2021年1月22日 · Final results from a phase II study of infigratinib (BGJ398), an FGFR-selective tyrosine kinase inhibitor, in patients with previously treated advanced cholangiocarcinoma harboring an FGFR2 gene fusion or rearrangement.. JCO 39, 265-265 (2021).

Infigratinib (BGJ-398; NVP-BGJ398) is a potent inhibitor of the FGFR family with IC50 s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Infigratinib (BGJ-398) 抑制 FGFR1、FGFR2 和 FGFR3，IC 50 =~1 nM，抑制 FGFR3 K650E，IC 50 =4.9 nM，抑制 FGFR4，IC 50 =60 nM。

2021年8月3日 · Infigratinib is a selective, ATP-competitive inhibitor of fibroblast growth factor receptors. We aimed to evaluate the antitumour activity of infigratinib in patients with locally advanced or metastatic cholangiocarcinoma, FGFR2 …

2018年1月20日 · Fibroblast growth factor receptor 2 ( FGFR2) fusions/translocations are present in 13% to 17% of intrahepatic cholangiocarcinomas. BGJ398, an orally bioavailable, selective pan-FGFR kinase inhibitor, has shown preliminary …

2023年6月20日 · Infigratinib是一种口服的、ATP竞争性的成纤维细胞生长因子受体酪氨酸激酶抑制剂（TKI），靶向纤维细胞生长因子受体（FGFR）蛋白，阻断下游活性。 Infigratinib. 在临床研究中，infigratinib在胆管癌中显示出具有临床意义的肿瘤缩小率（客观缓解率）和反应持续时间。 2021 年 5 月，FDA加速批准infigratinib用于治疗先前接受过治疗的局部晚期或转移性胆管癌患者，这些患者具有FGFR2融合或重排。 然而，2022 年 10 月，联拓生物称其合作伙伴BridgeBio …

nfigratinib（BGJ398）是一种口服给药的选择性成纤维细胞生长因子受体（FGFR）酪氨酸激酶抑制剂，2020年1月初被FDA授予快速通道资格。 II期研究发现， 既往化疗失败、FGFR2融合的晚期胆管癌患者接受Infigratinib治…

2017年1月10日 · Antitumor activity (seven partial responses [six confirmed]) was demonstrated with BGJ398 doses ≥ 100 mg in patients with FGFR1-amplified sqNSCLC and FGFR3-mutant bladder/urothelial cancer. Conclusion BGJ398 at the MTD/RP2D had a tolerable and manageable safety profile and showed antitumor activity in several tumor types, including FGFR1 ...

Infigratinib is a selective, ATP-competitive inhibitor of fibroblast growth factor receptors. We aimed to evaluate the antitumour activity of infigratinib in patients with locally advanced or metastatic cholangiocarcinoma, FGFR2 alterations, and previous gemcitabine-based treatment.

2016年11月21日 · BGJ398, an orally bioavailable, selective FGFR1 to 3 inhibitor (half maximal inhibitory concentration values range from 0.9 to 1.4 nM for FGFR1-3 to 60 nM for FGFR4), 19 inhibits proliferation and tumor growth in preclinical cancer models bearing FGFR1-3 genetic alterations. 19,20

2017年12月3日 · bgj398是一个口服的、选择性泛fgfr激酶抑制剂，在动物实验中显示出较好的活性。在早期的临床试验中，bgj398显示出较好的安全性和抗肿瘤活性，常见的副作用包括高磷血症、便秘、食欲减低和胃炎。