Abstract |
A phase I study of a new floxuridine derivative, FF-705, was performed in patients with various types of solid tumors. Efficacy of single oral administration with dose range of 300 to 700 mg/body was studied in 12 patients. At a dose of 500 mg/body transient increases of s GOT and s GPT were noted in one patient and, of 700 mg/body, nausea, vomiting or stomach dullness sensation was noted in two patients. The maximum tolerated dose was considered to be 700 mg/body or more. The dose limiting factor was a gastrointestinal toxicity. Oral administration in five consecutive days was studied in 23 patients to doses ranging 100 to 700 mg/body. The incidence of side effects were increased with dose escalation, and at a dose of 700 mg/body side effects were seen in all patients. The maximum tolerated dose was considered to be 700 mg/body/day, and the dose limiting factor was gastrointestinal toxicity. The optimal dose of FF-705 for consecutive administration is considered to be within the range of 200 to 300mg/body/day. Serum and urine concentrations of metabolites were assayed in 7 patients receiving single dose of 600 mg/body. In all patients serum concentration of floxuridine ( FUDR) was higher than that of 5-FU and other metabolites at all points of measurement. The highest concentration of FUDR was detected at 2 hours after drug administration and the mean value was 0.04 microgram/ml. The main metabolite in the urine was 5'-acetyl-FUDR which was excreted 0.8% to the dose for 24 hours. The other metabolites were excreted less than 0.2%.
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Authors | |
Journal | Gan to kagaku ryoho. Cancer & chemotherapy
(Gan To Kagaku Ryoho)
Vol. 11
Issue 1
Pg. 143-9
(Jan 1984)
ISSN: 0385-0684 [Print] Japan |
PMID | 6230054
(Publication Type: English Abstract, Journal Article)
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Chemical References |
- Capsules
- Floxuridine
- 2'-deoxy-3',5'-di-O-acetyl-5-fluoro-3-(3-methylbenzoyl)uridine
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Topics |
- Administration, Oral
- Adult
- Aged
- Breast Neoplasms
(drug therapy, metabolism)
- Capsules
- Drug Administration Schedule
- Drug Evaluation
- Female
- Floxuridine
(analogs & derivatives, therapeutic use)
- Humans
- Lung Neoplasms
(drug therapy, metabolism)
- Male
- Middle Aged
- Neoplasms
(drug therapy, metabolism)
- Stomach Neoplasms
(drug therapy, metabolism)
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