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ACTEMRA(托珠单抗,tocilizumab) -白细胞介素-6受体抑制剂

2012-11-22 11:04:39 作者：新特药房来源：中国新特药网天津分站浏览次数：412 文字大小：【大】【中】【小】

简介：FDA批准治疗类风湿性关节炎新药tocilizumab(Actemra)美国食品药品管理局（FDA）批准 tocilizumab（Actemra）用于治疗类风湿性关节炎，该药适用于使用其他已获批的治疗药物无效的成年中重度类风湿性关节炎患者。 ...

关键字：ACTEMRA(托珠单抗 tocilizumab) 白细胞介素-6受体抑制剂

FDA批准治疗类风湿性关节炎新药tocilizumab(Actemra)
美国食品药品管理局（FDA）批准 tocilizumab（Actemra）用于治疗类风湿性关节炎，该药适用于使用其他已获批的治疗药物无效的成年中重度类风湿性关节炎患者。Actemra通过抑制白介素-6（类风湿性关节炎患者体内一种过多的免疫蛋白）受体的活性而发挥作用。
基于其在临床研究中显示的严重的安全性问题，Actemra仅被推荐用于其他治疗无效的患者。这些安全性担忧主要包括肝酶升高、低密度脂蛋白（LDL）升高或胆固醇水平升高、高血压、胃肠穿孔。
在已开展的对类风湿性关节炎成年患者治疗的5项临床研究显示了Actemra的有效性和安全性。这些临床研究显示，该药与安慰剂组比，使用Actemra进行治疗的患者，在关节柔韧度与肿胀度方面均有更大程度的改善。
临床研究显示，使用Actemra治疗类风湿性关节炎最常见的不良反应有上呼吸道感染、头痛、鼻或鼻腔发炎、高血压和肝酶升高。一些患者中偶见LDL水平升高或胆固醇水平升高，需要额外使用降脂药物。使用Actemra的患者出现严重感染的风险更高。临床研究中出现感染的患者大多数也同时使用了抑制免疫系统作用的其他药物，如甲氨蝶呤或皮质类固醇。
tocilizumab（Actemra）为此非常严重疾病患者提供一种新选择!

Generic Name and Formulations:
Tocilizumab 20mg/mL; soln for IV infusion after dilution; preservative-free.

Company:
Genentech, Inc.
Indications:
Moderately-to-severely active rheumatoid arthritis (RA) in patients who have had an inadequate response to ≥1 DMARDs; may be used as monotherapy or concomitantly with methotrexate or other DMARDs. Active systemic juvenile idiopathic arthritis (SJIA), as monotherapy or in combination with methotrexate.

Adult Dose:
RA: Give as a 60-minute single IV infusion. Initially 4mg/kg every 4 weeks, followed by an increase to 8mg/kg every 4 weeks based on clinical response. Doses >800mg per infusion: not recommended. Do not start if ANC<2000/mm3, platelets <100000/mm3, or ALT/AST >1.5xULN. Reduce dose to 4mg/kg if elevated liver enzymes, neutropenia, or thrombocytopenia occur (see literature).

Children's Dose:
RA: not recommended. SJIA: <2yrs: not recommended. ≥2yrs: Give once every 2 weeks as a 60-minute IV infusion. <30kg: 12mg/kg. ≥30kg: 8mg/kg. Do not start if ANC<2000/mm3, platelets <100000/mm3, or ALT/AST >1.5xULN. May need to interrupt dose if elevated liver enzymes, neutropenia, or thrombocytopenia occur.

Pharmacological Class:
Interleukin-6 receptor inhibitor.

Warnings/Precautions:
Increased risk of serious or fatal infections (eg, TB, bacterial, invasive fungal, viral, and other opportunistic infections); if develop, interrupt until controlled. Active infections: do not give therapy. Consider risks/benefits prior to initiating: chronic or recurrent, or history of opportunistic infections, exposed to TB, travel to, or residence in, areas with endemic TB or mycoses, conditions that predispose to infection. Monitor closely for signs/symptoms of infection during and after therapy; interrupt if serious or opportunistic infection or sepsis develop. Test for and treat latent TB prior to starting therapy. HBV or HCV infection. ANC <500mm3, platelets <50000mm3, or ALT/AST >5xULN: not recommended. Monitor neutrophils, platelets, liver function tests: RA: every 4–8 weeks; SJIA: at the time of the 2nd infusion and then every 2–4 weeks. Monitor lipids 4–8 weeks after initiation, then every 6 months. Increased risk of GI perforation. Active hepatic disease or impairment: not recommended. Immunosuppression. Malignancies. CNS demyelinating disorders. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions:
Increased risk for infection with concomitant immunosuppressants (eg, TNF antagonists, IL-1R antagonists, anti-CD20 monoclonal antibodies, selective co-stimulation modulators). Avoid live vaccines. Caution with CYP3A4 substrate drugs (eg, oral contraceptives, lovastatin, atorvastatin). Monitor warfarin, cyclosporine, theophylline, other drugs that are CYP450 substrates with narrow therapeutic indices.

Adverse Reactions:
Upper respiratory tract infections, nasopharyngitis, headache, hypertension, increased ALT; hypersensitivity reactions (may be severe and fatal), neutropenia, thrombocytopenia, gastrointestinal perforations, increased lipids.

Generic Availability:
NO

How Supplied:
Single-use vials (80mg/4mL, 200mg/10mL, 400mg/20mL)—1, 4

关于RoActemra

Actemra是首个人源抗IL-6受体单克隆抗体，获批用于治疗中至重度成年人类风湿关节炎。该药由罗氏旗下的基因泰克公司生产，于2010年1月获得FDA批准，并已在日本、澳大利亚和欧洲获得批准，商品名为RoActemra。此外，Actemra也被批准用于治疗2岁及以上全身型幼年特发性关节炎（SJIA）患者。
罗氏公司（Roche）宣布，其战略联盟伙伴日本中外制药株式会社的新药（Actemra）已在日本获得用于类风湿关节炎（RA）治疗的上市许可。
中外公司的抗人白介素-6受体单克隆抗体Actemra（tocilizumab，MRA）（Ⅰ），已经在日本上市，用以治疗罕见的Castleman病。该产品不仅是第一个日本研发的单抗，也是第一个治疗这种少见的淋巴增生性疾病的已商品化药物。