This technology is a radiolabeled microtubule binding agent that enables positron emission tomography (PET) imaging of microtubules in the brain for diagnosis and treatment monitoring of tumors and neurological disease.
Unmet Need: CNS-penetrating PET tracer for in vivo microtubule imaging
Microtubule dysregulation is associated with many diseases including cancer and neurodegenerative diseases such as Alzheimer’s Disease, Parkinson’s Disease, and ALS, making them an important diagnostic and therapeutic target. PET is a non-invasive molecular imaging technique currently used for in vivo imaging. Although this imaging technique is powerful, imaging the brain is challenging because the radiotracers used must be capable of crossing the blood brain barrier (BBB). There are currently no PET tracers available for the in vivo imaging of microtubules in the brain.
The Technology: Radiolabeled microtubule binding agents for PET imaging in the CNS
This technology identifies high affinity microtubule-binding agents that can be radiolabeled with carbon-11 (11C) or fluorine-18 (18F). These agents are small enough to penetrate the BBB and be used for radiolabeling microtubules in the central nervous system (CNS) and other parts of the body. These radiolabeled microtubule binding agents enable live in vivo PET and single photon emission computed tomography (SPECT) imaging that can be used to look at tumors, neuropsychiatric, and neurodegenerative disorders.
[11C]MPC-6827 was synthesized and shown to cross the BBB and distribute rapidly to multiple brain regions in imaging studies.
Applications:
- PET or SPECT diagnostic imaging and treatment monitoring of brain tumors
- PET or SPECT diagnostic imaging and treatment monitoring of neurodegenerative diseases including Alzheimer’s or Parkinson’s disease
- Diagnosis and treatment monitoring of traumatic brain injury, psychiatric disorders, and other microtubule-associated disease in the brain and peripheral body parts
- Evaluating response to microtubule-targeting drugs
- Quantification of disease progression and remission
- Quantification of target occupancy
- Research tool for identification of genetic determinants of microtubule-mediated disease
- Tumor drug resistance determination
- Drug development based on microtubule pathophysiology
- Studying pathophysiology of psychiatric disorders
Advantages:
- Microtubule-specific
- Capable of crossing the blood-brain barrier
- Can be used for imaging and quantification
- Labels microtubules in both periphery and brain
- Non-invasive
- Can be used repeatedly over time
Lead Inventor:
J. John Mann, M.D.
Patent Information:
Patent Status
Related Publications:
Solingapuram Sai KK, Prabhakaran J, Ramanathan G, Rideout S, Whitlow C, Mintz A, Mann JJ, Kumar JSD. “Radiosynthesis and Evaluation of [11C]HD-800, a High Affinity Brain Penetrant PET Tracer for Imaging Microtubules” ACS Med Chem Lett. 2018 Apr 30;9(5):452-456.
Kumar JSD, Solingapuram Sai KK, Prabhakaran J, Oufkir HR, Ramanathan G, Whitlow CT, Dileep H, Mintz A, Mann JJ. “Radiosynthesis and in Vivo Evaluation of [11C]MPC-6827, the First Brain Penetrant Microtubule PET Ligand” J Med Chem. 2018 Mar 8; 61(5): 2118-2123.
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