title: [Drug concentration in cancerous large bowel tissue and thymidylate synthase inhibition rate after administration of tegafur and UFT].
abstract: Tegafur and UFT are most widely used for the treatment of cancers of the gastrointestinal tract. FdUMP, a metabolite of 5-fluorouracil(5-FU), is known to have an inhibitory activity of thymidylate synthase (TS). We administered 600 mg/day of tegafur or UFT to 37 patients with cancer of the large bowel beginning 1 week prior to surgery and then measured the concentrations of tegafur and 5-FU, and TS inhibition rate in the excised tissue. Our results showed that the concentrations of 5-FU in tumor were 0.077 +/- 0.026 microgram/g in tegafur group and 0.208 +/- 0.143 microgram/g in UFT group, with the UFT showing significantly higher levels (p less than 0.05). On the other hand, TS inhibition rates in tumor tissue were 45.5 +/- 13.3% in tegafur group and 56.1 +/- 13.0% in UFT group, with a significantly higher level existing in the latter group (p less than 0.05). Furthermore, the same high 5-FU concentration and TS inhibition rates were observed in the lymph nodes affected by metastasis. No difference between the tegafur and UFT groups was noted in normal tissue or normal lymph nodes, and compared to tegafur, UFT showed an effective action on cancerous large bowel tissue.
authors.affiliation: Dept. of Surgery, Chikushi Hospital, Fukuoka University.
authors.forename: K
authors.initials: K
authors.lastname: Futami
authors.forename: S
authors.initials: S
authors.lastname: Arima
authors.forename: S
authors.initials: S
authors.lastname: Yoshimura
authors.forename: T
authors.initials: T
authors.lastname: Okamoto
authors.forename: K
authors.initials: K
authors.lastname: Yamasaki
authors.forename: T
authors.initials: T
authors.lastname: Koto
authors.forename: S
authors.initials: S
authors.lastname: Yamasaki
authors.forename: K
authors.initials: K
authors.lastname: Kawahara
authors.forename: T
authors.initials: T
authors.lastname: Ikuno
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D000971:Antineoplastic Combined Chemotherapy Protocols; D003106:Colon / Q000378:metabolism*; D015179:Colorectal Neoplasms / Q000188:drug therapy / Q000201:enzymology* / Q000473:pathology; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D005641:Tegafur / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured; D014498:Uracil / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D005641:Tegafur; D014498:Uracil; D013940:Thymidylate Synthase