Esophageal cancer chemotherapy drug docetaxel experimental study

By | January 22, 2012

Taxotere Potiere by the French scholar and Rhone-Poulenc Rorer co-development. The premise is from the European yew (Taxus baccata) needles extract, obtained by semi-synthetic drug.Experimental study of docetaxel in vitro experiment, 29 kinds of tumor more sensitive to this drug than the Taxol, but only 13 kinds of tumor more sensitive to paclitaxel. On breast cancer, membrane adenocarcinoma, lung cancer , bladder cancer, colon cancer and melanoma are valid, inhibition was significantly higher than DDP, ADM and VP-16, is also superior to paclitaxel. The activity of B16 melanoma 2.7 times large than paclitaxel, subcutaneous inoculation of P03 and colon adenocarcinoma C51 film effective, but Lewis lung carcinoma, Glasgow osteosarcoma and L12l0, leukemia had no significant effect. Study confirmed that the two drugs do not completely cross-resistance between, DDP and 5-FU with no cross resistance.
Harrison observed such as Taxotere for 6 mice transplanted human tumors, including lung cancer, colon cancer, breast cancer and melanoma. Nicoletti and other observed Taxotere on HOC8, HOCl8 and HOC22 effective graft of ovarian cancer. Other researchers observed that docetaxel to 5 kinds of human ovarian cancer cell line effectively, and more effective than DDP, CTX and ADM.
Experimental Study of Docetaxel, Taxotere and Taxol same mechanism of action, the role of stabilizing microtubules paclitaxel 2 times larger than that, and can induce the assembly of microtubules, but not changing the original Silk. This product is a cycle specific drug, the cells were blocked at M phase. Proliferating cells than non-proliferating cells. Generally does not inhibit DNA, RNA and protein synthesis.
Experimental study of docetaxel in pre-clinical studies have shown that docetaxel and CTX, VP-16 or 5-FU combined synergistic effect, but combined with DDP and ADM did not show any synergistic effect. With paclitaxel is similar to docetaxel radiosensitization also. The intravenous LD50 in mice was 414mg/ml, major toxicity in the cell update soon apparent in the organization. An intravenous drug and medication daily, once a 5, compared the two, the latter in the dog's blood system, digestive tract, nervous system toxicity of testosterone and greater. Taxotere phase distribution of the drug system, and 7min, respectively, and since the half-life of 1.1h, the plasma clearance rate of 2.2L / (kg h). Washout phase also, the terminal half-life of 1h. Drugs in the liver, gallbladder, small intestine and the stomach contents of radioactivity in the highest. After administration of 96h, the drug remaining in the tissue is less than 0.8%, mainly observed in the thymus and the nerve root, cartilage, retina and liver also have a small amount of residue. Dogs and mice, drugs, primarily by the liver, gallbladder removed, excluded less than 10% of urine.

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