近日,突破性抗癌药Imbruvica(ibrutinib)获欧盟批准，用于既往已接受过至少一次治疗的Waldenstrom巨球蛋白血症(WM)成人患者，以及慢性淋巴细胞白血病的不适合化学-免疫疗法的WM成人患者的一线治疗。
最新批准日期：2016年3月  公司：Janssen Biotech, Inc.
IMBRUVICA®（依鲁替尼 ibrutinib）胶囊，供口服使用
最初美国批准：2013
目前的主要变化
适应证和用途   3/2016
警告和注意事项   3/2016
药物过量   3/2016
作用机理
Ibrutinib是BTK的小分子抑制剂。Ibrutinib形成与BTK活性位点的半胱氨酸残基形成共价键，从而抑制BTK的酶活性。BTK是B细胞抗原受体（BCR）和细胞因子受体途径的信号传导分子。BTK在通过必要的B细胞贩卖，趋化和粘附途径的激活的B细胞表面受体的结果的信号的作用。非临床研究显示，ibrutinib在体外抑制体内恶性B细胞增殖和存活以及细胞迁移和基板的粘合性。
适应症和用法
IMBRUVICA为患者的治疗所示的激酶抑制剂：
谁收到至少一个前治疗的套细胞淋巴瘤（MCL）。
加速得到批准的基础上整体回应率这一指标。这个指示继续批准可不经确证试验的临床效果验证队伍。
慢性淋巴细胞白血病（CLL）。
慢性淋巴细胞白血病17p缺失。
华氏巨球蛋白血症（WM）。
用法用量
MCL：560毫克，每天一次口服（4粒 140毫克胶囊，每天一次）。
CLL和WM：420毫克，每天一次口服（三级140毫克胶囊，每天一次）。
胶囊应口服一杯水服用。不要打开，休息，或咀嚼胶囊。
剂型和规格
胶囊：140毫克
禁忌症
没有
警告和注意事项
出血：监测出血和管理。
感染：监测患者发热和感染，及时评估和治疗。
血细胞减少：检查全血细胞计数每月。
心房颤动：监测房颤和管理。
高血压：监测血压和治疗。
第二原发恶性肿瘤：其它恶性肿瘤发生在患者，包括皮肤癌和其他癌。
肿瘤溶解综合征（TLS）：评估基准风险，并采取预防措施。监测和治疗为TLS。
胚胎 - 胎儿毒性：可引起胎儿造成伤害。指教的潜在风险妇女胎儿和避免怀孕同时服用的药物和1个月的治疗停止之后。建议男士以避免在同一时间内抚养一个被孩子。
不良反应
最常见的不良反应（≥20％）患者B细胞恶性肿瘤（MCL，CLL，WM）为血小板减少症，腹泻，贫血，白细胞减少，肌肉骨骼疼痛，疲劳，青紫，恶心，皮疹和上呼吸道感染。
药物相互作用
CYP3A抑制剂：避免联合用药具有较强的和中度CYP3A抑制剂。如果必须使用适度CYP3A抑制剂，降低IMBRUVICA剂量。
CYP3A诱导：避免联合用药具有较强的CYP3A诱导。
特殊人群中使用
肝损伤：避免在患者使用IMBRUVICA的中度或重度基线肝功能损害。在轻度损伤，减少IMBRUVICA剂量。
包装规格/储存与处理
140毫克：每瓶90粒
140毫克：每瓶120粒
瓶子储存在室温20°C至25°C（68°F至77°F）。游览允许15°C至30°C（59°F至86°F）之间。在保留原包装，直到配药。

IMBRUVICA®
Generic Name:Ibrutinib
Trade Name:IMBRUVICA®
For which conditions is this drug approved?IMBRUVICA is indicated for treatment of mantle cell lymphoma (MCL) for chronic lymphocytic leukemia (CLL), both in patients who have received at least one prior therapy.
What is the mechanism of action? IMBRUVICA is a tyrosine kinase inhibitor. These drugs work by blocking the action of enzymes called tyrosine kinases, which are involved in many cell functions, including cell signaling, growth, and division. These enzymes may be too active or found at high levels in some types of cancer cells and blocking them may help keep cancer cells from growing. Specifically, IMBRUVICA blocks the action of a kinase known as Bruton’s tyrosine kinase, orBTK.
How is IMBRUVICA typically given (administered)? IMBRUVICA is given once a day orally at approximately the same time each day. The capsules must be swallowed whole with water and never opened, broken, or chewed
How are patients typically monitored?Before taking IMBRUVICA, discuss any medical conditions withyour healthcare provider. This includes: a recent or planned surgery or dental procedure, bleeding problems, liver problems, if you are pregnant or plan to become pregnant, are breast feeding or plan to breast feed. IMBRUVICA can harm an unborn baby, so women should not become pregnant while taking this drug. Patients taking IMBRUVICA should be monitored for bleeding, fever and infection, kidney problems, and secondary primary cancers. Blood counts should be taken monthly.
What are the common (occur in 20% or more of patients) side effects of treatment with IMBRUVICA for patients with MCL?
Thrombocytopenia (lower-than-normal number of platelets in the blood)
Diarrhea
Neutropenia (lower-than-normal number of neutrophils, a type of white blood cell)
Anemia
Fatigue
Musculoskeletal pain
Peripheral edema
Upper respiratory tract infection
Nausea
Bruising
Dyspnea (difficult, painful breathing or shortness of breath)
Constipation
Rash
Abdominal pain
Vomiting
Decreased appetite What are the common (occur in 20% or more of patients) side effects of treatment with IMBRUVICA for patients with CLL?
Thrombocytopenia (lower-than-normal number of platelets in the blood)
Diarrhea
Bruising
Neutropenia (lower-than-normal number of neutrophils, a type of white blood cell)
Anemia
Upper respiratory tract infection
Fatigue
Musculoskeletal pain
Rash
Fever
Constipation
Peripheral edema
Joint pain
Nausea
Stomatitis (inflammation or irritation of the mucous membranes in the mouth)
Sinus infection
Dizziness This is not a complete list of side effects. Some patients may experience other side effects that are not listed here. Patients may wish to discuss with their physician the other less common side effects of this drug, some of which may be serious.
Some side effects may require medical attention. Other side effects do not require medical attention and may go away during treatment. Patients should check with their physician about any side effects that continue or are bothersome.
What can patients do to help alleviate or prevent discomfort and side effects?
Take IMBRUVICA exactly as your healthcare provider tells you to take it (once daily and swallowed whole with water) and take it at about the same time each day. If you miss a dose of IMBRUVICA, take it as soon as you remember on the same day, then take your next dose at your regular time the next day. Do not take two doses of IMBRUVICA on the same day to make up for a missed dose. Tell your healthcare provider about all the medicines you take, including prescription and over­-the-counter medicines, vitamins, and herbal supplements. Certain other medicines may affect how IMBRUVICA works and can cause side effects.
Are there any special precautions patients should be aware of before starting treatment?
You should not drink grapefruit juice, eat grapefruit, or eat Seville oranges (often used in marmalades) while you are taking IMBRUVICA. These products may increase the amount of IMBRUVICA in your blood.
When should patients notify their physician?
Tell your doctor if you experience any side effects that bother you or don’t go away. This includes persistent diarrhea and signs of bleeding, such as blood in stools or urine and prolonged or uncontrolled bleeding.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0dfd0279-ff17-4ea9-89be-9803c71bab44