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Synthesis and Distribution of a Radiolabeled Antitumor Agent: cis-Diamminedichloroplatinum (II)

Yale University School of Medicine, New Haven, Connecticut

Correspondence: For reprints contact: Richard P. Spencer, Nuclear Medicine Section, Yale University School of Medicine, 333 Cedar St., New Haven, Conn. 06510.

ABSTRACT

The antitumor compound cis-Pt(NH₃)₂Cl₂ was synthesized from ^193mPt, and its structure confirmed by three criteria. Following intravenous injection into rabbits, most activity occurred in the kidneys, urine, and liver. In mice a similar distribution was shown with rapid excretion of the radiolabel (79% eliminated by 24 hr). There was little, if any, activity in the brain. The radiolabeled compound presents an almost unique opportunity to trace the distribution of an antineoplastic substance during life.