Antitumor activity of a novel nucleotide derivative, 5'-(1,2-dipalmitoyl-sn-glycero-3-phospho)-5-fluorouridine (TJ14026) on murine tumors.
The antitumor activity of a nucleotide derivative, 5'-(1,2-dipalmitoyl-sn-glycero-3-phospho)-5-fluorouridine (TJ14026), was confirmed following both intraperitoneal and oral administration against a number of murine experimental tumor systems in vivo, which included Meth A fibrosarcoma, B16 melanoma, 5-fluorouracil (5-FU) resistant P388 leukemia, P815 mastocytoma and L5178Y-ML lymphoma. Successive i.p. injections of a small dose (10 mg/kg/d x 10) or intermittent i.p. injections of a larger dose (50 mg/kg/d x 3) were equally effective against the solid form of Meth A fibrosarcoma. Intraperitoneal injection of TJ14026 prolonged the life of mice with 5-FU resistant P388 leukemia. Oral administration of TJ14026 was also effective against P815 mastocytoma and L-5178Y-ML lymphoma in the liver, an P388 leukemia metastasized to the lymph nodes. Glutamate oxaloacetate transaminase (GOT) and glutamate pyruvate transaminase (GPT) levels were elevated in the serum of un-treated mice bearing P815 mastocytoma but not in mice treated with TJ14026.
Hayashi
M
M
Research Division, Kitasato Institute, Tokyo, Japan.
Itoh
H
H
Koshio
T
T
Nakagami
K
K
Komiyama
K
K
D000284:Administration, Oral; D000410:Alanine Transaminase / Q000097:blood; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001219:Aspartate Aminotransferases / Q000097:blood; D004075:Diglycerides / Q000008:administration & dosage / Q000627:therapeutic use*; D004351:Drug Resistance; D007274:Injections, Intraperitoneal; D007680:Kidney Neoplasms / Q000188:drug therapy / Q000556:secondary; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy / Q000556:secondary; D051379:Mice; D008807:Mice, Inbred BALB C; D008815:Mice, Inbred Strains; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D014500:Uracil Nucleotides / Q000008:administration & dosage / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D004075:Diglycerides; D014500:Uracil Nucleotides; C084195:TJ 14026; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase