Melanoma-targeted delivery system (part 2): Synthesis, radioiodination and biological evaluation in B16F0 bearing mice.

Here we report the synthesis and radiolabelling with iodine-125 of a melanoma-selective prodrug ( 17a* ) and its parent drug IUdR . The in vivo and ex vivo biodistributions of [ 125 I]( 17a* ) and [ 125 I] IUdR were evaluated in a model of melanoma B16F0-bearing mice. The pharmacokinetic profile of [ 125 I]( 17a* ) suggests rapid release of the active drug [ 125 I] IUdR after i.v. administration of [ 125 I]( 17a* ). Preliminary metabolism studies in dedicated compartments (i.e. blood, urine and tumour) yielded results consistent with this hypothesis. [ABSTRACT FROM AUTHOR]