Department of Pharmacy Practice, Thomas J. Long School of Pharmacy, University of the Pacific, Stockton, CA, USA.
Ann Pharmacother. 2023 Apr;57(4):450-462. doi: 10.1177/10600280221113092. Epub 2022 Aug 2.
To review the characteristics, efficacy, safety, pharmacoeconomics, and place in therapy of upadacitinib, a Janus kinase (JAK) inhibitor, in the treatment of rheumatoid arthritis (RA).
PubMed (January 2003-May 2022) was searched using upadacitinib and ABT-494.
Human studies published in peer-reviewed publications in English were the primary sources for efficacy and safety data.
In randomized, double-blind, controlled clinical studies, upadacitinib demonstrated statistically significant improvement in RA symptoms as monotherapy and in combination with conventional synthetic disease-modifying antirheumatic drugs (csDMARDs) when compared with csDMARD monotherapy or to adalimumab or abatacept in combination with csDMARD therapy in patients with RA. American College of Rheumatology 20% response rates were 68% to 79% for upadacitinib monotherapy and 64% to 84% for upadacitinib plus csDMARD therapy, compared with 28% to 59% for csDMARD-only therapy and 63% to 74% for biologic DMARD (bDMARD) plus csDMARD therapy. Long-term extension studies demonstrated similar findings. Upadacitinib had similar rates of serious infections, herpes zoster, major cardiovascular events, and venous thromboembolic events as other JAK inhibitors. Upadacitinib was similar in cost to tofacitinib and twice as high as baricitinib based on current estimated costs to patients, but actual costs may vary.
Upadacitinib is an alternative therapy to other JAK inhibitors and bDMARDs in patients with moderate to severe RA who have had an inadequate response to a tumor necrosis factor inhibitor alone or in combination with a csDMARD.
Upadacitinib is an effective JAK inhibitor for use in RA.
综述 JAK 抑制剂乌帕替尼在治疗类风湿关节炎（RA）中的特点、疗效、安全性、药物经济学和治疗地位。
通过 upadacitinib 和 ABT-494 在 PubMed（2003 年 1 月-2022 年 5 月）进行检索。
以同行评审出版物中发表的人体研究为主要来源，获取疗效和安全性数据。
在随机、双盲、对照临床试验中，与 csDMARD 单药治疗或与阿达木单抗或阿巴西普联合 csDMARD 治疗相比，乌帕替尼单药治疗或联合 csDMARD 治疗 RA 患者时，在 RA 症状方面表现出统计学显著改善。乌帕替尼单药治疗的美国风湿病学会 20%缓解率为 68%至 79%，乌帕替尼联合 csDMARD 治疗的缓解率为 64%至 84%，而 csDMARD 单药治疗的缓解率为 28%至 59%，生物 DMARD（bDMARD）联合 csDMARD 治疗的缓解率为 63%至 74%。长期扩展研究得出了类似的结果。乌帕替尼与其他 JAK 抑制剂相比，严重感染、带状疱疹、主要心血管事件和静脉血栓栓塞事件的发生率相似。基于目前估计的患者成本，乌帕替尼的成本与托法替尼相似，是巴瑞替尼的两倍，但实际成本可能有所不同。
对于肿瘤坏死因子抑制剂单药或联合 csDMARD 治疗反应不足的中重度 RA 患者，乌帕替尼是其他 JAK 抑制剂和 bDMARD 的替代治疗选择。
乌帕替尼是治疗 RA 的一种有效的 JAK 抑制剂。
