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Phase I study of ftorafur, an analog of 5‐fluorouracil
Author(s) -
Smart Charles R.,
Townsend Leroy B.,
Rusho William J.,
Eyre Harmon J.,
Quagliana Joseph M.,
Wilson Merrill L.,
Edwards Charles B.,
Manning Steven J.
Publication year - 1975
Publication title -
cancer
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.052
H-Index - 304
eISSN - 1097-0142
pISSN - 0008-543X
DOI - 10.1002/1097-0142(197507)36:1<103::aid-cncr2820360106>3.0.co;2-k
Subject(s) - medicine , nausea , retching , vomiting , leukopenia , fluorouracil , toxicity , anesthesia , gastroenterology , chemotherapy
Abstract Ftorafur, a furanyl analog of 5‐fluorouracil (5‐FU), is reported to be five to six times less toxic and possibly more effective in cancer of the breast and colon than 5‐FU. The drug was synthesized, formulated, and utilized in toxicologic studies, and then in 24 patients with advanced incurable malignancies. When Ftorafur is given by intravenous push, it results in immediate flushing, dizziness, nausea, retching, and in some cases transient hypotension. These immediate side effects are largely eliminated by administering the drug slowly by infusion. In patients, 60 mg/kg of Ftorafur given i.v. daily for up to 10 days resulted in mild toxicity. However, 80 mg/kg given i.v. daily for 7 days resulted in severe toxicity, with nausea, vomiting, stomatitis, leukopenia, and thrombocytopenia. These studies confirm those of the Russian investigators as to toxicity and dosage, even with a different method of administration more convenient for therapy. Phase II studies are presently being carried out to compare the effectiveness of Ftorafur and 5‐FU.