A collaboration of Australian scientists has identified a new imaging radiotracer as an excellent PET contrast agent for melanoma in laboratory mice. The so called [18F]N-(2-(Diethylamino)ethyl)-6-fluoronicotinamide is now scheduled to begin clinical trials sometime next year, according to the press release by the American Chemical Society.
From the abstract in Journal of Medicinal Chemistry:
The high melanoma uptake and rapid body clearance displayed by our series of [123I]iodonicotinamides prompted the development of [18F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([18F]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [18F]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [18F]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.
Image: [18F]2 PET image analysis of murine melanoma. (A) Whole body and (B) transaxial PET images of a C57BL/J6 black mouse bearing a B16F0 tumor allograft (right flank) at 1 h postinjection of [18F]2. (C) Autoradiographic and (D) photographic images of [18F]2 uptake in melanotic areas of a B16F0 tumor frozen section from a 1 h autoradiographic acquisition of [18F]fluorine disintegrations.
Press statement by the American Chemical Society: A potential new imaging agent for early diagnosis of most serious skin cancer…
Full article in Journal of Medicinal Chemistry: Discovery of [18F]N-(2-(Diethylamino)ethyl)-6-fluoronicotinamide: A Melanoma Positron Emission Tomography Imaging Radiotracer with High Tumor to Body Contrast Ratio and Rapid Renal Clearance