Carbon-11 labelling of the antitumour agent N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and determination of plasma metabolites in man

• Published in: Applied radiation and isotopes Vol. 48; no. 4; pp. 487 - 492
• Main Authors: Brady, Frank, Luthra, Sajinder K., Brown, Gavin, Osman, Safiye, Harte, Robert J.A., Denny, William A., Baguley, Bruce C., Jones, Terry, Price, Patricia M.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.04.1997
• Subjects: Acridines - chemical synthesis; Acridines - metabolism; Adult; Aged; Aged, 80 and over; Antineoplastic Agents - blood; Antineoplastic Agents - chemical synthesis; Carbon Radioisotopes - chemistry; Dose-Response Relationship, Drug; Female; Humans; Isotope Labeling - methods; Male; Middle Aged; Neoplasms - blood; Neoplasms - diagnostic imaging; Tomography, Emission-Computed
• ISSN: 0969-8043; 1872-9800
• DOI: 10.1016/S0969-8043(96)00294-1

The potential anti-cancer agent n-[2-(dimethylamino)ethyl]acridine-4-carboxamide, DACA has been labelled with carbon-11. N-[2- 11C- methyl]DACA was produced in 73% radiochemical yield from [ 11C]iodomethane in 40 min from EOB. The average radiochemical yield was 3.2 GBq with specific radioactivity of 41.5 GBq μmol −1 at EOS, corresponding to 24 μg of stable DACA. The position of labelling was confirmed by co-labelling with [ 11 13 C] iodomethane . PET studies in patients have been performed prior to Phase I trial of DACA and during Phase I trial of DACA. Analysis of serial plasma samples showed that the metabolism of N-[2- 11C- methyl]DACA is rapid and extensive in patient plasma.