title: 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.
abstract: 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.
authors.affiliation: Radiopharmaceuticals Research Institute, Australian Nuclear Science and Technology Organisation, Menai, NSW 2234, Sydney, Australia. ivg@ansto.gov.au
authors.forename: Ivan
authors.initials: I
authors.lastname: Greguric
authors.forename: Stephen R
authors.initials: SR
authors.lastname: Taylor
authors.forename: Delphine
authors.initials: D
authors.lastname: Denoyer
authors.forename: Patrice
authors.initials: P
authors.lastname: Ballantyne
authors.forename: Paula
authors.initials: P
authors.lastname: Berghofer
authors.forename: Peter
authors.initials: P
authors.lastname: Roselt
authors.forename: Tien Q
authors.initials: TQ
authors.lastname: Pham
authors.forename: Filomena
authors.initials: F
authors.lastname: Mattner
authors.forename: Thomas
authors.initials: T
authors.lastname: Bourdier
authors.forename: Oliver C
authors.initials: OC
authors.lastname: Neels
authors.forename: Donna S
authors.initials: DS
authors.lastname: Dorow
authors.forename: Christian
authors.initials: C
authors.lastname: Loc'h
authors.forename: Rodney J
authors.initials: RJ
authors.lastname: Hicks
authors.forename: Andrew
authors.initials: A
authors.lastname: Katsifis
mesh_terms: 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
chemical_list: C543821:N-(2-(diethylamino)ethyl)-6-fluoronicotinamide; D011849:Radioactive Tracers; D009536:Niacinamide