罗加替尼（BAY 1163877）的发现：一种泛 FGFR 抑制剂。
Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor.
机构信息
Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
Research Pharmacokinetics Group, Drug Discovery, Bayer AG, Germany.
出版信息
ChemMedChem. 2018 Mar 6;13(5):437-445. doi: 10.1002/cmdc.201700718. Epub 2018 Feb 16.
Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1-4) for oral application currently being investigated in phase 1 clinical trials for the treatment of cancer. In this publication, we report its discovery by de novo structure-based design and medicinal chemistry optimization together with its pharmacokinetic profile.
罗加替尼（BAY 1163877）是一种高效且选择性的小分子泛成纤维细胞生长因子受体（FGFR）抑制剂（FGFR1-4），可口服，目前正在进行临床 1 期试验，用于癌症治疗。在本出版物中，我们报告了通过从头基于结构的设计和药物化学优化以及药代动力学特征来发现它。
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