Targetable Pathways in Advanced Bladder Cancer: FGFR Signaling

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.

(2021) Milind M. Javle et al.   JOURNAL OF CLINICAL ONCOLOGY

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2021) Hyuna Sung et al.   CA-A CANCER JOURNAL FOR CLINICIANS

An adaptive, biomarker-directed platform study of durvalumab in combination with targeted therapies in advanced urothelial cancer

(2021) Thomas Powles et al.   NATURE MEDICINE

GZD824 overcomes FGFR1‐V561F/M mutant resistance in vitro and in vivo

(2021) Kaili Jiang et al.   Cancer Medicine

FORT-1: Phase II/III study of rogaratinib versus chemotherapy (CT) in patients (pts) with locally advanced or metastatic urothelial carcinoma (UC) selected based on FGFR1/3 mRNA expression.

(2020) David I. Quinn et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Study of AZD4547 in Patients With Tumors Harboring Aberrations in the FGFR Pathway: Results From the NCI-MATCH Trial (EAY131) Subprotocol W

(2020) Young K. Chae et al.   JOURNAL OF CLINICAL ONCOLOGY

Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study

(2020) Ghassan K Abou-Alfa et al.   LANCET ONCOLOGY

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models

(2020) Phillip C. C. Liu et al.   PLoS One

Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling

(2020) Evan K. Day et al.   Cell Reports

Treatment of muscle‐invasive and advanced bladder cancer in 2020

(2020) Vaibhav G. Patel et al.   CA-A CANCER JOURNAL FOR CLINICIANS

FGFR3 Mutation Status and FGFR3 Expression in a Large Bladder Cancer Cohort Treated by Radical Cystectomy: Implications for Anti-FGFR3 Treatment?†

(2020) Bas W.G. van Rhijn et al.   EUROPEAN UROLOGY

Pharmacological inhibition of FGFR modulates the metastatic immune microenvironment and promotes response to immune checkpoint blockade

(2020) Saeed S Akhand et al.   Cancer Immunology Research

FGF13 Is a Novel Regulator of NF-κB and Potentiates Pathological Cardiac Hypertrophy

(2020) Jia Sun et al.   iScience

FGFR Inhibition Overcomes Resistance to EGFR-targeted Therapy in Epithelial-like Cutaneous Carcinoma

(2020) Adrià Bernat-Peguera et al.   CLINICAL CANCER RESEARCH

Fierce-21: Phase II study of vofatmab (B-701), a selective inhibitor of FGFR3, as salvage therapy in metastatic urothelial carcinoma (mUC).

(2019) Andrea Necchi et al.   JOURNAL OF CLINICAL ONCOLOGY

Rogaratinib: A potent and selective pan‐FGFR inhibitor with broad antitumor activity in FGFR‐overexpressing preclinical cancer models

(2019) Sylvia Grünewald et al.   INTERNATIONAL JOURNAL OF CANCER

FIERCE-22: Clinical activity of vofatamab (V) a FGFR3 selective inhibitor in combination with pembrolizumab (P) in WT metastatic urothelial carcinoma, preliminary analysis.

(2019) Arlene O. Siefker-Radtke et al.   JOURNAL OF CLINICAL ONCOLOGY

A Nationwide Population Based Analysis of Organ-Confined Muscle-Invasive Bladder Cancer Patients Not Receiving Curative Intent Therapy in Sweden from 1997 to 2014.

(2019) Dan-Olle Westergren et al.   JOURNAL OF UROLOGY

Fibroblast Growth Factor Receptor 3 Alterations and Response to PD-1/PD-L1 Blockade in Patients with Metastatic Urothelial Cancer

(2019) Li Wang et al.   EUROPEAN UROLOGY

Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma

(2019) Yohann Loriot et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting FGFR overcomes EMT-mediated resistance in EGFR mutant non-small cell lung cancer

(2019) Sana Raoof et al.   ONCOGENE

The combined effect of FGFR inhibition and PD-1 blockade promotes tumor-intrinsic induction of antitumor immunity

(2019) Sangeetha Palakurthi et al.   Cancer Immunology Research

Rogaratinib in patients with advanced cancers selected by FGFR mRNA expression: a phase 1 dose-escalation and dose-expansion study

(2019) Martin Schuler et al.   LANCET ONCOLOGY

Oncogenic Signaling Pathways in The Cancer Genome Atlas

(2018) Francisco Sanchez-Vega et al.   CELL

Cell-of-Origin Patterns Dominate the Molecular Classification of 10,000 Tumors from 33 Types of Cancer

(2018) Katherine A. Hoadley et al.   CELL

Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor

(2018) Marie-Pierre Collin et al.   ChemMedChem

Cancer-mutation network and the number and specificity of driver mutations

(2018) Jaime Iranzo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Efficacy of BGJ398, a Fibroblast Growth Factor Receptor 1–3 Inhibitor, in Patients with Previously Treated Advanced Urothelial Carcinoma with FGFR3 Alterations

(2018) Sumanta K. Pal et al.   Cancer Discovery

FGFR3 mutation increases bladder tumourigenesis by suppressing acute inflammation

(2018) Mona Foth et al.   JOURNAL OF PATHOLOGY

A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma

(2017) Liqin Wang et al.   EUROPEAN UROLOGY

PPARgamma agonists rescue increased phosphorylation of FGF14 at S226 in the Tg2576 mouse model of Alzheimer's disease

(2017) Wei-Chun J. Hsu et al.   EXPERIMENTAL NEUROLOGY

Mutation in the FGFR1 tyrosine kinase domain or inactivation of PTEN is associated with acquired resistance to FGFR inhibitors in FGFR1-driven leukemia/lymphomas

(2017) John K. Cowell et al.   INTERNATIONAL JOURNAL OF CANCER

Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib

(2017) Jayaprakash D. Karkera et al.   MOLECULAR CANCER THERAPEUTICS

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

(2017) Timothy P.S. Perera et al.   MOLECULAR CANCER THERAPEUTICS

Fusions in solid tumours: diagnostic strategies, targeted therapy, and acquired resistance

(2017) Alison M. Schram et al.   Nature Reviews Clinical Oncology

Pembrolizumab as Second-Line Therapy for Advanced Urothelial Carcinoma

(2017) Joaquim Bellmunt et al.   NEW ENGLAND JOURNAL OF MEDICINE

A place for precision medicine in bladder cancer: targeting the FGFRs

(2016) Erica di Martino et al.   Future Oncology

Drug resistance originating from a TGF-β/FGF-2-driven epithelial-to-mesenchymal transition and its reversion in human lung adenocarcinoma cell lines harboring an EGFR mutation

(2016) RYOTA KURIMOTO et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Atezolizumab in patients with locally advanced and metastatic urothelial carcinoma who have progressed following treatment with platinum-based chemotherapy: a single-arm, multicentre, phase 2 trial

(2016) Jonathan E Rosenberg et al.   LANCET

A combinatorial strategy for treating KRAS-mutant lung cancer

(2016) Eusebio Manchado et al.   NATURE

Polarized localization of voltage-gated Na+channels is regulated by concerted FGF13 and FGF14 action

(2016) Juan Lorenzo Pablo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

FGF14 is a regulator of KCNQ2/3 channels

(2016) Juan Lorenzo Pablo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A phase I, first in human study of FP-1039 (GSK3052230), a novel FGF ligand trap, in patients with advanced solid tumors

(2015) A. W. Tolcher et al.   ANNALS OF ONCOLOGY

Comparative effectiveness of gemcitabine plus cisplatin versus methotrexate, vinblastine, doxorubicin, plus cisplatin as neoadjuvant therapy for muscle-invasive bladder cancer

(2015) Matthew D. Galsky et al.   CANCER

Detection, Characterization, and Inhibition of FGFR-TACC Fusions in IDH Wild-type Glioma

(2015) A. L. Di Stefano et al.   CLINICAL CANCER RESEARCH

Genomic Predictors of Survival in Patients with High-grade Urothelial Carcinoma of the Bladder

(2015) Philip H. Kim et al.   EUROPEAN UROLOGY

Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan–Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors

(2015) Josep Tabernero et al.   JOURNAL OF CLINICAL ONCOLOGY

Redesigning a Monospecific Anti-FGFR3 Antibody to Add Selectivity for FGFR2 and Expand Antitumor Activity

(2015) Y. Yin et al.   MOLECULAR CANCER THERAPEUTICS

The Fibroblast Growth Factor signaling pathway

(2015) David M. Ornitz et al.   Wiley Interdisciplinary Reviews-Developmental Biology

Abstract CT326: Phase I study of BGJ398, a selective pan-FGFR inhibitor in genetically preselected advanced solid tumors

(2015) Lecia V. Sequist et al.   CANCER RESEARCH

Drug Resistance via Feedback Activation of Stat3 in Oncogene-Addicted Cancer Cells

(2014) Ho-June Lee et al.   CANCER CELL

Acquired resistance to TKIs in solid tumours: learning from lung cancer

(2014) D. Ross Camidge et al.   Nature Reviews Clinical Oncology

The tumorigenic FGFR3-TACC3 gene fusion escapes miR-99a regulation in glioblastoma

(2013) Brittany C. Parker et al.   JOURNAL OF CLINICAL INVESTIGATION

Postnatal Soluble FGFR3 Therapy Rescues Achondroplasia Symptoms and Restores Bone Growth in Mice

(2013) S. Garcia et al.   Science Translational Medicine

Identification of Targetable FGFR Gene Fusions in Diverse Cancers

(2013) Yi-Mi Wu et al.   Cancer Discovery

AZD4547: An Orally Bioavailable, Potent, and Selective Inhibitor of the Fibroblast Growth Factor Receptor Tyrosine Kinase Family

(2012) P. R. Gavine et al.   CANCER RESEARCH

Fibroblast Growth Factor 13 Is a Microtubule-Stabilizing Protein Regulating Neuronal Polarization and Migration

(2012) Qing-Feng Wu et al.   CELL

βKlotho Is Required for Fibroblast Growth Factor 21 Effects on Growth and Metabolism

(2012) Xunshan Ding et al.   Cell Metabolism

Retrospective Analysis of Clinical Outcomes With Neoadjuvant Cisplatin-Based Regimens for Muscle-Invasive Bladder Cancer

(2012) Sumanta K. Pal et al.   Clinical Genitourinary Cancer

Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance

(2012) V Chell et al.   ONCOGENE

Transforming Fusions of FGFR and TACC Genes in Human Glioblastoma

(2012) D. Singh et al.   SCIENCE

Neoadjuvant chemotherapy with gemcitabine/cisplatin vs. methotrexate/vinblastine/doxorubicin/cisplatin for muscle-invasive urothelial carcinoma of the bladder: A retrospective analysis from the University of Southern California

(2012) Adrian S. Fairey et al.   UROLOGIC ONCOLOGY-SEMINARS AND ORIGINAL INVESTIGATIONS

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

(2011) Vito Guagnano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rapidly Acquired Resistance to EGFR Tyrosine Kinase Inhibitors in NSCLC Cell Lines through De-Repression of FGFR2 and FGFR3 Expression

(2010) Kathryn E. Ware et al.   PLoS One

The FGFRL1 Receptor Is Shed from Cell Membranes, Binds Fibroblast Growth Factors (FGFs), and Antagonizes FGF Signaling inXenopusEmbryos

(2009) Florian Steinberg et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice

(2009) Jing Qing et al.   JOURNAL OF CLINICAL INVESTIGATION

Mutant fibroblast growth factor receptor 3 induces intracellular signaling and cellular transformation in a cell type- and mutation-specific manner

(2009) E di Martino et al.   ONCOGENE

FGF-21/FGF-21 receptor interaction and activation is determined by βKlotho

(2007) Alexei Kharitonenkov et al.   JOURNAL OF CELLULAR PHYSIOLOGY