title: [Selective anticancer effects of intra-arterial infusion of 3',5'-dioctanoyl-5-fluoro-2'-deoxyuridine (TT82) in hepatocellular carcinoma].
abstract: 3'-5'-Dioctanoyl-5-fluoro-2'-deoxyuridine (TT 82), one of the lipophilic prodrugs of 5-fluoro-2'-deoxyuridine mixed with Lipiodol (LPD), was injected into the hepatic artery before hepatic resection in 4 patients with hepatocellular carcinoma. Later, the anti-cancer effects of the drug were evaluated mainly by the examination of resected specimens. The serum alpha-fetoprotein levels of three patients in whom the values were over normal range fell to less than 50% of pretreatment values from 7 to 14 days after the injections. In pathological observation of the specimens, the necrosis rates of main tumors were 100%, 70%, 30% and 0%, respectively. In three patients whose main tumors showed complete or partial necrosis, selective depositions of LPD in the tumors were observed on soft X-ray photographs. The concentrations of TT 82 and its metabolites in the tissues of LPD-depositing areas were markedly higher than those in tissue of the regions without LPD deposits. These findings suggested that TT82-Lipiodol mixture remained selectively in the cancerous tissues and exhibited anticancer effects following injection into the hepatic artery.
authors.affiliation: Dept. of Surgery, Center for Adult Diseases, Osaka.
authors.forename: T
authors.initials: T
authors.lastname: Shibata
authors.forename: Y
authors.initials: Y
authors.lastname: Sasaki
authors.forename: S
authors.initials: S
authors.lastname: Imaoka
authors.forename: H
authors.initials: H
authors.lastname: Wada
authors.forename: H
authors.initials: H
authors.lastname: Nagano
authors.forename: O
authors.initials: O
authors.lastname: Ishikawa
authors.forename: H
authors.initials: H
authors.lastname: Ohigashi
authors.forename: I
authors.initials: I
authors.lastname: Fukuda
authors.forename: T
authors.initials: T
authors.lastname: Kabuto
authors.forename: M
authors.initials: M
authors.lastname: Hiratsuka
mesh_terms: D000368:Aged; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D003131:Combined Modality Therapy; D004341:Drug Evaluation; D005260:Female; D005467:Floxuridine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D006499:Hepatic Artery; D006801:Humans; D007261:Infusions, Intra-Arterial; D007459:Iodized Oil / Q000008:administration & dosage / Q000627:therapeutic use; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008297:Male; D008875:Middle Aged; D009336:Necrosis; D014018:Tissue Distribution
chemical_list: D000964:Antimetabolites, Antineoplastic; D005467:Floxuridine; C051858:3',5'-dioctanoyl-5-fluoro-2'-deoxyuridine; D007459:Iodized Oil