Daunomycin metabolism

A third focus has been directed toward incorporation of conventional PET radionuclides nC or 18F into existing substrates or inhibitors known to interact with Pgp [113-115]. This strategy has been employed to produce various PET agents, including 1 -colchicine, 11C-verapamil, nC-daunomycin, and uC/18F-paclitaxel[115-123]. While promising data have been generated, some of these PET agents suffer from modest radiochemical yields and others from complex pharmacokinetics in vivo mediated, at least in part, by rapid metabolism of the radiolabeled compounds. 

In view of the extensive metabolism of adriamycin and daunomycin it is important to distinguish between parent drug and metabolites in studies of the disposition of these drugs. This was not the case in the early studies and so care has to... 

Neither adriamycin nor daunomycin is absorbed orally [128] due to hydrolysis in the g.i,t. and so they must be administered by i.v. infusion. Both drugs undergo metabolism [129,130] and the predominant metabolites are adriamyci-nol (83) and daunorubicinol (84) respectively, in which the 13-keto group has been reduced. The enzyme responsible is a cytoplasmic aldo-ketoreductase which is found in all tissues, the kidney having the highest activity [131,132]. This is not the only metabolic transformation however, both the parent drug and its 13-dihydro-metabolite are metabolised by microsomal enzymes. Most of the... 

Used as experimental tools, all the nucleic acid binding drugs mentioned in Paragraph 8.1.6 have some kind of antiviral activity (proflavine, daunomycin, actinomycin-D, etc.). Other potential antiviral agents are considered here, as well as substances which for different reasons are more active against the viral than the normal cell metabolism, and interferon which is a natural means of defence of the cell against viral invasion. 

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