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紫杉醇(tax、泰素、特素、紫素)(Paclitaxel (Taxol, tax, paclitaxel, paclitaxel))
紫杉醇(tax、泰素、特素、紫素)(Paclitaxel (Taxol, tax, paclitaxel, paclitaxel))
[name of drug]
Paclitaxel
English Name: Paclitaxel
Other name: Paclitaxel, taxol, paclitaxel, paclitaxel, Anzatax, Paclitaxelum, PTX, Taxol
[clinical application]
Mainly used for the treatment of ovarian cancer and breast cancer (ovarian cancer after first-line chemotherapy or chemotherapy; multiple failure after combination chemotherapy in metastatic breast cancer failed or breast cancer recurrence within 6 months of adjuvant chemotherapy), and has a certain curative effect on lung cancer, esophageal cancer, gastric cancer, colorectal cancer, soft tissue sarcoma, melanoma, head and neck cancer, lymphoma, brain tumor, seminoma etc..
[pharmacology]
1. pharmacodynamics. This medicine is an anticancer drug extracted from short leaf yew (Taxus brevis) or semisynthetic. Can be applied to the microtubule / microtubule system, promote tubulin assembly into microtubules, but also inhibit the depolymerization of microtubules, which leads to the abnormal arrangement of microtubules, the formation of star shaped body, the spindle lose normal function, leading to cell death. The drug also induces the formation of nonfunctional microtubules in the absence of guanosine three phosphate (GTP) and microtubule associated protein (MAP).
In the screening of human tumor cell lines and experimental animals, this medicine is effective for many kinds of tumors and belongs to broad-spectrum antitumor agents. For cisplatin and doxorubicin resistant individuals, the use of this drug is also effective.
2. 、 the peak concentration (Cmax) of serum was 435-802ng/mL after intravenous drip, and the concentration of serum could reach the level of cytotoxic activity 6-12 hours after the end of infusion (85ng/mL). The binding rate of plasma protein was 89%-98%. In the plasma, the elimination was two compartment model, with an average half-life of alpha phase of 0.27 hours, and a beta phase of 6.4 hours. Mainly metabolized in the liver
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