Ann Intern Med. 2013 Aug 20;159(4):253-61. doi: 10.7326/0003-4819-159-4-201308200-00006.
Many patients with rheumatoid arthritis (RA) do not achieve adequate and safe responses with disease-modifying antirheumatic drugs (DMARDs). Tofacitinib is a novel, oral, Janus kinase inhibitor that treats RA.
To evaluate the efficacy and safety of tofacitinib in combination with nonbiologic DMARDs.
1-year, double-blind, randomized trial (ClinicalTrials.gov: NCT00856544).
114 centers in 19 countries.
792 patients with active RA despite nonbiologic DMARD therapy.
Patients were randomly assigned 4:4:1:1 to oral tofacitinib, 5 mg or 10 mg twice daily, or placebo advanced to tofacitinib, 5 mg or 10 mg twice daily.
Primary end points were 20% improvement in American College of Rheumatology (ACR20) criteria; Disease Activity Score for 28-joint counts based on the erythrocyte sedimentation rate (DAS28-4[ESR]) of less than 2.6; DAS28-4(ESR)-defined remission, change in Health Assessment Questionnaire Disability Index (HAQ-DI) score, and safety assessments.
Mean treatment differences for ACR20 response rates (month 6) for the 5-mg and 10-mg tofacitinib groups compared with the combined placebo groups were 21.2% (95% CI, 12.2% to 30.3%; P < 0.001) and 25.8% (CI, 16.8% to 34.8%; P < 0.001), respectively. The HAQ-DI scores (month 3) and DAS28-4(ESR) less than 2.6 response rates (month 6) were also superior in the tofacitinib groups versus placebo. The incidence rates of serious adverse events for patients receiving 5-mg tofacitinib, 10-mg tofacitinib, or placebo were 6.9, 7.3, or 10.9 events per 100 patient-years of exposure, respectively. In the tofacitinib groups, 2 cases of tuberculosis, 2 cases of other opportunistic infections, 3 cardiovascular events, and 4 deaths occurred. Neutrophil counts decreased, hemoglobin and low- and high-density lipoprotein cholesterol levels increased, and serum creatinine levels had small increases in the tofacitinib groups.
Placebo groups were smaller and of shorter duration. Patients received primarily methotrexate. The ability to assess drug combinations other than tofacitinib plus methotrexate was limited.
Tofacitinib improved disease control in patients with active RA despite treatment with nonbiologic DMARDs, primarily methotrexate.
Pfizer.
许多类风湿关节炎(RA)患者在使用疾病修饰抗风湿药物(DMARDs)后无法达到充分和安全的应答。托法替尼是一种新型的、口服的、Janus 激酶抑制剂,用于治疗 RA。
评估托法替尼联合非生物 DMARD 治疗的疗效和安全性。
1 年、双盲、随机试验(ClinicalTrials.gov:NCT00856544)。
19 个国家的 114 个中心。
792 例接受非生物 DMARD 治疗后仍有活动期 RA 的患者。
患者随机分为 4:4:1:1 组,分别接受口服托法替尼 5 mg 或 10 mg、每日 2 次,或安慰剂,随后进展为托法替尼 5 mg 或 10 mg、每日 2 次。
主要终点是美国风湿病学会(ACR)20%改善标准;红细胞沉降率(ESR)为 28 个关节疾病活动度评分(DAS28-4[ESR])<2.6;DAS28-4(ESR)定义的缓解,健康评估问卷残疾指数(HAQ-DI)评分的变化,以及安全性评估。
5 mg 和 10 mg 托法替尼组与联合安慰剂组相比,ACR20 应答率(第 6 个月)的平均治疗差异分别为 21.2%(95%CI,12.2%至 30.3%;P<0.001)和 25.8%(CI,16.8%至 34.8%;P<0.001)。托法替尼组在第 3 个月的 HAQ-DI 评分和第 6 个月的 DAS28-4(ESR)<2.6 应答率也优于安慰剂组。接受 5 mg 托法替尼、10 mg 托法替尼或安慰剂治疗的患者严重不良事件的发生率分别为每 100 患者-年暴露 6.9、7.3 或 10.9 例。托法替尼组发生 2 例结核病、2 例其他机会性感染、3 例心血管事件和 4 例死亡。中性粒细胞计数下降,血红蛋白、低和高密度脂蛋白胆固醇水平升高,血清肌酐水平略有升高。
安慰剂组较小且持续时间较短。患者主要接受甲氨蝶呤治疗。评估除托法替尼加甲氨蝶呤以外的药物联合的能力有限。
托法替尼改善了接受非生物 DMARDs(主要是甲氨蝶呤)治疗的活动期 RA 患者的疾病控制。
辉瑞公司。