近日，美国FDA批准Cimzia被用于成人中度至重度活动性类风湿关节炎的治疗，用于缓解克罗恩病的症状体征，以及用于对常规治疗无应答的中度至重度活动性疾病成人患者维持临床应答。在欧盟，Cimzia联合甲氨蝶呤(MTX)被批准治疗对缓解疾病抗风湿药(DMARDs，如MTX)应答不足的中度至重度活动性RA患者。
批准日期：2016年11月3日 公司：比利时制药
CIMZIA (聚乙二醇结合赛妥珠单抗[certolizumab pegol])冻干粉，为皮下使用溶液
美国初次批准：2008
最近重大改变
适应证和用途：09/2013
剂量和给药方法：09/2013
警告和注意事项：11/2012
警告和注意事项：10/2012
作用机制
聚乙二醇结合赛妥珠单抗结合至人类TNFα有一个KD为90pM. TNFα是一个关键促炎性细胞因子在炎性过程中起中心作用。聚乙二醇结合赛妥珠单抗选择性地中和TNFα(IC90为4 ng/mL 在体外L929鼠类纤维母细胞瘤细胞毒性试验对人类TNFα的抑制作用)但不中和淋巴毒素α TNFβ)。聚乙二醇结合赛妥珠单抗与啮齿类和兔TNF交叉反应差，因此体内用动物模型评价疗效其中人类TNFα是生理学上活性分子。
聚乙二醇结合赛妥珠单抗被显示以依赖剂量方式中和膜结合和可溶性人类TNFα。在人类单核细胞中单核细胞与聚乙二醇结合赛妥珠单抗培育导致依赖剂量的LPS-诱导TNFα和IL-1β生成的抑制作用。
聚乙二醇结合赛妥珠单抗不含可结晶的(Fc)区片段，在完整抗体中正常存在，和因此在体外不固定补体或引起抗体依赖细胞介导的细胞毒性。在体外不诱导人类外周学衍生单核细胞或淋巴细胞凋亡，聚乙二醇结合赛妥珠单抗也不诱导中性粒细胞脱颗粒[degranulation]。进行一项在体外体内(ex vivo)组织反应性研究评价聚乙二醇结合赛妥珠单抗与正常人类组织冰冻切片的潜在交叉反应性。聚乙二醇结合赛妥珠单抗显示与被设计的人类正常组织标准名单无反应性。
适应证和用途
CIMZIA是一种肿瘤坏死因子(TNF)阻断剂适用为：
（1）在克罗恩病对常规治疗反应不佳的有中度至严重活动性疾病成年患者中减轻体征和症状和维持临床反应。
（2）治疗有中度至严重活动性类风湿样关节炎成年。
（3）治疗有活动性银屑病关节炎成年患者。
剂量和给药方法
CIMZIA是通过皮下注射给药。CIMZIA的初始剂量是400mg(给予两次皮下注射200 mg)。
克罗恩病
（1）初始400mg和在第2和4周时。如发生反应，接着每4周400mg。
类风湿样关节炎
（2）初始400mg和在2和4周时，接着每隔周200mg；为维持给药可考虑每4周400mg。
银屑病关节炎
（3）初始400mg和在第2和4周时，接着每隔周200mg；为维持给药可考虑每4周400mg。
剂型和规格
（1）为重建200mg冻干粉，在单次使用玻璃小瓶内，与1mL无菌注射用水，USP
（2）200mg/mL溶液在一个单次使用预装注射器内
禁忌证
无。
警告和注意事项
（1）严重感染 –活动性感染期间不要开始CIMZIA。如发生一种感染，小心监视，和如感染变成严重停止CIMZIA。
（2）侵袭性真菌感染– 对用CIMZIA发生全身性疾病患者，对对至真菌是地方病的地区居住和旅游患者考虑经验性抗真菌治疗。
（3）接受TNF阻断剂患者中曾观察到淋巴瘤和其他恶性病病例
（4）可能发生心衰，恶化或新发作
（5）可能发生过敏性反应或严重的过敏反应
（6）乙型肝炎病毒再激活–开始CIMZIA前测试HBV感染。治疗期间和几个月后监视HBV携带者。如发生再激活，停止CIMZIA和开始抗-病毒治疗
（7）可能发生脱髓鞘疾病，加重或新发作
（8）血细胞减少，全血细胞减少–劝告患者如发生症状立即求医，和考虑停止CIMZIA
（9）狼疮样综合征–如发生症状停止CIMZIA
不良反应
最常见不良反应(发生率≥7%和较高于安慰剂)：上呼吸道感染，皮疹，和泌尿道感染
药物相互作用
（1）与生物制品DMARDs使用–严重感染的风险增加
（2）活疫苗–不要与CIMZIA给予
（3）实验室测试–可能干扰aPTT测试
包装规格
CIMZIA 400MG SDV (INST ONLY) 2  CERTOLIZUMAB PEGOL  UCB PHARM  50474-0700-62
CIMZIA KIT FOR INJ 200MG SDV 2/PAC  CERTOLIZUMAB PEGOL  "UCB, INC."  50474-0700-62
CIMZIA KIT FOR INJ 200MG SYR 2/PAC  CERTOLIZUMAB PEGOL  "UCB, INC."  50474-0710-79
CIMZIA PRE FILLED SYR 200MG 2  CERTOLIZUMAB PEGOL  UCB PHARM  50474-0710-79
CIMZIA START KIT INJ 200MG SYR 6/PAC  CERTOLIZUMAB PEGOL  "UCB, INC."  50474-0710-81        
CIMZIA START KIT 200MG 6PFS3X2  CERTOLIZUMAB PEGOL  UCB PHARM  50474-0710-81
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b4c2c9dc-a0bb-4d64-a667-a67ebe88392d
Cimzia(Certolizumab Pegol Injection)
GENERIC NAME: certolizumab
BRAND NAME: Cimzia
DRUG CLASS AND MECHANISM: Certolizumab is an injectable synthetic (man-made) protein antibody that binds to tumor necrosis factor alpha (TNFα) in the body and blocks the effects of TNFα in patients with rheumatoid arthritis and Crohn's disease. Adalimumab (Humira) and etanercept (Enbrel) are two other injectable drugs that block TNFα. Inflammation is the body's reaction to injury and is a necessary process for the repair of injury.
TNF is a protein that the body produces when there is inflammation.
TNF promotes inflammation and the signs of inflammation, which, in the case of arthritis, include fever as well as pain, tenderness, and swelling of joints. In the case of Crohn's disease, the signs of inflammation include fever, abdominal pain, and diarrhea. The unchecked
inflammation of rheumatoid arthritis eventually leads to destruction of the joints. The inflammation in Crohn's disease can lead to strictures (narrowing) of the intestine or intestinal perforation.
Certolizumab binds to TNF in the body and thereby blocks the effects of TNF. As a result, inflammation and its consequences in the joints
and intestine are reduced. In arthritis, the progressive destruction of the joints is slowed or prevented. The FDA approved Certolizumab in April 2008.
GENERIC AVAILABLE: No
PRESCRIPTION: Yes
PREPARATIONS: Injection (powder): 200 mg. Injection (prefilled syringe): 200 mg
STORAGE: Certolizumab should be stored refrigerated at 2 to 8 C (36 to 46 F). Reconstituted certolizumab should be used within two hours if kept at room temperature or within 24 hours if refrigerated.
PRESCRIBED FOR: Certolizumab is used for treating signs and symptoms of moderate to severe Crohn's disease and maintaining response in adults unresponsive to usual treatment.
It is also used for treating rheumatoid arthritis.
It may be used alone or combined with methotrexate (Rheumatrex, Trexall) or other drugs used for treating rheumatoid arthritis.
DOSING: Certolizumab is injected under the skin (thigh or abdomen).
Injection sites should be rotated. The recommended dose for treating Crohn‘s disease is 400 mg initially (2 injections of 200 mg), followed by 400 mg at weeks 2 and 4. For those who respond, the recommended maintenance dose is 400 mg every 4 weeks.
The recommended dose for treating rheumatoid arthritis is 400 mg (2 injections of 200 mg) initially and at weeks 2 and 4, followed by 200 mg every other week.
DRUG INTERACTIONS: Combining anakinra (Kineret), abatacept(Orencia), rituximab (Rituxan) or natalizumab (Tysabri) with certolizumab may result in reduced white blood cells in the blood(neutropenia), serious infections and no additional benefit.
Certolizumab may interfere with the effectiveness of vaccines. Live vaccines, including attenuated vaccines, should not be used while patients are being treated with certolizumab. Certolizumab may interfere with tests of coagulation in patients receiving blood thinners.
PREGNANCY: There are no adequate studies of certolizumab in pregnant women.
NURSING MOTHERS: It is not known whether certolizumab is excreted in breast milk.
SIDE EFFECTS: The most common adverse effects in clinical studies were respiratory tract infections, urinary tract infections, and arthralgia (pain in the joints). Abdominal pain, diarrhea, and intestinal obstruction also may occur.
Certolizumab may cause swelling, redness, pain and itching at the site of injection. Like other drugs that block TNFα, use of certolizumab has been associated with serious infections such as tuberculosis, sepsis (bacteria in the blood) and fungal infections.
Individuals with active infections should not be treated with certolizumab. Certolizumab may worsen or cause new diseases of the nervous system. Certolizumab also may cause or worsen congestive heart failure.
In studies, some patients who used certolizumab or other TNFα blocking drugs developed cancer.
Since patients with Crohn's disease have a higher risk of cancers than the general population, the connection between cancer and use of certolizumab is unclear. Other side effects of certolizumab include hypersensitivity (allergic) reactions (including anaphylaxis) and reduced levels in the blood of platelets and red blood cells (aplastic anemia).
Certolizumab may increase the risk of reactivating hepatitis B virus in chronic careers of the virus.