[關鍵詞]
[摘要]
轉化生長因子-β（TGF-β）信號通路在腫瘤發(fā)生和發(fā)展過程中起重要作用，是一個有良好發(fā)展前景的藥物靶點。galunisertib是禮來制藥公司研發(fā)的一類新型TGF-β受體I抑制劑，通過阻斷TGF-β信號通路來抑制腫瘤的生長、侵襲和轉移過程。在針對骨髓增生異常綜合征、原發(fā)性肝癌和膠質細胞瘤等腫瘤的臨床研究表明，galunisertib具有顯著的有效性和安全性。主要從藥物概況、相關背景、合成路線、藥理作用、臨床研究、安全性等方面進行介紹。
[Key word]
[Abstract]
Transforming growth factor-β (TGF-β) signaling pathway plays a crucial role in the evolution and progression in tumors, and has become a novel promising target for cancer chemotherapy. Galunisertib is a novel TGF-β receptor I inhibitor, which is developed by Eli Lilly and Company, can inhibit tumor growth, invasion and metastasis by blocking TGF-β signaling pathway. Clinical research towards myelodysplastic syndrome, hepatocellular carcinoma, and glioblastoma indicates that galunisertib shows favourable effectiveness and safety. The drug situation, background, route of synthesis, pharmacological action, clinical research, and safety of vibegron are reviewed in this paper.
[中圖分類號]
[基金項目]
國家自然科學基金資助項目（31670859）；中國醫(yī)學科學院醫(yī)學與健康科技創(chuàng)新工程經(jīng)費資助項目；中國醫(yī)學科學院中央級公益性科研院所基本科研業(yè)務費資助項目（2016ZX310068、2016ZX310198、2016RC310019、2016RC310017）；協(xié)和青年基金和中央高?；究蒲袠I(yè)務費專項（3332016100）；中國醫(yī)學科學院放射醫(yī)學研究所創(chuàng)新團隊基金（1650）；協(xié)和小規(guī)模特色辦學經(jīng)費（10023201601602）
