生物活性

• 描述Microtubules are the main constituent of mitotic apparatus in all eukaryotic cells, thus make it become an important pharmacological target for the treatment of tumor . Docetaxel Trihydrate is the trihydrate form of Docetaxel. Docetaxel, belong to the taxane family including paclitaxel, can promote the assembly and polymerization of microtubule with an appearance of twice as active in depolymerization inhibition compared with paclitaxel . When treated with Docetaxel for 72h, the significant growth inhibition can be observed in ovarian cancer cell line, including A2780, H134, IGROV-1 and OVCAR-3, with IC50 ranging from 2.8-87nM. Activation of caspase, upregulation of Bcl-2 phosphorylation and apoptosis can be observed in cells with prolonged G2/M arrest by Docetaxel, which may be one of the mechanism for cell death induced by Docetaxel in tumor therapy. However, Docetaxel also shows antiangiogenic effect in in vitro and in vivo studies. It can inhibit HUVEC proliferation in a dose-dependent manner with an IC50 of 0.27 ng/ml, as well as reduce 54% of angiogenesis level compared with control on dose of 3 mg/kg in MCF-7 tumor bearing nude mice .Docetaxel is approved by FDA for treatment of head and neck cancer, gastric cancer, breast cancer, prostate cancer and non-small cell lung cancer (see in FDA net).

• 动物研究
  剂量	Mice: 20 mg/kg[3] (i.v.)
  给药途径	i.v.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01876251	Breast Cancer Metastatic	Phase 1	Terminated(The study was termi... more >>nated on June 24th, 2015 due to change in strategy of PF-03084014 development. There were no safety/efficacy concerns behind the decision.) Collapse <<	-	United States, Alabama ... more >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35233 University of Alabama at Birmingham, IDS Pharmacy Birmingham, Alabama, United States, 35249 University of Alabama at Birmingham Birmingham, Alabama, United States, 35249 United States, California Stanford Cancer Institute Stanford, California, United States, 94305 Stanford Hospital & Clinics-DRUG SHIPMENT ADDRESS only Stanford, California, United States, 94305 Stanford Hospital & Clinics Stanford, California, United States, 94305 Stanford Women's Cancer Center Stanford, California, United States, 94305 United States, Michigan Barbara Ann Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Karmanos Cancer Institute (KCI) Detroit, Michigan, United States, 48201 United States, North Carolina UNC Cancer Hospital Infusion Pharmacy Chapel Hill, North Carolina, United States, 27514 UNC Hospitals, The University of North Carolina at Chapel Hill Chapel Hill, North Carolina, United States, 27599-7600 Belgium Jules Bordet Institut Bruxelles, Belgium, 1000 Italy Instituto Europeo di Oncologia Milano, Italy, 20141 Spain Hospital Universitario 12 de Octubre Madrid, Spain, 28041 Collapse <<
  NCT01780545	Bladder Cancer ... more >> Urothelial Carcinoma Collapse <<	Phase 2	Completed	-	-
  NCT01780545	-	-	Completed	-	-

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• 参考文献

• [1] Buey RM, Diaz JF, et al. Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity. Chem Biol. 2004 Feb;11(2):225-36.

  [2] Riou JF, Naudin A, Lavelle F. Effects of Taxotere on murine and human tumor cell lines. Biochem Biophys Res Commun. 1992 Aug 31;187(1):164-70.