[Selective anticancer effects of intra-arterial infusion of 3',5'-dioctanoyl-5-fluoro-2'-deoxyuridine (TT82) in hepatocellular carcinoma].
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.
Shibata
T
T
Dept. of Surgery, Center for Adult Diseases, Osaka.
Sasaki
Y
Y
Imaoka
S
S
Wada
H
H
Nagano
H
H
Ishikawa
O
O
Ohigashi
H
H
Fukuda
I
I
Kabuto
T
T
Hiratsuka
M
M
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
D000964:Antimetabolites, Antineoplastic; D005467:Floxuridine; C051858:3',5'-dioctanoyl-5-fluoro-2'-deoxyuridine; D007459:Iodized Oil