瑞特西替尼：首次批准。
Ritlecitinib: First Approval.
机构信息
Springer Nature, Mairangi Bay, Private Bag 65901, Auckland, 0754, New Zealand.
出版信息
Drugs. 2023 Sep;83(14):1315-1321. doi: 10.1007/s40265-023-01928-y.
Abstract
Ritlecitinib (LITFULO), an orally administered kinase inhibitor, is being developed by Pfizer for the treatment of alopecia areata, vitiligo, ulcerative colitis and Crohn's disease. On 23 June 2023, ritlecitinib received approval in the USA for the treatment of severe alopecia areata in adults and adolescents 12 years and older. Ritlecitinib was approved in Japan on 26 June 2023 for the treatment of alopecia areata (limited to intractable cases involving widespread hair loss). Ritlecitinib has also received a positive opinion in the EU and is under regulatory review in the UK and China. This article summarizes the milestones in the development of ritlecitinib leading to this first approval for severe alopecia areata.
摘要
利特昔替尼（LITFULO）是一种口服激酶抑制剂，由辉瑞公司开发，用于治疗斑秃、白癜风、溃疡性结肠炎和克罗恩病。2023 年 6 月 23 日，利特昔替尼获得美国批准，用于治疗成人和 12 岁及以上青少年的重度斑秃。2023 年 6 月 26 日，利特昔替尼在日本获批用于治疗斑秃（仅限于涉及广泛脱发的难治性病例）。利特昔替尼在欧盟也获得了积极意见，正在英国和中国接受监管审查。本文总结了利特昔替尼开发的里程碑事件，最终使其获得了重度斑秃的首次批准。
相似文献
1
Ritlecitinib: First Approval.瑞特西替尼：首次批准。
Drugs. 2023 Sep;83(14):1315-1321. doi: 10.1007/s40265-023-01928-y.
2
LITFULO (Ritlecitinib) Capsules: A Janus Kinase 3 Inhibitor for the Treatment of Severe Alopecia Areata.利特福卢（瑞特替尼）胶囊：一种用于治疗严重斑秃的 Janus 激酶 3 抑制剂。
Skinmed. 2023 Dec 5;21(6):434-438. eCollection 2023.
3
Efficacy and safety of ritlecitinib in adults and adolescents with alopecia areata: a randomised, double-blind, multicentre, phase 2b-3 trial.利特昔替尼治疗成人和青少年斑秃的疗效和安全性：一项随机、双盲、多中心、2b-3 期临床试验。
Lancet. 2023 May 6;401(10387):1518-1529. doi: 10.1016/S0140-6736(23)00222-2. Epub 2023 Apr 14.
4
Evaluating the Therapeutic Potential of Ritlecitinib for the Treatment of Alopecia Areata.评估利特昔替尼治疗斑秃的治疗潜力。
Drug Des Devel Ther. 2022 Feb 17;16:363-374. doi: 10.2147/DDDT.S334727. eCollection 2022.
5
Ritlecitinib: an investigational drug for the treatment of moderate to severe alopecia areata.利特昔替尼：一种用于治疗中度至重度斑秃的研究药物。
Expert Opin Investig Drugs. 2021 Dec;30(12):1169-1174. doi: 10.1080/13543784.2021.2012149. Epub 2021 Dec 20.
6
Evolution of Ritlecitinib Population Pharmacokinetic Models During Clinical Drug Development.利特昔替尼群体药代动力学模型在临床药物研发中的演变。
Clin Pharmacokinet. 2023 Dec;62(12):1765-1779. doi: 10.1007/s40262-023-01318-3. Epub 2023 Nov 2.
7
A plain language summary on ritlecitinib treatment for adults and adolescents with alopecia areata.关于 ritlecitinib 治疗成人和青少年斑秃的通俗易懂的总结。
Immunotherapy. 2023 Oct;15(14):1093-1103. doi: 10.2217/imt-2023-0069. Epub 2023 Jul 5.
8
Efficacy and safety of ritlecitinib in adolescents with alopecia areata: Results from the ALLEGRO phase 2b/3 randomized, double-blind, placebo-controlled trial.利特昔替尼治疗青少年斑秃的疗效和安全性：ALLEGRO 期 2b/3 随机、双盲、安慰剂对照试验的结果。
Pediatr Dermatol. 2023 Nov-Dec;40(6):1003-1009. doi: 10.1111/pde.15378. Epub 2023 Jul 17.
9
A phase 2a randomized, placebo-controlled study to evaluate the efficacy and safety of the oral Janus kinase inhibitors ritlecitinib and brepocitinib in alopecia areata: 24-week results.一项评估口服 Janus 激酶抑制剂 ritlecitinib 和 brepocitinib 治疗斑秃的疗效和安全性的 2a 期随机、安慰剂对照研究：24 周结果。
J Am Acad Dermatol. 2021 Aug;85(2):379-387. doi: 10.1016/j.jaad.2021.03.050. Epub 2021 Mar 20.
10
Ritlecitinib (Litfulo) for severe alopecia areata.利特昔替尼（Litfulo）用于治疗重度斑秃。
Med Lett Drugs Ther. 2023 Nov 27;65(1690):185-186. doi: 10.58347/tml.2023.1690a.
引用本文的文献
1
Effective virtual screening strategy toward JAK3 covalent inhibitors: combining multi‑conformational consensus calculation with covalent docking.针对JAK3共价抑制剂的有效虚拟筛选策略：将多构象共识计算与共价对接相结合。
Mol Divers. 2025 Aug 21. doi: 10.1007/s11030-025-11329-w.
2
A twist in the tale: shifting from covalent targeting of a tyrosine in JAK3 to a lysine in MK2.故事的转折：从共价靶向JAK3中的酪氨酸转变为靶向MK2中的赖氨酸。
RSC Med Chem. 2025 Aug 1. doi: 10.1039/d5md00440c.
3
Is Intralesional Methotrexate an Effective Alternative to Intralesional Triamcinolone in Alopecia Areata? Findings From a Randomized Controlled Trial.病灶内注射甲氨蝶呤在斑秃治疗中是病灶内注射曲安奈德的有效替代方法吗？一项随机对照试验的结果
J Cosmet Dermatol. 2025 Aug;24(8):e70367. doi: 10.1111/jocd.70367.
4
Janus kinase inhibitors for alopecia areata: a review of clinical data.用于斑秃的Janus激酶抑制剂：临床数据综述
Front Immunol. 2025 May 13;16:1577115. doi: 10.3389/fimmu.2025.1577115. eCollection 2025.
5
Advancing Covalent Ligand and Drug Discovery beyond Cysteine.超越半胱氨酸推进共价配体与药物发现
Chem Rev. 2025 Jul 23;125(14):6653-6684. doi: 10.1021/acs.chemrev.5c00001. Epub 2025 May 22.
6
Polypharmacology: new drugs in 2023-2024.多靶点药理学：2023 - 2024年的新药
Pharmacol Rep. 2025 Jun;77(3):543-560. doi: 10.1007/s43440-025-00715-8. Epub 2025 Mar 17.
7
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.
8
The Stability-Indicating Ultra High-Performance Liquid Chromatography with Diode Array Detector and Tandem Mass Spectrometry Method Applied for the Forced Degradation Study of Ritlecitinib: An Appraisal of Green and Blue Metrics.采用二极管阵列检测器和串联质谱的稳定性指示超高效液相色谱法用于利特昔替尼的强制降解研究：绿色和蓝色指标评估
Pharmaceuticals (Basel). 2025 Jan 17;18(1):124. doi: 10.3390/ph18010124.
9
Mechanisms of autophagy and their implications in dermatological disorders.自噬的机制及其在皮肤科疾病中的意义。
Front Immunol. 2024 Nov 4;15:1486627. doi: 10.3389/fimmu.2024.1486627. eCollection 2024.
10
2D4, a humanized monoclonal antibody targeting CD132, is a promising treatment for systemic lupus erythematosus.2D4，一种针对 CD132 的人源化单克隆抗体，是治疗系统性红斑狼疮的一种有前途的方法。
Signal Transduct Target Ther. 2024 Nov 17;9(1):323. doi: 10.1038/s41392-024-02017-6.
本文引用的文献
1
Evolution of Symptoms After Ustekinumab Induction Therapy in Patients With Crohn's Disease.英夫利昔单抗诱导治疗克罗恩病患者症状的演变。
Clin Gastroenterol Hepatol. 2024 Jan;22(1):144-153.e2. doi: 10.1016/j.cgh.2023.06.014. Epub 2023 Jun 28.
2
Efficacy and safety of ritlecitinib in adults and adolescents with alopecia areata: a randomised, double-blind, multicentre, phase 2b-3 trial.利特昔替尼治疗成人和青少年斑秃的疗效和安全性：一项随机、双盲、多中心、2b-3 期临床试验。
Lancet. 2023 May 6;401(10387):1518-1529. doi: 10.1016/S0140-6736(23)00222-2. Epub 2023 Apr 14.
3
Evaluation of the effect of ritlecitinib on the pharmacokinetics of caffeine in healthy participants.评估利特昔替尼对健康参与者体内咖啡因药代动力学的影响。
Br J Clin Pharmacol. 2023 Jul;89(7):2208-2215. doi: 10.1111/bcp.15695. Epub 2023 Mar 2.
4
Efficacy and safety of oral ritlecitinib for the treatment of active nonsegmental vitiligo: A randomized phase 2b clinical trial.口服瑞特替尼治疗活动性非节段性白癜风的疗效和安全性：一项随机 2b 期临床试验。
J Am Acad Dermatol. 2023 Feb;88(2):395-403. doi: 10.1016/j.jaad.2022.11.005. Epub 2022 Nov 9.
5
Safety and Efficacy of Ritlecitinib and Brepocitinib in Alopecia Areata: Results from the Crossover Open-Label Extension of the ALLEGRO Phase 2a Trial.利特昔替尼和布雷西替尼治疗斑秃的安全性和有效性：ALLEGRO 2a期试验交叉开放标签扩展研究结果
JID Innov. 2022 Sep 7;2(6):100156. doi: 10.1016/j.xjidi.2022.100156. eCollection 2022 Nov.
6
Maintenance, withdrawal, and re-treatment with ritlecitinib and brepocitinib in patients with alopecia areata in a single-blind extension of a phase 2a randomized clinical trial.在一项2a期随机临床试验的单盲扩展试验中，对斑秃患者使用利特昔替尼和布雷西替尼进行维持、撤药及再治疗。
J Am Acad Dermatol. 2022 Aug;87(2):390-393. doi: 10.1016/j.jaad.2021.12.008. Epub 2021 Dec 13.
7
A phase 2a randomized, placebo-controlled study to evaluate the efficacy and safety of the oral Janus kinase inhibitors ritlecitinib and brepocitinib in alopecia areata: 24-week results.一项评估口服 Janus 激酶抑制剂 ritlecitinib 和 brepocitinib 治疗斑秃的疗效和安全性的 2a 期随机、安慰剂对照研究：24 周结果。
J Am Acad Dermatol. 2021 Aug;85(2):379-387. doi: 10.1016/j.jaad.2021.03.050. Epub 2021 Mar 20.
8
PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor.PF-06651600，一种双重 JAK3/TEC 家族激酶抑制剂。
ACS Chem Biol. 2019 Jun 21;14(6):1235-1242. doi: 10.1021/acschembio.9b00188. Epub 2019 May 22.
9
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.一种JAK3选择性抑制剂的发现：JAK3选择性抑制相对于泛JAK或JAK1选择性抑制的功能差异
ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. doi: 10.1021/acschembio.6b00677. Epub 2016 Nov 10.
Zotero 插件