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DOCETAXEL
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DOSAGE FORM: Liquid Injection, 20mg/0.5ml, 80mg/2ml, 120mg/3ml.

BIOLOGICAL SIGNIFICANCE

Docetaxel binds to microtubules reversibly with high affinity and has a maximum stoichiometry of 1 mole docetaxel per mole tubulin in microtubules. This binding stabilizes microtubules and prevents depolymerisation from calcium ions, decreased temperature and dilution, preferentially at the plus end of the microtubule. Docetaxel has been found to accumulate to higher concentration in ovarian adenocarcinoma cells than kidney carcinoma cells, which may contribute to the more effective treatment of ovarian cancer by docetaxel. It has also been found to lead to the phosphorylation of oncoprotein bcl-2, which is apoptosis blocking in its oncoprotein form.

CLINICAL USE

The main use of docetaxel is the treatment of a variety of cancers after the failure of anthracycline-based chemotherapy. Some of them are –

Breast Cancer
Non-Small Cell Lung Cancer
Prostate Cancer
Gastric Adenocarcinoma
Head and Neck Cancer

MODE OF ACTION

The cytotoxic activity of docetaxel is exerted by promoting and stabilizing microtubule assembly, while preventing physiological microtubule depolymerisation/disassembly in the absence of GTP. This leads to a significant decrease in free tubulin, needed for microtubule formation and results in inhibition of mitotic cell division between metaphase and anaphase, preventing further cancer cell progeny.

Because microtubules do not disassemble in the presence of docetaxel, they accumulate inside the cell and cause initiation of apoptosis. Apoptosis is also encouraged by the blocking of apoptosis-blocking bcl-2 oncoprotein. The anti-neoplastic activity of docetaxel to is effective against a wide range of known cancer cells, cooperate with other anti-neoplastic agents activity, and have greater cytotoxicity than paclitaxel, possibly due to its more rapid intracellular uptake. The main mode of therapeutic action of docetaxel is the suppression of microtubule dynamic assembly and disassembly, rather than microtubule bundling leading to apoptosis, or the blocking of bcl-2.

STRUCTURE:

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