Targeting COPA to Enhance Erdafitinib Sensitivity in FGFR‐Altered Bladder Cancer
Sign Up to like & getrecommendations! Published in 2025 at "Advanced Science"
DOI: 10.1002/advs.202413209
Abstract: Fibroblast growth factor receptor (FGFR) family aberrations are common in urothelial cancer. The FGFR tyrosine kinase inhibitor erdafitinib has been approved for locally advanced or metastatic urothelial cancer with FGFR2/3 alterations. Despite the initial efficacy… read more here.
Keywords: cancer; fgfr; erdafitinib; altered bladder ... See more keywords
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00713
Abstract: Aberrant activation of FGFR has been linked to the pathogenesis of many tumor types. Selective inhibition of FGFR has emerged as a promising approach for cancer treatment. Herein, we describe the discovery of compound 38… read more here.
Keywords: potent selective; inhibitor; pemigatinib; fgfr ... See more keywords
DW14383 is an irreversible pan-FGFR inhibitor that suppresses FGFR-dependent tumor growth in vitro and in vivo.
Sign Up to like & getrecommendations! Published in 2020 at "Acta pharmacologica Sinica"
DOI: 10.1038/s41401-020-00567-3
Abstract: Fibroblast growth factor receptor (FGFR) is a promising anticancer target. Currently, most FGFR inhibitors lack sufficient selectivity and have nonnegligible activity against kinase insert domain receptor (KDR), limiting their feasibility due to the serious side… read more here.
Keywords: dw14383; fgfr; fgfr inhibitor; fgfr1 ... See more keywords
Benzimidazole–dioxoisoindoline conjugates as dual VEGFR-2 and FGFR-1 inhibitors: design, synthesis, biological investigation, molecular docking studies and ADME predictions
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DOI: 10.1039/d4ra05462h
Abstract: In this investigation, a new series of benzimidazole–dioxo(benzo)isoindoline hybrids 8a–o were rationally designed and synthesized. All the synthesized hits 8a–o were investigated for their VEGFR-2 inhibitory activity at 10 μM. The conjugates 8l and 8m… read more here.
Keywords: molecular docking; fgfr; investigation; cell ... See more keywords
Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma
Sign Up to like & getrecommendations! Published in 2020 at "Expert Opinion on Investigational Drugs"
DOI: 10.1080/13543784.2021.1864320
Abstract: ABSTRACT Introduction The fibroblast growth factor receptor (FGFR) pathway is essential in cell proliferation, differentiation, migration, and survival. Cancers such as intrahepatic cholangiocarcinoma (IHCA) have demonstrated alterations of FGFR allowing unregulated growth. Infigratinib (BGJ398) is… read more here.
Keywords: agent treatment; fgfr; treatment; intrahepatic cholangiocarcinoma ... See more keywords
Pemigatinib in cholangiocarcinoma with a FGFR2 rearrangement or fusion
Sign Up to like & getrecommendations! Published in 2022 at "Expert Review of Anticancer Therapy"
DOI: 10.1080/14737140.2022.2150168
Abstract: ABSTRACT Introduction Cholangiocarcinoma (CCA) accounts for approximately 3% of gastrointestinal malignancies and is associated with a high mortality rate. Recent progress in the understanding of cholangiocarcinoma tumorigenesis and molecular markers has led to the development… read more here.
Keywords: fgfr; fusion; cca; cholangiocarcinoma ... See more keywords
EPCT-10. DEBIO1347, AN ORAL FGFR INHIBITOR: RESULTS FROM A SINGLE CENTER STUDY IN RECURRENT/REFRACTORY FGFR ALTERED PEDIATRIC GLIOMAS
Sign Up to like & getrecommendations! Published in 2021 at "Neuro-Oncology"
DOI: 10.1093/neuonc/noab090.196
Abstract: Abstract Background Oncogenic driver alterations in FGFR are present in a subset of pediatric gliomas. Debio1347 is an orally available, highly selective FGFR 1–3 inhibitor that had a favorable safety profile and encouraging preliminary clinical… read more here.
Keywords: gliomas; fgfr; fgfr inhibitor; patient ... See more keywords
Inhibiting FGFR by toadflax reverses erlotinib resistance in nonsmall cell lung cancer.
Sign Up to like & getrecommendations! Published in 2024 at "Anti-cancer drugs"
DOI: 10.1097/cad.0000000000001649
Abstract: This study aims to demonstrate the effect of toadflax (bufalin) on erlotinib resistance in nonsmall cell lung cancer (NSCLC) by inhibiting the fibroblast growth factor receptor (FGFR). The microfluidic mobility transferase and caliper mobility-shift assays… read more here.
Keywords: cancer; fgfr; erlotinib resistance; hcc827 cells ... See more keywords
Abstract LB-C12: Derazantinib (DZB): A dual FGFR/CSF1R-inhibitor active in PDX-models of urothelial cancer
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-19-lb-c12
Abstract: Background: DZB is an oral small-molecule Fibroblast Growth Factor Receptor 1/2/3 inhibitor (FGFRi) with clinically relevant activity in FGFR2-fusion cholangiocarcinoma. Extensive kinase profiling identified Colony-Stimulating Factor 1 receptor (CSF1R) as an additional anti-cancer target for… read more here.
Keywords: urothelial cancer; fgfr; csf1r; csf1r inhibitor ... See more keywords
Abstract 2870: A specific pan-FGFR inhibitor has antitumor activity against prostate cancer patient derived xenografts, PDX, expressing high FGFR1
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-2870
Abstract: Prostate Cancer (PCa) is one of the most commonly diagnosed malignancies in men. Patients with advanced metastatic PCa have effective treatment options, but none of them are curative. Androgen deprivation is the most effective therapy,… read more here.
Keywords: therapy; fgfr; prostate cancer; antitumor activity ... See more keywords
Abstract 2929: Radiosensitization of head and neck cancer by FGFR inhibition
Sign Up to like & getrecommendations! Published in 2019 at "Tumor Biology"
DOI: 10.1158/1538-7445.am2019-2929
Abstract: Objective: Fibroblast growth factor receptors are frequently amplified or overexpressed in head and neck squamous cell carcinomas (HNSCC). We assessed the potential of a selective FGFR-kinase inhibitor, AZD4547, to act as a radiosensitizer in head… read more here.
Keywords: cancer; fgfr inhibition; cell; fgfr ... See more keywords