Discovery of [F-18]N-(2-(Diethylamino)ethyl)-6-fluoronicotinamide: a melanoma positron emission tomography imaging radiotracer with high tumor to body contrast ratio and rapid renal clearance

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. © 2009, American Chemical Society

Keywords

Drugs, Neoplasms, Renal clearance, Positron computed tomography, Nicotinamide, Clinical trials

Citation

Greguric, I., Taylor, S. R., Denoyer, D., Ballantyne, P., Berghofer, P., Roselt, P., Pham, T.Q., Mattner, F., Bourdier, T., Neels, O. C., Dorow, D.S., Loc'h, C., Hicks, R. J., & Katsifis, A. (2009). Discovery of [f-18]n-(2-(diethylamino)ethyl)-6-fluoronicotinamide: a melanoma positron emission tomography imaging radiotracer with high tumor to body contrast ratio and rapid renal clearance. Journal of Medicinal Chemistry, 52(17), 5299-5302. doi:10.1021/jm9008423