NEW SGLT PET TRACERS TO MONITOR GLUCOSE TRANSPORT AND METABOLISM
UCLA Technology Available For Licensing

BACKGROUND:  2-deoxy-2-[18F]fluoro-D-glucose (2-FDG) is the most widely used positron emission tomography (PET) tracer. 2-FDG is a substrate for facilitated glucose transporters (GLUTs) and when taken up be cells it is converted to 2-FDG-6-phosphate. This enables the in vivo assessment of regional glucose metabolic rates in animals and humans. 2-FDG has also been widely used to detect tumors in the body since tumors have a high demand for energy intake associated with high GLUT activity. However, 2-FDG has certain drawbacks. First, not all tumors express GLUTs, and second, 2-FDG is rapidly excreted by the kidneys into the urinary bladder. This makes it difficult to use 2-FDG to diagnose certain cancers, e.g., prostate cancer since 2-FDG excreted in the bladder as urine obscures visualization of the prostate.

There is a second class of glucose transporters expressed in the body, the sodium-D-glucose co-transporters (SGLTs), for which 2-FDG is a poor substrate. The SGLTs are expressed in the kidneys, intestine and other organs such as the heart and brain and in the field of diabetes much attention has focused on the use of oral SGLT inhibitors to control blood glucose levels,. For example, inhibitors of the renal isoform, SGLT2, are in clinical trials to lower blood glucose by increasing renal excretion. In addition, nitrogen mustard glucose derivatives, substrates for SGLTs, are in clinical trials for treatment of tumors expressing SGLTs.

INNOVATION:  UCLA researchers have developed a new and novel set of PET tracers specific for SGLT glucose transporters.

POTENTIAL APPLICATIONS:  UCLA researchers have shown that these tracers may be used to measure in the living human the efficacy of SGLT inhibitors which are associated with a variety of metabolic diseases such as obesity, diabetes and diabetes related complications. These researchers have also shown in clinical trials that these new SGLT tracers may be used to follow the progress and efficacy of various treatments for some brain tumors and other brain diseases.

These new tracers may be used in patients to detect, stage and monitor a variety of tumors expressing SGLT activity such as prostate, pancreatic and brain cancers. In addition, these new tracers may be used to evaluate renal failure, and monitor renal function in patients with diabetes, transplanted kidneys and end stage renal disease, and to monitor SGLT activity in the brain of patients suffering from Alzheimer's disease, Parkinson's disease, dementia, brain injury, trauma, stoke, and epilepsy before and after therapeutic interventions. Not only may these tracers be used to measure patient response to treatments but they may also accelerate drug development, facilitating the selection of experimental drug candidates and evaluating their efficacy in animals and humans, thus increasing the savings for pharmaceutical companies during drug development and clinical trials; moreover, immediate information regarding the efficacy of their SGLT therapeutics may be gathered from cells and animal and human subjects.

Reference: UCLA Case No. 2004-192 Patent Application: WO/2006/127842

For additional technical details and current licensing
availability, please contact the following UCLA office:

UCLA Office of Intellectual Property
11000 Kinross Avenue, Suite #200
Los Angeles, CA 90095-7231
Tel: 310-794-0558 Fax: 310-794-0638
email: ncd@research.ucla.edu
NCD URL:   http://www.research.ucla.edu/tech/ucla04-192.htm

Lead Inventor: Ernest Wright

UCLA Technologies Available for Licensing
http://www.research.ucla.edu/oipa/industry

Copyright © 2006 The Regents of the University of California.

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