药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201892520375615.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分CABOMETYX处方资料(仅供参考)
CABOMETYX™(卡赞替尼[cabozantinib])片,为口服使用
初始批准:2012 欧洲批准:2016年9月16日
作用机制
体外生化和/或细胞学分析曽显示卡赞替尼抑制MET,VEGFR-1,-2和-3,AXL,RET,ROS1,TYRO3,MER,KIT,TRKB,FLT-3,和TIE-2酪氨酸激酶的活性。这些受体酪氨酸激酶是涉及正常细胞学功能和病理学过程两个方面例如肿瘤发生,转移,肿瘤血管生成,药物抗性,和肿瘤慰环境的维持。
适应证和用途
CABOMETYX是一个激酶抑制剂适用为有晚期肾细胞癌(RCC)曽接受以前抗血管生成治疗患者的治疗。
剂量和给药方法
⑴ 推荐剂量:60mg口服,每天1次。
⑵ 指导患者服用CABOMETYX前和后至少1小时不要吃共至少2小时。
⑶ 不要用卡赞替尼胶囊替代CABOMETYX片。
剂型和规格
20mg,40mg,和60mg片。
禁忌证
无。
警告和注意事项
⑴ 出血:如最近严重出血病史不要给予CABOMETYX。
⑵ GI穿孔和瘘管:监视症状。对不能适当地处理或穿孔的瘘管终止。
⑶ 血栓性事件:对心肌梗死,脑梗塞,或其他严重动脉血栓栓塞事件终止CABOMETYX。
⑷高血压和高血压危象:定期地监视血压。对不能用抗高血压治疗控制高血压危象或严重高血压终止CABOMETYX。
⑸ 腹泻:可能是严重。立即中断CABOMETYX治疗直至腹泻解决或减轻至1级。推荐标准抗治疗。
⑹ 掌跖红感觉迟钝综合征(PPES):中断CABOMETYX治疗直至PPES解决或减轻至1级。
⑺ 可逆性后部白质脑病综合征(RPLS):终止CABOMETYX。
⑻ 胚胎-胎儿毒性:可致胎儿危害。忠告生殖潜能女性对胎儿潜在风险和使用有效避孕。
不良反应
最常报道的(≥ 25%)不良反应为:腹泻,疲乏,恶心,食欲减退,掌跖红感觉迟钝综合征(PPES),高血压,呕吐,体重减低,和便秘。
药物相互作用
强CYP3A4抑制剂:减低CABOMETYX剂量。
特殊人群中使用
⑴ 轻度至中度肝受损:减低CABOMETYX剂量。
⑵ 哺乳:当服用CABOMETYX时忠告不要哺乳喂养。
生产厂家:易普森公司 Ipsen Pharma
2016年2月29日,Exelixis和Ipsen联合宣布了一项独家许可协议,用于商业化和进一步开发美国,加拿大和日本以外的cabozantinib。
CABOMETYXTM (cabozantinib) tablets for oral use
Initial Approval: 2012 European Approval: September 16, 2016
Action mechanism
In vitro biochemical and/or cytological analysis showed that cazanidatin inhibits MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3, and TIE -2 tyrosine kinase activity. These receptor tyrosine kinases are involved in both normal cytological and pathological processes such as tumorigenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor comfort environment.
Indications and Uses
CABOMETYX is a kinase inhibitor suitable for the treatment of patients with advanced renal cell carcinoma (RCC) who have received previous anti-angiogenic therapy.
Dose and method of administration
(1) Recommended dose: 60mg orally, once a day.
(2) Instruct patients to take at least 2 hours before and after taking CABOMETYX for at least 1 hour.
(3) Do not replace CABOMETYX tablets with cazantinib capsules.
Formulations and specifications
20 mg, 40 mg, and 60 mg tablets.
Contraindications
no.
Warnings and Precautions
(1) Bleeding: Do not give CABOMETYX a history of severe bleeding.
(2) GI perforation and fistula: monitor symptoms. The fistula that is not properly treated or perforated is terminated.
(3) Thrombotic events: CABOMETYX is terminated for myocardial infarction, cerebral infarction, or other severe arterial thromboembolic events.
(4) Hypertension and hypertensive crisis: Regularly monitor blood pressure. CABOMETYX can be terminated by not being able to control hypertensive crisis or severe hypertension with antihypertensive therapy.
(5) Diarrhea: May be severe. Immediately discontinue CABOMETYX treatment until diarrhea is resolved or reduced to level 1. Recommended standard anti-treatment.
(6) Palmoplantar Red Syndrome Syndrome (PPES): discontinue CABOMETYX treatment until PPES resolves or reduces to grade 1.
(7) Reversible posterior leukoencephalopathy syndrome (RPLS): termination of CABOMETYX.
(8) Embryo-fetal toxicity: can cause fetal harm. Advise women with reproductive potential on potential risks to the fetus and use effective contraception.
Adverse reactions
The most frequently reported (≥ 25%) adverse reactions were: diarrhea, fatigue, nausea, loss of appetite, palmoplantar redness syndrome (PPES), hypertension, vomiting, weight loss, and constipation.
Drug interaction
Strong CYP3A4 inhibitor: Reduce the CABOMETYX dose.
Use in special people
(1) Mild to moderate liver damage: Reduce the CABOMETYX dose.
(2) Breastfeeding: Do not breastfeed when taking CABOMETYX.
Manufacturer: Ipsen Pharma
February 29, 2016, Exelixis and Ipsen jointly announced an exclusive licensing agreement for the commercialization and further development of cabozantinib indications outside of the United States, Canada and Japan.
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