Ocular Surface Center, Bascom Palmer Eye Institute, University of Miami Miller School of Medicine, Miami, FL, USA.
Ocular Surface Center, Department of Ophthalmology, Baylor College of Medicine, Houston, TX, USA.
Ocul Surf. 2016 Apr;14(2):207-15. doi: 10.1016/j.jtos.2016.01.001. Epub 2016 Jan 22.
The etiology of dry eye disease (DED) is complex and not yet fully understood, but the disease is now recognized as being associated with ocular surface inflammation. The latest advances in the understanding of the pathophysiology of DED have directed the focus of recent drug development to target the inflammatory pathways involved in the disease. Lifitegrast is a novel small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), thus lessening overall inflammatory responses. This review highlights the role of T cells and integrins in the inflammatory process involved in the pathophysiology of DED and outlines the scientific rationale for the role of lifitegrast. In addition, the preclinical development, pharmacological properties, clinical efficacy, and safety of lifitegrast are described.
干眼症(DED)的病因复杂,目前尚未完全阐明,但该疾病现已被认为与眼表面炎症有关。对 DED 病理生理学的最新认识使最近药物研发的重点转向针对疾病相关炎症途径的靶向治疗。利福平是一种新型小分子整合素拮抗剂,通过阻断两种重要细胞表面蛋白(淋巴细胞功能相关抗原 1 和细胞间黏附分子 1)的结合来抑制 T 细胞介导的炎症,从而减轻整体炎症反应。本文重点介绍 T 细胞和整合素在 DED 病理生理学涉及的炎症过程中的作用,并概述利福平的作用的科学依据。此外,还描述了利福平的临床前开发、药理学特性、临床疗效和安全性。