转化生长因子-β(TGF-β)信号通路在肿瘤发生和发展过程中起重要作用,是一个有良好发展前景的药物靶点。galunisertib是礼来制药公司研发的一类新型TGF-β受体Ⅰ抑制剂,通过阻断TGF-β信号通路来抑制肿瘤的生长、侵袭和转移过程。在针对骨髓增生异常综合征、原发性肝癌和胶质细胞瘤等肿瘤的临床研究表明,galunisertib具有显著的有效性和安全性。主要从药物概况、相关背景、合成路线、药理作用、临床研究、安全性等方面进行介绍。 Transforming growth factor-β (TGF-β) signaling plays an important role in tumorigenesis and progression and is a promising drug target. Galunisertib is a new class of TGF-β receptor I inhibitors developed by Eli Lilly and Company that inhibits tumor growth, invasion and metastasis by blocking the TGF-β signaling pathway. Clinical studies on tumors such as myelodysplastic syndrome, primary liver cancer and glioma have shown that galunisertib has significant efficacy and safety. Mainly from the drug profile, the relevant background, synthetic routes, pharmacological effects, clinical research, safety and other aspects are introduced.