Historically, the main classes of drug targets have been receptors, enzymes, ion channels and transporters. However, owing largely to the rise of antibody-based therapies in the past two decades, soluble protein ligands such as inflammatory cytokines have become an increasingly important class of drug targets. In this Review, we analyse drugs targeting ligands that have reached clinical development at some point since 1992. We identify 291 drugs that target 99 unique ligands, and we discuss trends in the characteristics of the ligands, drugs and indications for which they have been tested. In the last 5 years, the number of ligand-targeting drugs approved by the FDA has doubled to 34, while the number of clinically validated ligand targets has doubled to 22. Cytokines and growth factors are the predominant types of targeted ligands (70%), and inflammation and autoimmune disorders, cancer and ophthalmological diseases are the top therapeutic areas for both approved agents and agents in clinical studies, reflecting the central role of cytokine and/or growth factor pathways in such diseases.

历史上，药物靶点的主要类别是受体、酶、离子通道和转运蛋白。然而，很大程度上由于过去二十年基于抗体的疗法的兴起，可溶性蛋白配体（如炎性细胞因子）已成为越来越重要的一类药物靶点。在这篇综述中，我们分析了自 1992 年以来已达到临床开发阶段的靶向配体的药物。我们确定了靶向 99 个独特配体的 291 种药物，并讨论了配体、药物和已测试适应症的特征趋势. 在过去 5 年中，FDA 批准的配体靶向药物数量翻了一番，达到 34 个，而临床验证的配体靶点数量翻了一番，达到 22 个。细胞因子和生长因子是靶向配体的主要类型（70%） ,