2012年11月7日讯 /生物谷BIOON/ --辉瑞（Pfizer）今天宣布，药物Xeljanz（tofacitinib）获FDA批准，用于对氨甲喋呤（methotrexate）治疗反应不足或不耐受的中度至重度活动性类风湿性关节炎（RA）成人患者的治疗，该药将与雅培（Abbott）重磅药物阿达木单抗（Humira）展开竞争。
RA是一种自身免疫性疾病，由于人体免疫系统错误地攻击健康组织，导致关节及周围组织的炎症。据疾病预防控制中心数据，在美国约有150万人受RA困扰。Xeljanz是一种日服2次的药物，通过阻断Janus激酶发挥作用，该激酶在RA的关节发炎中具有重要作用。
有关Xeljanz的处方药用户收费目标日为2012年11月21日，但FDA提前完成了对药物的审查。
Xeljanz的安全性及疗效，在7个临床试验中进行了评价。这些实验在中度至重度活动性RA患者中开展，在所有的试验中，与安慰剂组相比，Xeljanz治疗组经历了临床反应及身体机能的改善。
Xeljanz用药，与增加的严重感染风险相关，包括机会性感染、结核、肿瘤、淋巴瘤。Xeljanz附带有一个有关这些风险的黑框警告。Xeljanz治疗也与胆固醇和肝酶的增加及血液计数的减少相关。
FDA通过风险评估及建在策略（REMS）程序批准了Xeljanz，REMS包括一份用药指南，告知患者有关药物的安全信息，同时也包含一项沟通计划，来告知卫生保健提供者有关Xeljanz用药相关的严重风险。
为研究Xeljanz对心脏疾病、癌症、严重感染的长期影响，FDA要求辉瑞开展一项上市后研究，该研究将评价2种剂量的Xeljanz，同时还包括一组用另一种已获批药物治疗的患者组，作为对照。
在临床试验中，最常见的不良反应为上呼吸道感染头疼、腹泻、鼻道及上咽部炎症
适应症和用途
● XELJANZ，一种Janus激酶(JAKs)的抑制剂，适用于治疗中度至严重活动性类风湿性关节炎成年患者对氨甲喋呤已反应不佳或不能耐受。可用作单药治疗或与氨甲喋呤或其他非生物制品疾病修饰抗风湿药物(DMARDs)联用。
● XELJANZ不应与生物制品DMARD或强免疫抑制剂例如硫唑嘌呤[zathioprine]和环孢菌素[cyclosporine]联用。 (1.1)

剂量和给药方法
类风湿性关节炎
XELJANZ的推荐剂量是5 mg每天2次。
剂型和规格
● 片：5 mg (3)
禁忌症
无 (4)
XELJANZ (tofacitinib citrate) tablet, film coated
[U.S. Pharmaceuticals]
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use XELJANZ safely and effectively. See full prescribing information for XELJANZ.
XELJANZ ® (tofacitinib) tablets for oral administration
Initial U.S. Approval: 2012
WARNING: SERIOUS INFECTIONS AND MALIGNANCY
See full prescribing information for complete Boxed Warning.
• Serious infections leading to hospitalization or death, including tuberculosis and bacterial, invasive fungal, viral, and other opportunistic infections, have occurred in patients receiving XELJANZ. (5.1)
 • If a serious infection develops, interrupt XELJANZ until the infection is controlled. (5.1)
 • Prior to starting XELJANZ, perform a test for latent tuberculosis; if it is positive, start treatment for tuberculosis prior to starting XELJANZ. (5.1)
 • Monitor all patients for active tuberculosis during treatment, even if the initial latent tuberculosis test is negative. (5.1)
 • Lymphoma and other malignancies have been observed in patients treated with XELJANZ. Epstein Barr Virus- associated post-transplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with XELJANZ and concomitant immunosuppressive medications. (5.2)
INDICATIONS AND USAGE
•XELJANZ, an inhibitor of Janus kinases (JAKs), is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs).
 •XELJANZ should not be used in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine. (1.1)
DOSAGE AND ADMINISTRATION
Rheumatoid Arthritis
  The recommended dose of XELJANZ is 5 mg twice daily.
DOSAGE FORMS AND STRENGTHS
•Tablets: 5 mg (3)
CONTRAINDICATIONS
None (4)
WARNINGS AND PRECAUTIONS
•Serious Infections