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Clinical Evaluation of 5-Bromo-5-fluoro-6-methoxy-dihydro-2'-deoxyurindine¹

Division of Chemotherapy Research, Sloan-Kettering Institute for Cancer Research, the Medical Oncology Service, Department of Medicine, Memorial and James Ewing Hospitals, and Cornell University Medical College, New York, New York, and Hoffmann-La Roche Inc., Nutley, New Jersey

5 - Bromo - 5 - fluoro - 6 - methoxy - dihydro - 2' - deoxyuridine (MeOBrFUdR) was given to 22 patients with far-advanced, nonresectable neoplastic diseases. Of these, 16 received an adequate course of therapy. MeOBrFUdR produced biologic effects indistinguishable from those caused by 5-fluoro-2'-deoxyuridine (FUdR) at approximately equimolar doses. Two of the 16 patients showed significant therapeutic responses, a response rate that would be expected with FUdR.

By biochemical and microbiologic methods, appreciable levels of FUdR were found to persist in the blood and urine of patients for 16 hours after administration of MeOBrFUdR, a much longer period than that following the administration of similar doses of FUdR. The persistence of detectable levels of FUdR in the blood did not result in increased toxicity of MeOBrFUdR as compared to FUdR.

¹ This investigation was supported in part by Research Grants CA-03215 and CA-05826 and CA-08748 from the National Cancer Institute, USPHS. Some of this material was presented at the 57th Annual Meeting of the American Association for Cancer Research in 1966 (22). Send reprint requests to Dr. Bayard Clarkson, Sloan-Kettering Institute, 410 East 68th Street, New York, N. Y. 10021.

Received 1/27/67. Accepted 6/29/67.