制造商：
赛诺菲安万特
药理分类：
抗肿瘤药（紫杉烷- antimicrotubule剂）。
活性成分（补）：
Cabazitaxel 60mg/1.5mL;稀释后静脉输注的溶液，含有聚山梨酯80，稀释剂含有乙醇。
指示（补）：
在与强的松联合，激素难治性转移性前列腺癌与多西紫杉醇治疗以前含方案。
药理作用：
Cabazitaxel是一种半合成紫杉烷类抗肿瘤剂从红豆杉针叶中提取的准备。 Cabazitaxel是一种抑制剂，微管微管蛋白结合，促进成微管，同时抑制其组装拆卸。这导致了微管稳定，这在有丝分裂间期细胞功能和抑制的结果。它已被证明在肿瘤模型的活动，多西紫杉醇的化疗不敏感，以及在那些被多西紫杉醇敏感。
Cabazitaxel是由肝脏代谢广泛，它不适合在患者使用肝功能受损是由于cabazitaxel水平和毒性可能增加推荐。
临床试验：
Cabazitaxel是比较多中心米托蒽醌，随机，开放标签研究中755例激素难治性转移性前列腺以前用多西他赛含方案治疗癌症。患者随机接受（最多10次10毫克强的松25mg/m2，每3个星期每天）要么cabazitaxel或米托蒽醌（12mg/m2，每3个周期长达10个星期每天10毫克强的松）。与肝功能损害，高血压和某些心脏疾病患者被排除在审判。
在意向性治疗分析，为cabazitaxel组中位生存时间为15.1个月，而12.7米托个月，在cabazitaxel 61.9％的患者死亡组由30个月相比，74％的米托蒽醌胳膊。研究者评估的肿瘤反应较高的cabazitaxel组（14.4％）相比，米托蒽醌组（4.4％）。
法律分类：
接收
成人：
预处理与IV抗组织胺，类固醇和H2受体阻滞剂30分钟后各剂量（见文献）和止吐（静脉或口服如需要）。 25mg/m2由四超过1小时，每3周治疗期间口服强的松10mg/day，输液。如果不治疗中性粒细胞计数≤1500 cell/mm3之。长期≥3级中性粒细胞减少（“1周），发热性中性粒细胞减少，等级≥3腹泻：延误治疗和/或降低剂量20mg/m2（见文献）。如果反应后，停止在20mg/m2剂量存在。
儿童：
不推荐。
禁忌（补）：
中性粒细胞计数≤基线1500 cell/mm3之。过敏聚山梨酯80。
警告/注意事项：
央行是否在第一个周期以后每次周期前一周。中性粒细胞减少并发症的风险增加，考虑的G - CSF治疗。肝功能不全：不推荐。严重肾功能损害（肌酐清除率<30mL/min）或终末期肾病。老人（易感性增加不良反应）;密切监测。妊娠（Cat.D，避免）。哺乳母亲：不推荐。
互动（补）：
避免强烈的CYP3A4抑制剂（如酮康唑，克拉霉素，atazanavir，奈法唑酮，奈非那韦，利托那韦，沙奎那韦，伏立康唑）（会增强cabazitaxel），与CYP3A4抑制剂适度谨慎。避免强烈的CYP3A4的诱导剂（如苯妥英，卡马西平，利福平，苯巴比妥）（可拮抗cabazitaxel）。避免圣约翰草。
不良反应（补）：
骨髓抑制（尤其是中性粒细胞减少，贫血，白细胞减少，血小板减少），发热性中性粒细胞减少，胃肠不适（尤其是腹泻，可致命），肾功能衰竭，疲劳，便秘，乏力，腹痛，血尿，腰痛，食欲减退，周边神经病变，发热，呼吸困难，味觉障碍，咳嗽，关节痛，脱发，过敏反应（如皮疹，低血压，支气管痉挛）。
如何提供：
套件（单用小瓶+稀释剂）-1
最后更新：
2010年9月2日
Manufacturer:
Sanofi-aventis
Pharmacological Class:
Antineoplastic (taxane antimicrotubule agent).
Active Ingredient(s):
Cabazitaxel 60mg/1.5mL; soln for IV infusion after dilution; contains polysorbate 80, diluent contains ethanol.
Indication(s):
In combination with prednisone, hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing regimen.
Pharmacology:
Cabazitaxel is a semisynthetic taxane antineoplastic agent prepared from an extract of yew needles. Cabazitaxel is a microtubule inhibitor that binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly. This leads to the stabilization of microtubules, which results in the inhibition of mitotic and interphase cellular functions. It has been shown to have activity in tumor models that were insensitive to docetaxel chemotherapy as well as in those that were docetaxel-sensitive.
Cabazitaxel is extensively metabolized by the liver, and it is not recommended for use in patients with impaired hepatic function due to a probable increase in cabazitaxel levels and toxicity.
Clinical Trials:
Cabazitaxel was compared to mitoxantrone in a multicenter, randomized, open-label study in 755 patients with hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing regimen. Patients were randomized to receive either cabazitaxel (25mg/m2 every 3 weeks for up to 10 cycles with prednisone 10mg daily) or mitoxantrone (12mg/m2 every 3 weeks for up to 10 cycles with prednisone 10mg daily). Patients with hepatic impairment, hypertension, and certain cardiac conditions were excluded from the trial.
In an intent-to-treat analysis, the median survival time for the cabazitaxel group was 15.1 months, compared to 12.7 months for mitoxantrone; 61.9% of the patients in the cabazitaxel group died by the 30th month, compared to 74% in the mitoxantrone arm. The investigator-assessed tumor response was higher in the cabazitaxel group (14.4%) compared to the mitoxantrone group (4.4%).
Legal Classification:
Rx
Adults:
Pretreat with IV antihistamine, corticosteroid, and H2 blocker 30 min before each dose (see literature) and with antiemetic (IV or oral as needed). 25mg/m2 by IV infusion over 1 hour every 3 weeks, with oral prednisone 10mg/day during treatment. Do not treat if neutrophil count ≤1,500 cells/mm3. Prolonged grade ≥3 neutropenia (>1 week), febrile neutropenia, grade ≥3 diarrhea: delay treatment and/or reduce dose to 20mg/m2 (see literature). Discontinue if reactions persist after dosing at 20mg/m2.
Children:
Not recommended.
Contraindication(s):
Baseline neutrophil count ≤1,500cells/mm3. Allergy to polysorbate 80.
Warnings/Precautions:
Do CBC weekly in 1st cycle and before each subsequent cycle. Increased risk of neutropenia complications; consider G-CSF prophylaxis. Hepatic impairment: not recommended. Severe renal impairment (CrCl <30mL/min) or ESRD. Elderly (increased susceptibility to adverse reactions); monitor closely. Pregnancy (Cat.D; avoid). Nursing mothers: not recommended.
Interaction(s):
Avoid strong CYP3A4 inhibitors (eg, ketoconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, saquinavir, voriconazole) (may potentiate cabazitaxel); caution with moderate CYP3A4 inhibitors. Avoid strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin, phenobarbital) (may antagonize cabazitaxel). Avoid St. John’s Wort.
Adverse Reaction(s):
Bone marrow suppression (esp. neutropenia, anemia, leukopenia, thrombocytopenia), febrile neutropenia, GI upset (esp. diarrhea, may be fatal), renal failure, fatigue, constipation, asthenia, abdominal pain, hematuria, back pain, anorexia, peripheral neuropathy, pyrexia, dyspnea, dysgeusia, cough, arthralgia, alopecia, hypersensitivity reactions (eg, rash, hypotension, bronchospasm).
How Supplied:
Kit (single-use vial + diluent)—1