014年2月13日，强生（JNJ）和Pharmacyclics公司2月12日宣布，抗癌药Imbruvica（ibrutinib胶囊）获FDA批准，用于既往接受过至少一次治疗的慢性淋巴细胞白血病（CLL）患者的治疗。Imbruvica已于2013年11月获FDA批准，用于既往接受过至少一次来那度胺或其他药物治疗的套细胞淋巴瘤（MCL）患者的治疗。这2个适应症的获批，均基于整体缓解率（ORR）数据，该药对存活或疾病相关症状改善的数据尚未建立。
Imbruvica是首个每日一次、单一制剂、口服布鲁顿酪氨酸激酶（BTK）抑制剂，由强生和Pharmacyclics公司联合开发和商业化。此前，Imbruvica治疗CLL和MCL适应症均已授予优先审查资格，并根据FDA的加速批准程序批准。同时，Imbruvica也是FDA授予突破性疗法认定并获批的首批药物之一。
突破性疗法称号是2012年FDA安全和创新法案中制定的部分内容，目的是帮助加快用于严重致命疾病的潜在新药的开发进度，这些药物的临床前研究就已显示比现有的治疗药物在一项或多项临床指标上具有明显改进。
慢性淋巴细胞白血病（Chronic Lymphocytic Leukemia，CLL）是一种淋巴细胞血液癌症，在美国，CLL是一种罕见病。据估计，每年有1.6万人确诊为CLL，有近4600人不幸死于CLL。
Imbruvica是布鲁顿酪氨酸激酶（BTK）抑制剂，通过阻断BTK抑制肿瘤细胞的复制和转移，从而起到抗癌作用。
完整资料附件：
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0dfd0279-ff17-4ea9-89be-9803c71bab44
Imbruvica(Ibrutinib)140mg Capsules
IMBRUVICA Rx
Generic Name and Formulations:
Ibrutinib 140mg; caps.
Company:
Pharmacyclics and Janssen Biotech
Indications for IMBRUVICA:
Mantle cell lymphoma (MCL) in patients who have received at least one prior therapy. Chronic lymphocytic leukemia (CLL) in patients who have received at least one prior therapy. CLL in patients with 17p deletion.
Adult:
Swallow whole with water. MCL: 560mg once daily. CLL: 420mg once daily. Concomitant moderate CYP3A inhibitors: 140mg once daily. Dose modifications for toxicities: see full labeling.
Children:
Not established.
Pharmacological Class:
Bruton’s tyrosine kinase (BTK) inhibitor.
Warnings/Precautions:
Risk of hemorrhage; consider the benefit/risk of withholding treatment for 3–7 days pre-and post-surgery. Monitor for fever and infections; eva luate promptly if occurs. Monitor for myelosuppression; obtain CBCs monthly. Periodically monitor for atrial fibrillation (esp. in those with cardiac risk factors, acute infections, history of atrial fibrillation); do ECG if arrhythmic symptoms or new onset dyspnea develop. Risk of second primary malignancies (eg, skin cancer or other carcinomas). Hepatic or renal impairment. Maintain adequate hydration. Pregnancy (Cat.D); avoid. Nursing mothers: not recommended.
Interactions:
Concomitant strong CYP3A inhibitors taken chronically (eg, ritonavir, indinavir, nelfinavir, saquinavir, boceprevir, telaprevir, nefazodone): not recommended; for short-term (≤7days) use of strong CYP3A inhibitors (eg, ketoconazole, itraconazole, voriconazole, posaconazole, clarithromycin, telithromycin); consider interrupting ibrutinib therapy. If concomitant moderate CYP3A inhibitors must be used (eg, fluconazole, darunavir, erythromycin, diltiazem, atazanavir, aprepitant, amprenavir, fosamprevir, crizotinib, imatinib, verapamil, ciprofloxacin): reduce ibrutinib dose (see Adults). Avoid grapefruit and Seville oranges during treatment. Avoid concomitant strong CYP3A inducers (eg, carbamazepine, rifampin, phenytoin, St. John’s Wort); consider alternatives. Increased risk of hemorrhage with concomitant antiplatelets or anticoagulants.
Adverse Reactions:
Thrombocytopenia, diarrhea, neutropenia, anemia, fatigue, musculoskeletal pain, peripheral edema, upper respiratory tract infection, nausea, bruising, dyspnea, constipation, rash, abdominal pain, vomiting, decreased appetite, pyrexia.
How Supplied:
Caps—90, 120
