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Manufacturer:
Pfizer Inc.
Pharmacological Class:
Kinase inhibitor.
Active Ingredient(s):
Axitinib 1mg, 5mg; tabs.
Indication(s):
Treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy.
Pharmacology:
Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations. These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression.
Clinical Trials:
The safety and efficacy of Inlyta were evaluated in an open-label, multicenter Phase 3 study. A total of 723 patients with advanced RCC whose disease had progressed on or after treatment with 1 prior systemic therapy, including sunitinib-, bevacizumab-, temsirolimus-, or cytokine-containing regimens were randomized (1:1) to receive Inlyta(N=361) or sorafenib (N=362). Progression-free survival (PFS) was assessed by a blinded independent central review committee. Other endpoints included objective response rate (ORR) and overall survival (OS).
There was a statistically significant advantage for Inlyta over sorafenib for the endpoint of PFS (6.7 months for Inlyta vs. 4.7 months for sorafenib; HR=0.67 (0.54, 0.81); P<0.0001). There was no statistically significant difference between the arms in OS.
Legal Classification:
Rx
Adults:
Take 12 hours apart. Swallow whole with a glass of water. Initially 5mg twice daily. If tolerated for at least two consecutive weeks with no adverse reactions >Grade 2, normotensive, and not receiving antihypertensives, may increase dose to 7mg twice daily, then 10mg twice daily. May reduce dose from 5mg twice daily to 3mg twice daily, then 2mg twice daily if additional dose reduction required. Concomitant strong CYP3A4/5 inhibitors: avoid; if warranted, decrease Inlyta dose by approximately ½. If strong CYP3A4/5 inhibitor discontinued, return Inlyta
dose (after 3–5 half-lives of the inhibitor) to that used prior to CYP3A4/5 inhibitor initiation. Moderate hepatic impairment: decrease dose by approximately ½.
Children:
Not studied.
Warnings/Precautions:
Control and monitor BP prior to and during therapy; discontinue if severe and persistent hypertension (despite antihypertensive therapy and dose reduction). Risk of thromboembolic events. Untreated brain metastasis, recent active GI bleed: not recommended. Interrupt therapy if bleeding requires medical intervention. GI perforation and fistula formation; monitor. Monitor thyroid, liver function (ALT, AST, bilirubin), and for proteinuria before starting therapy, then periodically. Reduce dose or temporarily interrupt for moderate to severe proteinuria. Risk of
reversible posterior leukoencephalopathy syndrome (permanently discontinue if occurs). Stop treatment at least 24hrs prior to scheduled surgery.
Severe hepatic impairment. End-stage renal disease. Pregnancy (Cat. D); avoid. Use adequate contraception during therapy. Nursing mothers: not recommended.
Interaction(s):
See Adult dose. Avoid strong CYP3A4/5 inhibitors (eg, grapefruit juice, ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole), CYP3A4/5 inducers (eg, rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentin, phenobarbital, St. John’s wort), moderate CYP3A4/5 inducers (eg, bosentan, efavirenz, etravirine, modafinil, nafcillin).
Adverse Reaction(s):
GI upset, hypertension, fatigue, decreased appetite, dysphonia, palmar-plantar erythrodysesthesia (hand-foot) syndrome, weight decreased, asthenia, constipation.
How Supplied:
Tabs 1mg—180; 5mg—60
Last Updated:
3/26/2012
西替尼(Axitinib)2012年1月27日FDA批准上市，用于其它系统治疗无效的晚期肾癌(Renal Cell Carcinoma, RCC)。阿西替尼由Pfizer公司开发，商品名Inlyta。与Pfizer的另一抗癌药物舒尼替尼(Sunitinib)类似，阿西替尼也是多靶点酪氨酸激酶抑制剂，可以抑制血管内皮细胞生长因子受体(Vascular Endothelial Growth Factor Receptor，VEGFR) VEGFR1, VEGFR2, VEGFR3,
血小板衍生生长因子受体(Platelet-derived growth factor receptor, PDGFR), 和c-KIT。
美国初次批准：2012 年
适应证和用途
INLYTA 是一种激酶抑制剂适用于一种既往全身治疗失败后晚期肾细胞癌的治疗。
剂量和给药方法
（1）开始剂量为5 mg口服每天2次。可根据个体安全性和耐受性调整剂量。
（2）约间隔12小时给予INLYTA剂量有或无食物。
（3）INLYTA应与一杯水整片吞服。
（4）如需要强CYP3A4/5抑制剂，减低INLYTA 剂量约半量.
（5）对中度肝受损患者，减低开始剂量约半量。
剂型和规格
1mg和5mg片。
禁忌证
无。
警告和注意事项
（1）曾观察到高血压包括高血压危象。开始INLYTA前应充分控制血压。需要监视和治疗高血压。尽管使用抗高血压药物，对持续高血压减低INLYTA剂量。
（2）曾观察到动脉和静脉血栓事件和可能致死。对这些事件风险增加患者慎用。
（3）曾报道出血事件, 包括致命性事件。尚未在未治疗脑转移或最近活动性胃肠道出血证据患者中研究过INLYTA和在这些患者中不应使用。
（4）曾发生胃肠道穿孔和瘘管，包括死亡。对胃肠道穿孔或瘘管风险患者慎用。
（5）曾报道甲状腺低下症需要甲状腺激素替代。用NLYTA治疗开始前监视甲状腺功能，和自始至终定期。
（6）计划手术前至少24小时停止INLYTA。
（7）曾观察到可逆性后部白质脑病综合征(RPLS)。如发生RPLS体征或症状永久终止INLYTA。
（8）用INLYTA治疗开始前，和自始至终定期监视蛋白尿。对中度至严重蛋白尿，减低剂量或暂时中断用INLYTA治疗。
（9）用INLYTA治疗时曾观察到肝酶升高。用INLYTA治疗开始前和自始至终定期监视ALT，AST和胆红素。
（10）中度肝受损患者如使用INLYTA开始剂量应减低。严重肝受损患者中未曾研究过INLYTA。
（11）当给予妊娠妇女根据其作用机制INLYTA可能致胎儿危害。应忠告生育能力妇女对胎儿潜在危害和当接受INLYTA避免成为妊娠。
不良反应
最常见(≥20%)不良反应是腹泻，高血压，疲乏，食欲减低，恶心，发音障碍，手掌-足底erythrodysesthesia (手-足)综合征，体重减轻，呕吐，乏力，和便秘。
药物相互作用
（1）避免强CYP3A4/5抑制剂。如不可避免，减低INLYTA 剂量。
（2）避免强CYP3A4/5诱导剂。
如何供应/贮存和储置
INLYTA片供应如下：
1 mg片是红色膜衣，椭圆片一侧凹有“Pfizer”和另一侧“1 XNB”；得到80片瓶: NDC 0069-0145-01。
5 mg片是红色膜衣，三角形一侧凹有“Pfizer”和另一侧“5 XNB”；得到60片瓶:: NDC 0069-0151-11.
贮存在20°C至25°C(68°F至77°F)；外出允许15°C至30°C(59°F至86°F)[见USP 控制室温]。
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注：以下产品不同规格和不同价格，购买时以咨询为准！
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产地国家: 美国
原产地英文商品名:
INLYTA 5MG/TAB 60TABS/BOTTLE (Controlled; can only sell to oncology centers and hospitals)
原产地英文药品名:
AXITINIB
中文参考商品译名:
INLYTA 5毫克/片 60片/瓶 (Controlled; can only sell to oncology centers
and hospitals)
中文参考药品译名:
阿西替尼
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER
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产地国家: 美国
原产地英文商品名:
INLYTA 1MG/TAB 180TABS/BOTTLE (Controlled; can only sell to oncology centers and hospitals)
原产地英文药品名:
AXITINIB
中文参考商品译名:
INLYTA 1毫克/片 180片/瓶(Controlled; can only sell to oncology centers
and hospitals)
中文参考药品译名:
阿西替尼
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER
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产地国家: 德国
原产地英文商品名:
INLYTA 5MG/TAB 56TABS/box(Controlled; can only sell to oncology centers and hospitals)
原产地英文药品名:
AXITINIB
中文参考商品译名:
INLYTA 5毫克/片 56片/盒 (Controlled; can only sell to oncology centers
and hospitals)
中文参考药品译名:
阿西替尼
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER
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产地国家: 德国
原产地英文商品名:
INLYTA 1MG/TAB 56TABS/box(Controlled; can only sell to oncology centers and hospitals)
原产地英文药品名:
AXITINIB
中文参考商品译名:
INLYTA 1毫克/片 56片/盒 (Controlled; can only sell to oncology centers
and hospitals)
中文参考药品译名:
阿西替尼
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER |
