Fatty acid-anticancer conjugates and uses thereof
a technology of conjugates and fatty acids, applied in the field of fatty acid-anticancer conjugates, can solve the problems of limited therapeutic doses, inability to achieve effective treatment of cancer, and inability to achieve and achieving the effect of improving the therapeutic index of anticancer compounds
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Example 1
The Effects of Taxoprexin and Paclitaxel Against M 109 Lung Carcinoma in Mice
[0069]Syngeneic mice were injected with mouse lung tumor line M (Madison) 109 subcutaneously in the flank. Four days after tumor implantation, when the tumor weighed about 30 mg, taxoprexin (OD=120 mg / kg / day×5 days) or paclitaxel (OD=20 mg / kg / day×5 days) were injected as a bolus through the tail vein on each of five successive days (days 4 through 8). Both drugs were dissolved in 10% cremophor EL / 10% ethanol / 80% saline. Tumor volume was estimated from tumor width and length. The results show that paclitaxel retarded tumor growth for about four days. In contrast, taxoprexin completely eliminated all measurable tumors in eight out of eight mice. (FIG. 1)
example 2
The Effects of Taxoprexin and Paclitaxel Against M 109 Lung Carcinoma in Mice
[0070]Syngeneic mice were injected with mouse lung tumor line M (Madison) 109 subcutaneously in the flank. Five days after tumor implantation, one day later than in the last figure, when the tumors had grown ten-fold larger to 300 mg, taxoprexin (OD=120 mg / kg / day×5 days) or paclitaxel (OD=20 mg / kg / day×5 days) were injected as a bolus through the tail vein on each of five successive days. Both drugs were dissolved in 10% cremophor EL / 10% ethanol / 80% saline. Tumor volume was estimated from tumor width and length. As in the previous experiment, paclitaxel retarded tumor growth for about four days (LCK=1.0). In contrast, taxoprexin completely eliminated all measurable tumors in seven out of eight mice (C / T=7 / 8) at 120 mg / kg / day×5 days, and in four out of seven mice at 80 mg / kg / day×5 days. Histological examination of the tissue where the tumors had showed no tumor cells, only scar tissue. These data show that ta...
example 3
Response of Human NCI-H522 Lung Tumor to Treatment with Taxoprexin and Paclitaxel in Mice
[0071]The Southern Research Institute studied the anti-tumor activity of taxoprexin against human NCI-H522 lung tumor growing in nude mice. The tumors were implanted subcutaneously. Tumor mass was determined by calculation from tumor length and width. The drugs were dissolved in 12.5% cremophor EL / 12.5% ethanol / 75% saline and delivered i.v. into the tail vein, once a day for 5 days, from day 15 to 19 after tumor implantation. The results show that taxoprexin at 50 mg / kg / day×5 days and paclitaxel at 20 mg / kg / day×5 days eliminated all measurable tumors in 10 / 10 mice. (FIG. 3)
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