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.
The high melanoma uptake and rapid body clearance displayed by our series of [(123)I]iodonicotinamides prompted the development of [(18)F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([(18)F]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [(18)F]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [(18)F]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.
Greguric
Ivan
I
Radiopharmaceuticals Research Institute, Australian Nuclear Science and Technology Organisation, Menai, NSW 2234, Sydney, Australia. ivg@ansto.gov.au
Taylor
Stephen R
SR
Denoyer
Delphine
D
Ballantyne
Patrice
P
Berghofer
Paula
P
Roselt
Peter
P
Pham
Tien Q
TQ
Mattner
Filomena
F
Bourdier
Thomas
T
Neels
Oliver C
OC
Dorow
Donna S
DS
Loc'h
Christian
C
Hicks
Rodney J
RJ
Katsifis
Andrew
A
D000818:Animals; D055808:Drug Discovery; D006801:Humans; D007668:Kidney / Q000378:metabolism*; D008545:Melanoma / Q000000981:diagnostic imaging* / Q000378:metabolism*; D008657:Metabolic Clearance Rate; D051379:Mice; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000032:analysis / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography; D011849:Radioactive Tracers; D011854:Radiochemistry; D014018:Tissue Distribution
C543821:N-(2-(diethylamino)ethyl)-6-fluoronicotinamide; D011849:Radioactive Tracers; D009536:Niacinamide