Isaacs John D, Zuckerman Andrea, Krishnaswami Sriram, Nduaka Chudy, Lan Shuping, Hutmacher Matthew M, Boy Mary G, Kowalski Ken, Menon Sujatha, Riese Richard
Arthritis Res Ther. 2014 Jul 25;16(4):R158. doi: 10.1186/ar4673.
Small increases in mean serum creatinine (SCr) were observed in studies of rheumatoid arthritis patients during tofacitinib treatment. These SCr changes were investigated and potential mechanisms explored.
SCr values and renal adverse event data were pooled from five Phase 3 and two long-term extension (LTE) studies. Dose-response relationships and association with inflammation (C-reactive protein (CRP)) were explored using Phase 2 data and confirmed with Phase 3 data.
In Phase 3, least squares mean SCr differences from placebo at Month 3 were 0.02 and 0.04 mg/dl for tofacitinib 5 and 10 mg twice daily (BID) (P <0.05), respectively. During Months 0 to 3, confirmed SCr ≥33% increases over baseline were reported in 17 (1.4%; 5 mg BID) and 23 (1.9%; 10 mg BID) patients. Generally, elevations plateaued and remained within normal limits throughout Phase 3 and LTE studies. Exposure-response modeling demonstrated small, reversible effects of tofacitinib on mean SCr, and significant (P <0.05) effects of CRP on model parameters. Phase 3 data confirmed that patients with higher baseline CRP or greater CRP decreases following tofacitinib treatment had the largest increases in SCr. Across Phase 3 and LTE studies, 22 tofacitinib-treated patients had clinical acute renal failure (ARF), predominantly in the setting of concurrent serious illness.
Tofacitinib treatment was associated with small, reversible mean increases in SCr that plateaued early. The mechanism behind these SCr changes remains unknown, but may involve effects of tofacitinib on inflammation. ARF occurred infrequently, was associated with concurrent serious illness, and was unrelated to prior SCr increases.
在托法替布治疗类风湿关节炎患者的研究中,观察到血清肌酐(SCr)均值有小幅升高。对这些SCr变化进行了研究,并探讨了潜在机制。
汇总了五项3期研究和两项长期扩展(LTE)研究中的SCr值和肾脏不良事件数据。使用2期数据探索剂量反应关系以及与炎症(C反应蛋白(CRP))的关联,并通过3期数据进行确认。
在3期研究中,托法替布5毫克和10毫克每日两次(BID)在第3个月时与安慰剂相比,SCr的最小二乘均值差异分别为0.02和0.04毫克/分升(P<0.05)。在第0至3个月期间,17名(1.4%;5毫克BID)和23名(1.9%;10毫克BID)患者报告SCr较基线升高≥33%。总体而言,在整个3期和LTE研究中,升高趋于平稳并保持在正常范围内。暴露反应模型显示托法替布对SCr均值有小的、可逆的影响,而CRP对模型参数有显著(P<0.05)影响。3期数据证实,基线CRP较高或托法替布治疗后CRP下降幅度较大的患者,其SCr升高幅度最大。在整个3期和LTE研究中,22名接受托法替布治疗的患者出现临床急性肾衰竭(ARF),主要发生在并发严重疾病的情况下。
托法替布治疗与SCr均值小幅度、可逆的升高相关,且早期趋于平稳。这些SCr变化背后的机制尚不清楚,但可能涉及托法替布对炎症的影响。ARF发生率较低,与并发严重疾病有关,与先前的SCr升高无关。