TA 077

07/01/1986 - "A phase I study on TA-077, a water-soluble nitrosourea, was performed by a 9-institution clinical group using 89 patients with various malignant tumors. "
10/01/1987 - "Repeated administration of TA-077 (29 to 40 N) for 5 or 6 consecutive days did not affect the pharmacokinetic parameters of TA-077 and TA-G in 7 cancer patients except for slight increases in the half-life and area under the curve of blood TA-G."
10/01/1987 - "TA-G was taken up by the tumor cells much more efficiently than TA-077, explaining the higher sensitivities of the cultured tumor cells to TA-G than to TA-077. "
07/01/1987 - "However, in the i.v.-i.v. system, in which the tumor cells were inoculated intravenously (i.v.) and the drugs were also administered i.v., TA-077 given on the same schedule showed a ratio of 13.7, which was the highest of all the drugs examined. "
07/01/1987 - "system, in which the tumor cells were inoculated intraperitoneally (i.p.) and the drugs were also administered i.p., TA-077 administered daily for five consecutive days showed a therapeutic ratio of 40.6, which was the third highest of all drugs tested. "

10/01/1986 - "Our study suggests that TA-077 is a useful agent as one of the drugs used in combination chemotherapy against NHL, since it was effective for refractory T cell malignancies such as ATLL."

06/01/1982 - "Among these 4 nitrosoureas, TA-077 produced the best therapeutic ratios (OD/ILS30) against leukemia L1210, irrespective of the administration route and schedule employed. "
07/01/1987 - "A comparison of a new nitrosourea derivative, 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea with various antitumor agents with respect to therapeutic ratios in L1210 leukemia systems."
07/01/1987 - "In order to further evaluate the antitumor activity of 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077), the therapeutic ratios (a ratio of the optimal dose versus the dose showing 25% increase in life span) of TA-077 were examined using two L1210 leukemia systems and the results were compared with those of twenty-six antitumor agents for reference. "
10/01/1987 - "TA-077 was also hydrolyzed by suspensions of Yoshida sarcoma, AH130 hepatoma, L1210 leukemia, P388 leukemia and DBLA-10/C leukemia cells. "
06/01/1982 - "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. "

10/01/1987 - "1-(2-Chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077) was hydrolyzed to its glucosyl metabolite TA-G by homogenates of guinea pig organs, rabbit VX-2 carcinoma and rat Yoshida sarcoma. "
10/01/1987 - "TA-077 was also hydrolyzed by suspensions of Yoshida sarcoma, AH130 hepatoma, L1210 leukemia, P388 leukemia and DBLA-10/C leukemia cells. "
06/01/1982 - "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. "

10/01/1987 - "TA-077 was also hydrolyzed by suspensions of Yoshida sarcoma, AH130 hepatoma, L1210 leukemia, P388 leukemia and DBLA-10/C leukemia cells. "
06/01/1982 - "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. "