Therapeutic advances in small-molecule drugs for moderate-to-severe ulcerative colitis

doi:10.12092/j.issn.1009-2501.2026.03.011

Abstract

Abstract:

Ulcerative colitis (UC) is a chronic non-infectious inflammation primarily affecting the colon and rectum, characterised by continuous inflammation and ulceration of the intestinal mucosal layer. In recent years, with deepening research into the pathogenesis of UC, treatment strategies have progressively shifted towards precision targeted therapy at the molecular level. Small-molecule drugs, owing to their distinct advantages such as convenient administration, lack of immunogenicity, and short half-life, demonstrate significant potential in the treatment of moderate-to-severe UC. This review summarises therapeutic advances in small-molecule drugs for moderate-to-severe UC, focusing on representative compounds and their clinical trial outcomes in recent years.

Key words: moderate-to-severe ulcerative colitis, small-molecule drugs, JAK/STAT signalling pathway, S1P/S1PR signalling pathway

CLC Number:

R574.1
R969

Furui WANG, Tian HUANG, Wenli JIANG, Zenan HU. Therapeutic advances in small-molecule drugs for moderate-to-severe ulcerative colitis[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2026, 31(3): 392-399.

Figures/Tables 3

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药物名称	作用机制	用法	获批情况	全球阶段	中国阶段
Tofacitinib	JAK抑制剂	口服	中重度UC（2018，FDA）	批准上市	暂未发现相关报道
Filgotinib	选择性JAK1抑制剂	口服	中重度UC（2021，EMA）	批准上市	Ⅲ期临床
Upadacitinib	选择性JAK1抑制剂	口服	中重度UC（2022，FDA）	批准上市	批准上市
Ozanimod	S1PR调节剂	口服	中重度UC（2021，FDA）	批准上市	批准上市
Etrasimod	S1PR调节剂	口服	中重度UC（2023，FDA）	批准上市	Ⅲ期临床

药物名称	作用机制	用法	获批情况	全球阶段	中国阶段
Tofacitinib	JAK抑制剂	口服	中重度UC（2018，FDA）	批准上市	暂未发现相关报道
Filgotinib	选择性JAK1抑制剂	口服	中重度UC（2021，EMA）	批准上市	Ⅲ期临床
Upadacitinib	选择性JAK1抑制剂	口服	中重度UC（2022，FDA）	批准上市	批准上市
Ozanimod	S1PR调节剂	口服	中重度UC（2021，FDA）	批准上市	批准上市
Etrasimod	S1PR调节剂	口服	中重度UC（2023，FDA）	批准上市	Ⅲ期临床