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Editorial
. 2023 Sep 6;13(9):1964-1965.
doi: 10.1158/2159-8290.CD-23-0728.

FGFR Inhibition: Understanding and Overcoming Resistance

Abhishek Tripathi  1 , Daneng Li  1 , Sumanta K Pal  1
Affiliations
Editorial

FGFR Inhibition: Understanding and Overcoming Resistance

Abhishek Tripathi et al. Cancer Discov. .

Abstract

Facchinetti and colleagues provide key insights into the evolution of resistance to fibroblast growth factor receptor (FGFR) inhibitors, including the development of kinase domain mutations and activation of the PI3K-AKT signaling axis. In a separate study, Subbiah and colleagues report extensive preclinical data and initial clinical data for RLY-4008, an FGFR2-selective inhibitor that is poised to minimize toxicity and overcome resistance through greater potency and selectivity. See related article by Facchinetti et al., p. 1998 (5). See related article by Subbiah et al., p. 2012 (7).

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Comment on

  • RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.
    Subbiah V, Sahai V, Maglic D, Bruderek K, Touré BB, Zhao S, Valverde R, O'Hearn PJ, Moustakas DT, Schönherr H, Gerami-Moayed N, Taylor AM, Hudson BM, Houde DJ, Pal D, Foster L, Gunaydin H, Ayaz P, Sharon DA, Goyal L, Schram AM, Kamath S, Sherwin CA, Schmidt-Kittler O, Jen KY, Ricard F, Wolf BB, Shaw DE, Bergstrom DA, Watters J, Casaletto JB. Subbiah V, et al. Cancer Discov. 2023 Sep 6;13(9):2012-2031. doi: 10.1158/2159-8290.CD-23-0475. Cancer Discov. 2023. PMID: 37270847 Free PMC article.
  • Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer.
    Facchinetti F, Hollebecque A, Braye F, Vasseur D, Pradat Y, Bahleda R, Pobel C, Bigot L, Déas O, Florez Arango JD, Guaitoli G, Mizuta H, Combarel D, Tselikas L, Michiels S, Nikolaev SI, Scoazec JY, Ponce-Aix S, Besse B, Olaussen KA, Loriot Y, Friboulet L. Facchinetti F, et al. Cancer Discov. 2023 Sep 6;13(9):1998-2011. doi: 10.1158/2159-8290.CD-22-1441. Cancer Discov. 2023. PMID: 37377403 Free PMC article.

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