Department of Pharmacy Practice and Pharmacy Administration, University of the Sciences in Philadelphia, Philadelphia, PA, USA.
Ann Pharmacother. 2010 Jan;44(1):135-44. doi: 10.1345/aph.1M227.
To review the pharmacologic, pharmacokinetic, efficacy, and safety data of golimumab, an anti-tumor necrosis factor alpha (TNF-alpha) monoclonal antibody.
A search of MEDLINE (1950-September 2009) was performed to identify any published clinical trials or review articles pertaining to golimumab. Key search terms included golimumab, rheumatoid arthritis, CNTO 148, and anti-TNF-alpha inhibitors. Bibliographies of selected articles were reviewed to identify other relevant citations. Abstracts from national and international meetings and information from the manufacturer were also reviewed.
All available published articles and abstracts describing golimumab's pharmacologic or pharmacokinetic profile, efficacy, and safety were included.
Golimumab is a fully humanized TNF-alpha monoclonal antibody that is specific for human TNF-alpha. Trials have investigated the use of golimumab in patients who have rheumatoid arthritis (RA) and are on methotrexate, are methotrexate-naïve, and have previously tried TNF-alpha inhibition therapy. When used in combination with methotrexate or another disease-modifying antirheumatic drug, golimumab therapy results in improvements of clinical outcomes including the American College of Rheumatology parameters in all of the aforementioned populations. Although multiple doses and dosing regimens have been studied, the Food and Drug Administration-approved dose is 50 mg subcutaneously every 4 weeks. The most common adverse effects include injection site erythema, headaches, and nausea. There were a limited number of incidences of serious infection or malignancy.
With 4 TNF-alpha monoclonal antibodies currently on the market, it is unclear what golimumab's place in therapy for RA will be. Some benefits include monthly injections, proven efficacy after previous TNF-alpha inhibitor therapy, and limited antibody development during therapy. However, with a lack of longer-term trials assessing efficacy and safety compared with other TNF-alpha inhibitors, golimumab should be reserved for use after other therapies fail.
综述肿瘤坏死因子-α（TNF-α）单克隆抗体戈利木单抗的药理学、药代动力学、疗效和安全性数据。
检索 MEDLINE（1950 年-2009 年 9 月），以查找与戈利木单抗相关的已发表的临床试验或综述文章。主要检索词包括戈利木单抗、类风湿关节炎、CNTO 148 和抗 TNF-α 抑制剂。还查阅了所选文章的参考文献，以确定其他相关引文。同时还查阅了国内外会议摘要和制造商的信息。
所有已发表的描述戈利木单抗药理学或药代动力学特征、疗效和安全性的文章和摘要均被纳入。
戈利木单抗是一种完全人源化的 TNF-α单克隆抗体，特异性针对人 TNF-α。临床试验已研究了戈利木单抗在接受甲氨蝶呤治疗、甲氨蝶呤初治以及先前接受 TNF-α 抑制治疗的类风湿关节炎（RA）患者中的应用。当与甲氨蝶呤或其他疾病修饰抗风湿药物联合使用时，戈利木单抗治疗可改善所有上述人群的临床结局，包括美国风湿病学会参数。虽然已研究了多种剂量和给药方案，但美国食品和药物管理局批准的剂量为 50mg 皮下注射，每 4 周 1 次。最常见的不良反应包括注射部位红斑、头痛和恶心。严重感染或恶性肿瘤的发生率有限。
目前有 4 种 TNF-α单克隆抗体上市，尚不清楚戈利木单抗在 RA 治疗中的地位如何。其具有一些优势，包括每月注射 1 次、先前 TNF-α 抑制剂治疗后疗效确切以及治疗过程中抗体产生有限。但是，与其他 TNF-α抑制剂相比，缺乏长期疗效和安全性评估的临床试验，因此，戈利木单抗应保留在其他治疗失败后使用。
