Effect of 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea on experimental tumors.
The antitumor activity of 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077), a novel water-soluble nitrosourea derivative, against leukemia L1210, Ehrlich carcinoma, sarcoma 180, Lewis lung carcinoma, Yoshida sarcoma, rat ascites hepatomas and Walker 256 carcinosarcoma was examined and compared with those of 3 reference nitrosourea antitumor agents, 1-(2-chloroethyl)-3-(beta-D-glucopyranosyl)-1-nitrosourea, 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-1-(2-chloroethyl)-1-nitrosourea hydrochloride and 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea. TA-077 exhibited a broad antitumor spectrum against the above tumors. Among these 4 nitrosoureas, TA-077 produced the best therapeutic ratios (OD/ILS30) against leukemia L1210, irrespective of the administration route and schedule employed. The ratio obtained by consecutive treatment (ip) was superior to that by single administration, a unique characteristic of this novel nitrosourea agent. The inhibitory effect of TA-077 on the growth of non-syngenic tumors (solid form) was also significant in all administration routes employed (ip, iv and po). Furthermore, TA-077 showed a marked life-prolonging effect on both early and advanced forms of Lewis lung carcinoma.
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D009607:Nitrosourea Compounds / Q000627:therapeutic use*; D051381:Rats; D011919:Rats, Inbred Strains; D012510:Sarcoma 180 / Q000188:drug therapy
D000970:Antineoplastic Agents; D009607:Nitrosourea Compounds; C035789:TA 077