Shibata T, Sasaki Y, Imaoka S, Wada H, Nagano H, Ishikawa O, Ohigashi H, Fukuda I, Kabuto T, Hiratsuka M
Dept. of Surgery, Center for Adult Diseases, Osaka.
Gan To Kagaku Ryoho. 1989 Aug;16(8 Pt 2):3057-61.
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.