全球首个抗IL-6抗炎药sarilumab（商品名 Kevzara 由赛诺菲/与再生元合作开发）被美国FDA批准用于治疗成人中度至重度活动性类风湿性关节炎 2017年2月3日，美国FDA批准上市，用于既往接受一种或多种疾病修饰抗风湿药物（DMARDs，例如甲氨蝶呤[MTX]）治疗缓解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。Kevzara是一种人源化单克隆抗体，靶向结合白介素-6受体（IL-6R），抑制该受体介导的炎性信号。Kevzara可作为单药治疗，也可与甲氨蝶呤（MTX）或其他传统的DMARDs药物联合用药。 Kevzara的获批，是基于全球性SARIL-RA III期临床项目的数据，该项目包括7个III期临床研究，涉及超过3300例活动性中度至重度RA成人患者，其中大部分患者对之前的治疗方案反应不足。SARIL-RA III期临床项目专注于对疾病修饰抗风湿药物（DMARDs，包括甲氨蝶呤）或肿瘤坏死因子-α（TNF-α）抑制剂应答不足的活动性中度至重度类风湿性关节炎（RA）成人患者群体，旨在广泛的患者中评估皮下注射sarilumab作为单药疗法或联合传统的疾病修饰抗风湿药物（DMARDs，包括氨甲喋呤）在改善疾病症状和体征、抑制RA放射学进展方面的疗效和安全性。 sarilumab（REGN88/SAR15319）是首个直接靶向IL-6受体复合物α亚基（IL-6R α）的全人源化单克隆抗体，能够特异性结合可溶性的和膜结合型的IL-6受体，抑制通过这些受体介导的细胞信号传导。IL-6在类风湿性关节炎（RA）患者血清和滑液（synovial fluid）中是含量最丰富的一种细胞因子，其水平与疾病活动度和关节破坏密切相关。sarilumab由Regeneron公司利用其专有的Veloclmmune抗体技术开发，该抗体能够阻断IL-6与其受体的结合，中断细胞因子介导的炎症信号级联。 Kevzara的推荐剂量：为200mg，每2周进行一次皮下注射；在特定情况下，该剂量可由200mg降低至150mg，以助管理特定的实验室异常（中性粒细胞减少症、血小板减少症、肝酶升高）。 包装规格 150mg/1.14mL或200mg/1.14mL强度溶液提供，这种溶液是2-count包装中的单剂量预充式注射器。 Kevzara(sarilumab) for the Treatment of Adult Patients with Moderately to Severely Active Rheumatoid Arthritis Sanofi and Regeneron announced that the Food and Drug Administration (FDA) has approved Kevzara (sarilumab) injection for the treatment of adults with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response or intolerance to one or more disease-modifying antirheumatic drugs (DMARDs) such as methotrexate. Kevzara, an interleukin-6 (IL-6) receptor antagonist, may be used alone or in combination with methotrexate or other DMARDs. Its approval was supported by data from two Phase 3 trials that evaluated approximately 2,900 adults with moderately to severely active RA with inadequate response to previous treatment regimens. In the studies, Kevzara + background DMARDs led to statistically significant, clinically meaningful improvements in patients with moderately to severely active RA. In the MOBILITY study, patients treated with Kevzara + methotrexate had reduced signs and symptoms, improved physical function, and significantly less radiographic progression of structural damage vs. patients treated with placebo + methotrexate. At Week 24, the Kevzara 200mg and 150mg groups had a greater improvement in the primary endpoint vs. placebo as measured by 20% improvement in the ACR20 criteria (66% and 58% vs. 33%, respectively).   In the TARGET study, patients treated with Kevzara + DMARD had reduced signs and symptoms and improved physical function vs. placebo + DMARD. At Week 24, the Kevzara 200mg and 150mg groups had a greater improvement in the primary endpoint vs. placebo as measured by achieving the ACR20 response (61% and 56% vs. 34%, respectively). The most common adverse reactions seen with Kevzara are neutropenia, increased alanine aminotransferase, injection site erythema, upper respiratory infections, and urinary tract infections. Kevzara is available as a 150mg/1.14mL or 200mg/1.14mL strength solution in single-dose prefilled syringes in 2-count packs.