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Initial Clinical Studies with 5-Iodo-2'-deoxyuridine^*

Paul Calabresi, Sergio S. Cardoso, Stuart C. Finch, Morton M. Kligerman, Carl F. von Essen, Ming Y. Chu and Arnold D. Welch

( Departments of Medicine, Pharmacology, and Radiology, Yale University School of Medicine, New Haven, Conn.)

The results of preliminary clinical pharmacological investigations of 5-iodo-2'-deoxyuridine (IUDR), an analog of thymidine, are reported.

With dosages of 100–120 mg IUDR/kg, infused intravenously during periods of 2–3 hours daily for 5 or 6 days, studies of the urinary excretion of IUDR, 5-iodouracil, and iodide indicated that significant blood levels of IUDR were maintained for approximately 4 hours. The major toxic effects of such dosage regimens were stomatitis, leukopenia, and alopecia.

In the present series, evidence of modest tumor inhibition was observed in six of sixteen patients with advanced neoplastic disease.

Possible areas for future investigations with this compound, particularly in combination with other antimetabolites and radiation therapy, have been discussed.

^* These studies were supported by grants from the National Cancer Institute (CY-2817), N.I.H. (OG-14) and by an emergency grant from the Connecticut Division of the American Cancer Society which permitted a supply of the compound (5-iodo-2'-deoxyuridine) to be obtained.

Field investigator, National Cancer Institute.

Research Fellows supported by a Training Grant (C-5012) of the National Cancer Institute.

Received 10/25/60.

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