ganu and ranimustine

Topics: Animals; Antineoplastic Agents; Drug Evaluation; Humans; Japan; Neoplasms; Neoplasms, Experimental; Nimustine; Nitrosourea Compounds; Streptozocin

The effects of Ara-C derivatives, 5-FU derivatives and water-soluble nitrosoureas on L1210 leukemia implanted intracerebrally have been evaluated. Daily treatment with BH-AC showed a similar effect to that of Ara-C and intermittent treatment with BH-AC showed a marked effect. Daily treatment with FT-207, UFT and HCFU, 5-FU derivatives, resulted in more than 50% ILS but the effects of these compounds were inferior to those of ACNU and BH-AC. MCNU, a water-soluble nitrosourea, was effective, but less so than ACNU.

Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Blood-Brain Barrier; Brain Neoplasms; Cytarabine; Fluorouracil; Leukemia L1210; Mice; Neoplasm Transplantation; Nimustine; Nitrosourea Compounds; Streptozocin; Tegafur; Uracil

ACNU, GANU and MCNU, water-soluble nitrosoureas, have been evaluated in terms of influence of treatment schedule on antitumor activity in mice bearing L1210 leukemia. The results obtained were as follows: 1) ACNU produced a significant increase in life span and long-term survivors by administration on day 1 only, once every 8 days for 2 doses or once every 4 days for 3 doses, and the compound was most effective when given on day 1 only. 2) GANU produced a significant increase in life span and long-term survivors by same administration schedules as ACNU, and the compound was most effective when given every 8 days for 2 doses. 3) MCNU produced a significant increase in life span and long-term survivors by each administration including daily treatment, and the compound was most effective when given every 4 days for 3 doses. 4) ACNU and MCNU displayed the same level of activity as CCNU when the drugs were given on day 1 only. Daily treatment with MCNU was as effective as daily treatment with CCNU. Our results suggest that ACNU, GANU and MCNU should be administered by intermittent schedule as lipid-soluble nitrosoureas such as BCNU, CCNU and MeCCNU.

Topics: Animals; Antineoplastic Agents; Drug Administration Schedule; Leukemia L1210; Mice; Nimustine; Nitrosourea Compounds; Solubility; Streptozocin

A new water-soluble nitrosourea derivative, 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077), was tested for antitumor activity against murine tumors and a human mammary carcinoma (MX-1) implanted in athymic mice, and the results were compared with those obtained with five other nitrosourea derivatives currently in clinical use: 1-(2-chloroethyl)-3-(methyl-alpha-D-glucopyranos-6-yl)-1-nitrosourea (MCNU), 1-(2-chloroethyl)-3-(beta-D-glucopyranosyl)-1-nitrosourea (GANU), 3-[(4-amino-2-methyl-5-pyrimidinyl) methyl]-1-(2-chloroethyl)-1-nitrosourea hydrochloride (ACNU), chlorozotocin, and 1-(2-chloroethyl)-3-(4-methylcyclohexyl)-1-nitrosourea (Me-CCNU).

Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Drug Administration Schedule; Female; Humans; Leukemia L1210; Leukemia P388; Lung Neoplasms; Male; Melanoma; Mice; Mice, Inbred C57BL; Mice, Nude; Neoplasm Transplantation; Neoplasms, Experimental; Nimustine; Nitrosourea Compounds; Streptozocin

Topics: Antineoplastic Agents; Drug Evaluation; Humans; Neoplasms; Nitrosourea Compounds; Streptozocin