receptor 5HT1A

Advantages:

  • F-18 tracers have an extended half-life compared to C-11
  • Ease of distribution allows for multi-center clinical trials for serotonin related diseases are possible
  • High selectivity towards the 5HT1A serotonin receptor

Patent Information:

Patent Pending (US 20080138283)

Tech Ventures Reference: IR 2717

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