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
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
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
Abstract PD4-01: The role of FGF/FGFR axis in resistance to SERDs and CDK4/6 inhibitors in ER+ breast cancer
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.sabcs17-pd4-01
Abstract: Approximately 70% of breast cancers express the estrogen receptor (ER), and estrogen signaling drives breast cancer cell growth and progression. ER-directed therapies are commonly used to treat ER+ breast cancer and have improved survival for… read more here.
Keywords: fgfr; breast cancer; resistance; cancer ... See more keywords
Rogaratinib treatment of patients with advanced urothelial carcinomas prescreened for tumor FGFR mRNA expression.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2018.36.6_suppl.494
Abstract: 494Background: Activation of FGFR signaling is involved in a variety of malignancies including advanced urothelial cancer (UC). Rogaratinib is an oral pan-FGFR kinase inhibitor. We report here the results from a phase I expansion cohort… read more here.
Keywords: fgfr; fgfr1 mrna; advanced urothelial; patients advanced ... See more keywords
Signaling Pathway and Small-Molecule Drug Discovery of FGFR: A Comprehensive Review
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2022.860985
Abstract: Targeted therapy is a groundbreaking innovation for cancer treatment. Among the receptor tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered substantial attention as promising therapeutic targets due to their fundamental biological functions and frequently… read more here.
Keywords: small molecule; fgfr; signaling pathway; review ... See more keywords