Our sustained investigation of the clinical pharmacology of antineoplastic agents continues to aid in the investigation of fundamental findings to clinical problems. We have elucidated a major portion of the human biotransformation pathway of adriamycin. This involves carbonyl reduction, reductive glycosidic cleavage, hydrolytic glycosidic cleavage, O-demethylation, O-sulfation, and O-beta-glucuronidation. We have aided in the application of a radioimmunoassay for the anthracyclines in clinical studies and have established new pharmacologic methods and parameters for these agents.