Ixabepilone(Ixempra,伊沙匹隆注射液) -乳腺癌化疗药物
Ixabepilone for treating breast cancer
Company:
Bristol-Myers Squibb
Pharmacologic class:
Antineoplastic (epothilone microtubule inhibitor)
Active ingredient:
Ixabepilone 15mg/vial, 45mg/vial; pwd; for IV infusion after constitution and dilution; diluent contains alcohol, polyoxyethylated castor oil.
Indication:
Metastatic or locally advanced breast cancer: In combination with capecitabine after failure of an anthracycline and a taxane; and as monotherapy after failure of an anthracycline, a taxane, and capecitabine.
Pharmacology:
Ixabepilone is a semi-synthetic analog of epothilone B, a microtubule inhibitor. It binds to microtubules, thus disrupting cell division on the nuclear level. It blocks cells from dividing in the mitotic phase of the cell division cycle, causing cell death.
Clinical trials:
A trial involving 752 patients with metastatic or locally advanced breast cancer was conducted to assess the efficacy and safety of ixabepilone in combination with capecitabine compared to capecitabine monotherapy. The primary endpoint was progression-free survival (PFS) (time from randomization to radiologic progression, clinical progression of measurable skin lesions or death). Ixabepilone in combination with capecitabine resulted in statistically significant improvement in PFS compared to capecitabine alone. The median PFS was 5.7 months for the combination compared to 4.1 months for capecitabine monotherapy.
A study in 126 women with metastatic or locally advanced breast cancer whose tumors had recurred or had progressed ≥2 chemotherapy regimens was conducted to evaluate the use of ixabepilone as monotherapy. The objective tumor response rates were 12.4% (independent radiologic review assessment) and 18.3% (investigator assessment).
Adults:
Pretreat with both H1 and H2 blockers 1 hr before infusion; and with steroid if previous hypersensitivity reaction occurred. 40mg/m2 by IV infusion over 3 hrs, once every 3 weeks. Use max body surface area (BSA) of 2.2m2 to calculate dose if BSA >2.2m2. Moderate hepatic impairment (as monotherapy): initially 20mg/m2 per dose; max 30mg/m2 per dose (see literature). Neuropathy, myelosuppression, concomitant CYP3A4 inhibitors: reduce dose (see literature).
Children:
Not recommended.
Contraindications:
Baseline neutrophils <1500cells/mm3 or platelets <100,000/mm3. AST or ALT >2.5xULN or bilirubin >1xULN (in combination with capecitabine).
Precautions:
Monitor liver function at baseline and periodically. Hepatic impairment (ALT or AST >10xULN or bilirubin >3xULN: not recommended; ALT or AST >5xULN: limited data, use caution). Diabetes. Neuropathy. Cardiac disease (discontinue if cardiac ischemia or cardiac dysfunction occurs). Monitor for neuropathy, neutropenia. Pregnancy (Cat.D), nursing mothers: not recommended.
Interactions:
Potentiated by strong CYP3A4 inhibitors; avoid (eg, azole antifungals, protease inhibitors, certain macrolides, nefazodone, grapefruit juice). Antagonized by strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin, phenobarbital). Avoid St. John抯 wort.
Adverse reactions:
Peripheral sensory neuropathy, fatigue, asthenia, myalgia, arthralgia, alopecia, GI upset, stomatitis, mucositis, musculoskeletal pain, palmar-plantar erythrody-sesthesia syndrome, anorexia, abdominal pain, nail disorder; myelosuppression (neutropenia, leukopenia, anemia, thrombocytopenia); hypersensitivity reactions; others.
How supplied:
Kit? vial (w. diluent)
用于治疗乳腺癌的xabepilone(Ixempra Kit)
公司名称：
施贵宝
药物类：
抗肿瘤药（埃博霉素微管抑制剂）
活性成分：
，45mg/vial ixabepilone 15mg/vial; PWD;静脉滴注后，宪法和稀释，稀释剂含有酒精，聚氧乙烯蓖麻油。
适应症：
转移性或局部晚期乳腺癌：与capecitabine合并失败后一种蒽环类和紫杉类和蒽环类，紫杉类，卡培他滨的失败后的单一。
药理作用：
ixabepilone是一种半合成埃博霉素B，一个微管抑制剂的模拟。微管结合，从而干扰细胞分裂，核水平。它可以阻止细胞在有丝分裂的细胞分裂周期阶段划分，造成细胞死亡。
临床试验：
一个试验，涉及752转移性或局部晚期乳腺癌患者进行了评估结合的疗效和安全ixabepilone与卡培他滨卡培他滨单药治疗相比。主要终点是无进展生存（PFS）（时间从随机影像学的进展，衡量的皮肤损伤或死亡的临床进展）。与capecitabine合并ixabepilone导致统计学意义PFS的改善相比，卡培他滨单。中位PFS为5.7个月的组合相比，卡培他滨单药治疗4.1个月。
，女126例，转移性或局部晚期乳腺癌的肿瘤已复发或已取得进展≥2化疗进行评估的ixabepilone的使用作为单一的研究。肿瘤客观缓解率分别为12.4％（独立放射学审查评估）和18.3％（调查评估）。
成人：
与H1和H2受体阻滞剂1小时输液前的预处理;与类固醇，如果以前的过敏反应发生。 40mg/m2静脉滴注超过3小时，每3周一次。使用最大的2.2平方米体表面积（BSA）计算剂量，如果牛血清白蛋白>2.2平方米。中度肝功能不全（单一）：最初每剂量20mg/m2;最大每剂量30mg/m2（见文献）。神经病变，骨髓抑制，伴随CYP3A4抑制剂：减少剂量（见文献）。
儿童：
不推荐使用。
禁忌症：
基线嗜中性粒细胞<1500cells/mm3或血小板<100,000 /立方毫米。 AST或ALT> 2.5xULN。或胆红素> 1xULN（卡培他滨的组合）。
注意事项：
在基线和定期监测肝功能。肝功能不全（ALT或AST> 10xULN或胆红素> 3xULN：不推荐; ALT或AST> 5xULN：数据有限的情况下，谨慎使用）。糖尿病。神经病。心脏病（停止，如果发生心肌缺血或心功能不全）。监测病变，中性粒细胞。 （Cat.D）怀孕，哺乳母亲：不推荐。
相互作用：
Potentiated强CYP3A4抑制剂;避免（如唑类抗真菌药物，蛋白酶抑制剂，某些大环内酯类抗生素，奈法唑酮，葡萄柚汁）。拮抗强CYP3A4诱导剂（如苯妥英钠，卡马西平，利福平，巴比妥）。避免圣约翰抯麦汁。
不良反应：
周边感觉神经病变，疲劳，乏力，肌痛，关节痛，脱发，胃肠不适，口腔炎，黏膜炎，肌肉骨骼疼痛，手掌足底erythrody sesthesia综合征，厌食，腹痛，指甲障碍;骨髓抑制（白细胞减少，白细胞减少，贫血，血小板减少）过敏反应等。
如何提供：
套件？瓶（W.稀释剂）
IXEMPRA INJ 15MG KIT
IXEMPRA INJ 45MG KIT
