148408-66-6 Usage
Pharmacology
Docetaxel principally exerts its cytotoxic activity by promoting and stabilising microtubule assembly while simultaneously preventing microtubule depolymerisation. This results in inhibition of normal cell division. In vitro and in vivo, docetaxel has antineoplastic activity against a wide range of cancer cells, demonstrates synergistic activity with several antineoplastic agents and often has greater cytotoxic activity against human breast cancer cell lines than paclitaxel. Docetaxel, binds to and stabilizes tubulin, which prevents physiological microtubule depolymerization/disassembly and results in cell-cycle arrest at the G2/M phase and cell death. This agent also is known to inhibit the anti-apoptotic gene Bcl2 and to encourage the expression of p27, a cell-cycle inhibitor, and further pro-angiogenic factors such as vascular endothelial growth factor (VEGF). Docetaxel is mainly metabolized in the liver by the cytochrome P450 CYP3A4 and CYP3A5 subfamilies of isoenzymes, and its clearance has been shown to be related to body surface area and hepatic enzyme and alpha1 acid glycoprotein plasma levels.
Tolerability
The tolerability of docetaxel in comparative clinical trials was generally acceptable. Severe neutropenia affects most docetaxel recipients, with febrile neutropenia occurring in approximately one-eighth of patients. Dose-cumulative severe fluid retention was reported in docetaxel recipients, despite premedication with prophylactic corticosteroids. Other adverse events include asthenia, stomatitis, infections, neurosensory, cutaneous or gastrointestinal events, nail changes, severe fever in the absence of infection, myalgia and hypersensitivity reactions.
Chemical Properties
White Crystalline Powder
Uses
Different sources of media describe the Uses of 148408-66-6 differently. You can refer to the following data:
1. An antineoplastic. An antimitotic agent that promotes the assembly of microtublules and inhibits their depolymerization to free tubulin
2. Docetaxel Trihydrate is an anti-cancer drugs; Semisynthetic analog of the taxane paclitaxel.
Definition
ChEBI: The trihydrate form of docetaxel. It is used for the treatment of breast, ovarian, and non-small cell lung cancer, and with prednisone or prednisolone in hormone-refractory metastatic prostate cancer.
Brand name
Taxotere (Sanofi Aventis).
Check Digit Verification of cas no
The CAS Registry Mumber 148408-66-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,8,4,0 and 8 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 148408-66:
(8*1)+(7*4)+(6*8)+(5*4)+(4*0)+(3*8)+(2*6)+(1*6)=146
146 % 10 = 6
So 148408-66-6 is a valid CAS Registry Number.
148408-66-6Relevant articles and documents
DOCETAXEL PROCESS AND POLYMORPHS
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Page/Page column 35, (2009/03/07)
Processes for preparing substantially pure docetaxel, new crystalline forms of docetaxel and processes for preparation thereof, processes for preparing docetaxel trihydrate, and pharmaceutical compositions comprising docetaxel.
THE PROCESS FOR THE PREPARATION OF DOCETAXEL TRIHYDRATE
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Page/Page column 3, (2008/06/13)
This invention is under the field of medicine synthesization technique that announces a method to prepare the compound of Docetaxel trihydrate. The method uses the mixture of acetone and water, which provides the product with good stability, less experime
PROCESS FOR PREPARATION OF PACLITAXEL TRIHYDRATE AND DOCETAXEL TRIHYDRATE
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Page 2, (2008/06/13)
A process for the preparation of paclitaxel trihydrate and doctaxel trihydrate comprising (a) treating taxane selected from paclitaxel and docetaxel with a mixture of alkane and chlorinated alkane to obtain a crude product of 65-75% assay, (b) dissolving
