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QuickView for Docetaxel (compound)

Name: docetaxel
PubChem Compound ID: 10417939
Molecular formula: C43H53NO14
Molecular weight: 809.872 g/mol
Name: docetaxel
Name (isomeric): DB01248
Drug Type: small molecule
Docetaxel, Trihydrate; TXL; Docetaxel anhydrous
Brand: Taxotere
Category: Antimalarials, Radiation-Sensitizing Agents, Antineoplastic Agents, Antineoplastic Agents, Phytogenic
CAS number: 114977-28-5
Indication: For the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy. Also used as a single agent in the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of prior platinum-based chemotherapy. Lastly, for use, in combination with prednisone, in the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer.
Docetaxel is a taxoid antineoplastic agent. It promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. In additi...
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Mechanism of Action:
Docetaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, docetaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, docet...
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Protein binding: About 94% protein bound, mainly to a1-acid glycoprotein, albumin, and lipoproteins.
Biotransformation: Hepatic. In vitro drug interaction studies revealed that docetaxel is metabolized by the CYP3A4 isoenzyme (1 major, 3 minor metabolites).
Route of elimination: Docetaxel was eliminated in both the urine and feces following oxidative metabolism of the tert-butyl ester group, but fecal excretion was the main elimination route. Within 7 days, urinary and fecal excretion accounted for approximately 6% and 75% of the administered radioactivity, respectively.
Half Life: Dose-dependent. Doses of 70 mg per square meter of body surface area (mg/m 2 ) or higher produce a triphasic elimination profile. With lower doses, assay limitations precluded detection of the terminal elimination phase. Alpha (distribution) 4 minutes. Beta 36 minutes. Gamma (terminal) 11.1 hours.
Clearance: 21 L/h/m2 [Cancer patients after IV administration of 20–115 mg/m2]
Toxicity: Oral LD50 in rat is >2000 mg/kg. Anticipated complications of overdosage include: bone marrow suppression, peripheral neurotoxicity, and mucositis. In two reports of overdose, one patient received 150 mg/m2 and the other received 200 mg/m2 as 1-hour infusions. Both patients experienced severe neutropenia, mild asthenia, cutaneous reactions, and mild paresthesia, and recovered without incident.
Affected organisms: Humans and other mammals
Drug interaction:
Testosterone PropionateTestosterone propionate may increase the serum levels and toxicity of docetaxel.
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
JosamycinJosamycin may increase the serum levels and toxicity of docetaxel.
MidazolamMidazolam may increase the serum levels and toxicity of docetaxel.
QuinupristinThis combination presents an increased risk of toxicity.
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