Optically Active Radio-labeled Reverse Transcriptase Inhibitors
Description of Invention:
Researchers at the NIH developed a novel and efficient method for preparing 18F-labeled reverse transcriptase inhibitors, particularly, 18F-labeled tenofovir analogues for use as PET imaging agents to monitor anti-retroviral drug biodistribution in anatomic compartments in HIV-1 infected patients. Fluorine-18 is often used to prepare radiotracers and radiopharmaceuticals, but its short half-life of 109 minutes demands efficient and rapid radiochemical syntheses and purification techniques. This technology provides high yields of labeled compounds utilizing rapid synthetic methods and HPLC purification in both racemic and optically active forms.
Available for licensing and commercial development are compositions of 18F-labeled tenofovir analogues, as well as methods of synthesis and methods of use for such labeled compounds.
Applications:
Non-invasive in vivo molecular imaging tracer useful for:
Evaluating the penetration and kinetics of anti-HIV drugs into anatomic compartments in vivo.
Addressing changes in drug penetration in anatomic compartments during prolonged exposure to anti-HIV drugs.
Market:
U.S. sales of diagnostic radiopharmaceuticals reached 1.69 billion dollars in 2005 and are expected to reach 3.52 billion dollars by 2012.
Development Status:
Early stage
Inventors:
Dale O. Kiesewetter (NIBIB) Michele Di Mascio (NIAID) Esther Lim (CC)
Patent Status:
DHHS Reference No. E-072-2007/0 Licensing Status: This technology is no longer available for licensing.
