Antineoplastic Agent, Antimicrotubular; Antineoplastic Agent, Taxane Derivative
FDA has approved for the treatment of breast cancer, non-small cell lung cancer (NSCLC), castration-resistant prostate cancer, gastric cancer, and squamous cell cancer of the head and neck
藥理
Docetaxel promotes the assembly of microtubules from tubulin dimers, and inhibits the depolymerization of tubulin which stabilizes microtubules in the cell. This results in inhibition of DNA, RNA, and protein synthesis. Most activity occurs during the M phase of the cell cycle.
藥動學
Absorption
1. Time to peak:IV, 1 to 2 hours Distribution
1. Vdss (mean): 113 L.
2. Protein binding: ~94% to 97% Metabolism:Hepatic; oxidation via CYP3A4 to metabolites. Excretion:Feces (~75%, <8% as unchanged drug); urine (~6%) Pharmakodynamics
1. Half-life Elimination: 116 hours
2. Clearance:18 L/hour/m2.
禁忌症
History of severe hypersensitivity to docetaxel or any component of the formulation; severe hypersensitivity to other medications containing polysorbate 80; neutrophil count <1,500/mm3.
懷孕分類
D
哺乳分類
It is not known if docetaxel is present in breast milk.Due to the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended by the manufacturer during treatment and for 1 week after the last docetaxel dose.
副作用
Common(>10%):Neutropenia、Infection、Localized erythema、Diarrhea、nausea、Central nervous system toxicity、Asthenia
Severe fluid retention (edema) occurs in 6.5% of patients receiving docetaxel
劑量和給藥方法
適應症:
1.Breast cancer:60 to 100 mg/m2 every 3 weeks (as a single agent) until disease progression or unacceptable toxicity for at least 6 cycles (Harvey 2006) or 100 mg/m2 every 3 weeks (as a single agent) for a maximum of 7 or 10 cycles
2. Gastric adenocarcinoma : IV: 75 mg/m2 every 3 weeks (in combination with cisplatin and fluorouracil) until disease progression or unacceptable toxicity
3.Head and neck cancer: IV: 75 mg/m2 every 3 weeks (in combination with cisplatin and fluorouracil) for 3 or 4 cycles
4.Non small cell lung cancer: IV: 75 mg/m2 every 3 weeks (as a single agent) for at least 6 cycles or until disease progression or unacceptable toxicity.
5.Prostate cancer: IV: 75 mg/m2 every 3 weeks.
小兒調整劑量
腎功能調整劑量
肝功能調整劑量
安定性
1.After dilution, docetaxel may be stored at 2 to 25 degrees C for up to 6 hours (including the 1 hour for IV administration).
2.Physical and chemical in-use stability of the infusion solution has also been demonstrated in non-PVC bags for up to 48 hours when stored between 2 and 8 degrees C .