Futibatinib: A Potent and Irreversible Inhibitor of Fibroblast Growth Factor Receptors for Treatment of the Bile Duct Cancer

被引:2
|
作者
De, Surya K. [1 ,2 ]
机构
[1] Conju Probe, Dept Chem, San Diego, CA 92121 USA
[2] Bharath Univ, Chennai 600126, Tamil Nadu, India
关键词
Cholangiocarcinoma; futibatinib; fibroblast growth factor receptor; pharmacodynamics; pharmacokinetics; drug interactions;
D O I
10.2174/0929867330666230416152913
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Cholangiocarcinoma is a rare type of cancer. Futibatinib is an irreversible, potent, selective inhibitor of fibroblast growth factor receptors (FGFR 1-4). On September 30, 2022, the US FDA first approved futibatinib to treat adult patients with bile duct cancer whose disease is unresectable, locally advanced, or metastatic intrahepatic cholangiocarcinoma harboring fibroblast growth factor receptor 2 (FGFR2) gene mutations or other classes of rearrangements. The approval of this medicine was based on phase 3 clinical trial results including an overall response rate (ORR) of 42% and a duration of response (DoR) of 9.7 months. This short perspective summarizes Futibatinib's synthesis, physicochemical properties, dosage, route of administration, mechanism of action, binding mode, pharmacodynamics, pharmacokinetics, drug interactions, adverse events, and possible mechanism of resistance.
引用
收藏
页码:666 / 670
页数:5
相关论文
共 50 条
  • [41] Sequential increases in the intrahepatic expression of epidermal growth factor, basic fibroblast growth factor, and transforming growth factor beta in a bile duct ligated rat model of cirrhosis
    Napoli, J
    Prentice, D
    Niinami, C
    Bishop, GA
    Desmond, P
    McCaughan, GW
    HEPATOLOGY, 1997, 26 (03) : 624 - 633
  • [42] Fibroblast growth factor and epidermal growth factor receptors in ligament healing
    Panossian, V
    Liu, SH
    Lane, JM
    Finerman, GAM
    CLINICAL ORTHOPAEDICS AND RELATED RESEARCH, 1997, (342) : 173 - 180
  • [43] Fibroblast growth factor 23 and its receptors
    Yu, XJ
    White, KE
    THERAPEUTIC APHERESIS AND DIALYSIS, 2005, 9 (04) : 308 - 312
  • [44] Roles of Fibroblast Growth Factor Receptors in Carcinogenesis
    Haugsten, Ellen Margrethe
    Wiedlocha, Antoni
    Olsnes, Sjur
    Wesche, Jorgen
    MOLECULAR CANCER RESEARCH, 2010, 8 (11) : 1439 - 1452
  • [45] Cellular signaling by fibroblast growth factor receptors
    Eswarakumar, VP
    Lax, I
    Schlessinger, J
    CYTOKINE & GROWTH FACTOR REVIEWS, 2005, 16 (02) : 139 - 149
  • [46] Targeting fibroblast growth factor receptors in rhabdomyosarcoma
    Alijaj, Nagjie
    Moutel, Sandrine
    Gray, Maxim
    Roveri, Maurizio
    Manzella, Gabriele
    Wachtel, Marco
    Perez, Franck
    Schafer, Beat
    Bernasconi, Michele
    CANCER RESEARCH, 2019, 79 (13)
  • [47] FINGERING FIBROBLAST GROWTH-FACTOR RECEPTORS
    不详
    NATURE GENETICS, 1994, 8 (01) : 1 - 2
  • [48] Collagen-binding fibroblast growth factor ameliorates liver fibrosis in murine bile duct ligation injury
    Shi, Qiangqiang
    Wei, Susu
    Li, Zhi Chao
    Xu, Jing
    Li, Yaxin
    Guo, Chuanlong
    Wu, Xianggen
    Shi, Chunying
    Di, Guohu
    JOURNAL OF BIOMATERIALS APPLICATIONS, 2022, 37 (05) : 918 - 929
  • [49] IGA IS A BILE-DUCT GROWTH-FACTOR
    BOSCAMP, J
    FALLONFRIEDLANDER, S
    HORWITZ, M
    MORECKI, R
    GLASER, J
    PEDIATRIC RESEARCH, 1987, 21 (04) : A264 - A264
  • [50] Basic fibroblast growth factor receptors and their prognostic value in human breast cancer
    Blanckaert, VD
    Hebbar, M
    Louchez, MM
    Vilain, MO
    Schelling, ME
    Peyrat, JP
    CLINICAL CANCER RESEARCH, 1998, 4 (12) : 2939 - 2947