近日，抗癌药Imbruvica（ibrutinib）获欧盟委员会（EC）批准，用于2种血液癌症：（1）用于复发性或难治性套细胞淋巴瘤（MCL）成人患者的治疗；（2）用于既往接受过至少一种疗法的慢性淋巴细胞白血病（CLL）和携带del17p删除突变或TP53突变且不适合化疗-免疫疗法的CLL成人患者的一线治疗。
Imbruvica的获批，是基于在CLL患者中开展的III期RESONATE（PCYC-1112-CA）研究和Ib/II期研究(PCYC-1102)以及在MCL患者中开展的II期研究（PCYC-1104）的积极数据。
套细胞淋巴瘤（MCL）是一种罕见侵袭性B细胞淋巴瘤，该病难以治疗且预后很差。慢性淋巴细胞白血病（CLL）是一种源于骨髓白血细胞（淋巴细胞）的血癌。染色体异常删除突变del 17p和TP53突变与癌症的恶化和耐药性相关，del 17p删除突变是指17号染色体部分片段丢失，携带该突变的CLL患者被认为预后最差。
Imbruvica（ibrutinib）是一种首创的口服布鲁顿酪氨酸激酶（BTK）抑制剂，通过抑制肿瘤细胞复制和转移需要的布鲁顿酪氨酸激酶（BTK）而起到抗癌的作用。BTK是B细胞受体信号复合体中的一种关键信号分子，在恶性B细胞的生存及扩散中起着重要作用。Imbruvica能够阻断介导恶性B细胞不可控地增殖和扩散的信号通路。
Ibrutinib (Imbruvica®)
WARNINGS
See precautions below.
DESCRIPTION  
IMBRUVICA™ (ibrutinib) capsules, for oral use
Initial U.S. Approval: 2013
Ibrutinib is an inhibitor of Bruton's tyrosine kinase (BTK). It is a white to off-white solid with the empirical formula C25H24N6O2 and a molecular weight 440.50. Ibrutinib is freely soluble in dimethyl sulfoxide, soluble in methanol and practically insoluble in water.
IMBRUVICA (ibrutinib) capsules for oral administration are supplied as white opaque capsules that contain 140 mg ibrutinib as the active ingredient. Each capsule also contains the following inactive ingredients: croscarmellose sodium, magnesium stearate, microcrystalline cellulose, sodium lauryl sulfate. The capsule shell contains gelatin, titanium dioxide and black ink. Each white opaque capsule is marked with "ibr 140 mg" in black ink.
CLINICAL PHARMACOLOGY: 
Mechanism of Action:
Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.  
INDICATIONS AND USAGE:
IMBRUVICA is a kinase inhibitor indicated for the treatment of patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.
This indication is based on overall response rate. An improvement in survival or disease-related symptoms has not been established
CONTRAINDICATIONS 
None.
PRECAUTIONS 
WARNINGS AND PRECAUTIONS
1.Hemorrhage: Monitor for bleeding.
2.Infections: Monitor patients for fever and infections and evaluate promptly.
3.Myelosuppression: Check complete blood counts monthly.
4.Renal Toxicity: Monitor renal function and maintain hydration.
5.Second Primary Malignancies: Other malignancies have occurred in patients, including skin cancers, and other carcinomas.
6.Embryo-Fetal Toxicity: Can cause fetal harm. Advise women of the potential risk to a fetus and to avoid pregnancy while taking the drug
ADVERSE REACTIONS 
ADVERSE REACTIONS
The most common adverse reactions (20%) in patients with MCL were thrombocytopenia, diarrhea, neutropenia, anemia, fatigue, musculoskeletal pain, peripheral edema, upper respiratory tract infection, nausea, bruising, dyspnea, constipation, rash, abdominal pain, vomiting and decreased appetite.
DRUG INTERACTIONS
CYP3A Inhibitors: Avoid co-administration with strong and moderate CYP3A inhibitors. If a moderate CYP3A inhibitor must be used, reduce IMBRUVICA dose .
CYP3A Inducers: Avoid co-administration with strong CYP3A inducers.
USE IN SPECIFIC POPULATIONS
Hepatic Impairment: Avoid use of IMBRUVICA in patients with baseline hepatic impairment.
See PACKAGE INSERT for PATIENT COUNSELING INFORMATION and Medication Guide
DOSAGE AND ADMINISTRATION  
DOSAGE AND ADMINISTRATION:
560mg taken orally once daily (four 140 mg capsules once daily.
Capsules should be taken orally with a glass of water. Do not open, break, or chew the capsules
HOW SUPPLIED 
DOSAGE FORMS AND STRENGTHS
Capsule: 140mg