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乌帕替尼:首次获批。

Upadacitinib: First Approval.

机构信息

Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2019 Nov;79(16):1819-1828. doi: 10.1007/s40265-019-01211-z.

DOI:10.1007/s40265-019-01211-z
PMID:31642025
Abstract

Upadacitinib (Rinvoq™), an orally-administered Janus kinase 1 (JAK-1) inhibitor, is being developed by AbbVie for the treatment of rheumatoid arthritis. In August 2019, based on positive results from multinational phase III trials conducted in patients with rheumatoid arthritis, upadacitinib received marketing approval in the USA for the treatment of moderately to severely active rheumatoid arthritis and an inadequate response or intolerance to methotrexate. This article summarizes the milestones in the development of upadacitinib leading to this first approval for the treatment of rheumatoid arthritis.

摘要

乌帕替尼(Rinvoq™)是一种口服 Janus 激酶 1(JAK-1)抑制剂,由 AbbVie 公司研发,用于治疗类风湿关节炎。2019 年 8 月,基于在类风湿关节炎患者中开展的多国 III 期临床试验的积极结果,乌帕替尼在美国获得批准,用于治疗中重度活跃性类风湿关节炎和对甲氨蝶呤应答不足或不耐受的患者。本文总结了乌帕替尼研发过程中的重要里程碑,这些进展促成了该药在类风湿关节炎治疗领域的首次批准。

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2
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本文引用的文献

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Effects of Upadacitinib Coadministration on the Pharmacokinetics of Sensitive Cytochrome P450 Probe Substrates: A Study With the Modified Cooperstown 5+1 Cocktail.乌帕替尼联合用药对敏感细胞色素 P450 探针底物药代动力学的影响:一项采用改良库珀斯敦 5+1 鸡尾酒的研究。
J Clin Pharmacol. 2020 Jan;60(1):86-95. doi: 10.1002/jcph.1496. Epub 2019 Aug 5.
2
Safety and effectiveness of upadacitinib or adalimumab plus methotrexate in patients with rheumatoid arthritis over 48 weeks with switch to alternate therapy in patients with insufficient response.48 周时对应答不足的患者转换为替代治疗,对比乌帕替尼或阿达木单抗加甲氨蝶呤治疗类风湿关节炎患者 48 周的安全性和有效性。
Ann Rheum Dis. 2019 Nov;78(11):1454-1462. doi: 10.1136/annrheumdis-2019-215764. Epub 2019 Jul 30.
3
Therapeutic Targeting of the Janus Kinase/Signal Transducer and Activator of Transcription Pathway in Cutaneous T-Cell Lymphoma.
皮肤T细胞淋巴瘤中Janus激酶/信号转导及转录激活因子通路的治疗靶向作用
Cancers (Basel). 2025 Feb 7;17(4):568. doi: 10.3390/cancers17040568.
4
FDA-Approved Janus Kinase-Signal Transducer and Activator of Transcription (JAK-STAT) Inhibitors for Managing Rheumatoid Arthritis: A Narrative Review of the Literature.美国食品药品监督管理局(FDA)批准的用于治疗类风湿性关节炎的 Janus 激酶-信号转导子和转录激活子(JAK-STAT)抑制剂:文献综述
Cureus. 2024 May 9;16(5):e59978. doi: 10.7759/cureus.59978. eCollection 2024 May.
5
Metabolic effects of upadacitinib in patients with psoriasis and atopic dermatitis.乌帕替尼对银屑病和特应性皮炎患者的代谢影响。
Arch Dermatol Res. 2024 May 2;316(5):143. doi: 10.1007/s00403-024-02892-7.
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Efficacy and safety of upadacitinib for the treatment of moderate-to-severe atopic dermatitis: a systematic review and meta-analysis.乌帕替尼治疗中重度特应性皮炎的疗效和安全性:一项系统评价和荟萃分析。
Postepy Dermatol Alergol. 2023 Dec;40(6):725-733. doi: 10.5114/ada.2023.133820. Epub 2024 Jan 8.
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Mol Divers. 2024 Dec;28(6):4467-4513. doi: 10.1007/s11030-023-10794-5. Epub 2024 Jan 18.
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Potential applications of JAK inhibitors, clinically approved drugs against autoimmune diseases, in cancer therapy.JAK抑制剂(临床上已获批用于治疗自身免疫性疾病的药物)在癌症治疗中的潜在应用。
Front Pharmacol. 2024 Jan 3;14:1326281. doi: 10.3389/fphar.2023.1326281. eCollection 2023.
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Front Immunol. 2023 Oct 26;14:1271102. doi: 10.3389/fimmu.2023.1271102. eCollection 2023.
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Predicting crystal form stability under real-world conditions.预测实际条件下的晶体形式稳定性。
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Arthritis Rheumatol. 2019 Nov;71(11):1788-1800. doi: 10.1002/art.41032. Epub 2019 Aug 28.
4
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Lancet. 2019 Jun 8;393(10188):2303-2311. doi: 10.1016/S0140-6736(19)30419-2. Epub 2019 May 23.
5
Characterization of the Effect of Hepatic Impairment on Upadacitinib Pharmacokinetics.评估肝功能损害对乌帕替尼激酶动力学的影响。
J Clin Pharmacol. 2019 Sep;59(9):1188-1194. doi: 10.1002/jcph.1414. Epub 2019 Apr 11.
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Clin Pharmacokinet. 2019 Aug;58(8):1045-1058. doi: 10.1007/s40262-019-00739-3.
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J Clin Pharmacol. 2019 Jun;59(6):856-862. doi: 10.1002/jcph.1375. Epub 2019 Jan 11.
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Lancet. 2018 Jun 23;391(10139):2513-2524. doi: 10.1016/S0140-6736(18)31116-4. Epub 2018 Jun 18.
10
Safety and efficacy of upadacitinib in patients with rheumatoid arthritis and inadequate response to conventional synthetic disease-modifying anti-rheumatic drugs (SELECT-NEXT): a randomised, double-blind, placebo-controlled phase 3 trial.乌帕替尼治疗对常规合成改善病情抗风湿药物应答不足的类风湿关节炎患者的安全性和疗效(SELECT-NEXT):一项随机、双盲、安慰剂对照的 3 期临床试验。
Lancet. 2018 Jun 23;391(10139):2503-2512. doi: 10.1016/S0140-6736(18)31115-2. Epub 2018 Jun 18.