Recent advances of dual FGFR inhibitors as a novel therapy for cancer

Targeting Fibroblast Growth Factor Receptor (FGFR) and Phosphoinositide 3-kinase (PI3K) Signaling Pathways in Medulloblastoma Cell Lines

(2020) STEFAN HOLZHAUSER et al.   ANTICANCER RESEARCH

Dual-target kinase drug design: Current strategies and future directions in cancer therapy

(2020) Dejuan Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Understanding the adverse event experience in the S-TRAC adjuvant trial of sunitinib for high-risk renal cell carcinoma

(2020) Sarah Yenser Wood et al.   Future Oncology

The inhibition profiles of 4'‐acylpyrrole–5‐fluoroindolin‐2‐ones with a C‐3' side chain for VEGFR2, PDGFR‐β, and FGFR‐1 protein kinases

(2020) Jiann‐Jyh Huang et al.   JOURNAL OF THE CHINESE CHEMICAL SOCIETY

GZD824 as a FLT3, FGFR1 and PDGFRα Inhibitor Against Leukemia In Vitro and In Vivo

(2020) Yuting Wang et al.   Translational Oncology

Discovery of Dual FGFR4 and EGFR Inhibitors by Machine Learning and Biological Evaluation

(2020) Xingye Chen et al.   Journal of Chemical Information and Modeling

Nintedanib can be used safely and effectively for idiopathic pulmonary fibrosis with predicted forced vital capacity ≤ 50%: A multi-center retrospective analysis

(2020) Satoru Senoo et al.   PLoS One

Pazopanib-related secondary polycythemia in metastatic myxofibrosarcoma: A case report and review of the literature

(2020) Martina Fanelli et al.   JOURNAL OF ONCOLOGY PHARMACY PRACTICE

A phase Ib dose allocation study of oral administration of lucitanib given in combination with fulvestrant in patients with estrogen receptor-positive and FGFR1-amplified or non-amplified metastatic breast cancer

(2019) M. Campone et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

FGFR1 Cooperates with EGFR in Lung Cancer Oncogenesis, and Their Combined Inhibition Shows Improved Efficacy

(2019) Alvaro Quintanal-Villalonga et al.   Journal of Thoracic Oncology

Emerging protein kinase inhibitors for the treatment of multiple myeloma

(2019) Judith Lind et al.   EXPERT OPINION ON EMERGING DRUGS

Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models

(2019) Xia Peng et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Phase II randomised discontinuation trial of brivanib in patients with advanced solid tumours

(2019) Robin L. Jones et al.   EUROPEAN JOURNAL OF CANCER

Brivanib Exhibits Potential for Pharmacokinetic Drug–Drug Interactions and the Modulation of Multidrug Resistance through the Inhibition of Human ABCG2 Drug Efflux Transporter and CYP450 Biotransformation Enzymes

(2019) Jakub Hofman et al.   MOLECULAR PHARMACEUTICS

Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC

(2019) Zixin Xie et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold

(2018) Jian Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Resistance to EGFR inhibitors in non-small cell lung cancer: Clinical management and future perspectives

(2018) Chiara Tomasello et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors

(2018) Manman Wei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synergistic anti-angiogenic treatment effects by dual FGFR1 and VEGFR1 inhibition in FGFR1-amplified breast cancer

(2018) Kristina Golfmann et al.   ONCOGENE

Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer

(2018) Yuan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

(2018) Tim H. Holmström et al.   MOLECULAR CANCER THERAPEUTICS

Up-Regulated FGFR1 Expression as a Mediator of Intrinsic TKI Resistance in EGFR-Mutated NSCLC

(2018) Kristine Raaby Gammelgaard et al.   Translational Oncology

Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma

(2018) Qi Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Type IIA - Type IIB protein tyrosine kinase inhibitors hybridization as an efficient approach for potent multikinase inhibitor development: Design, synthesis, anti-proliferative activity, multikinase inhibitory activity and molecular modeling of novel indolinone-based ureides and amides

(2018) Wagdy M. Eldehna et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A phase II evaluation of brivanib in the treatment of persistent or recurrent carcinoma of the cervix: An NRG Oncology/Gynecologic Oncology Group study

(2017) John K. Chan et al.   GYNECOLOGIC ONCOLOGY

Targeting HSP90-HDAC6 Regulating Network Implicates Precision Treatment of Breast Cancer

(2017) Shiyi Yu et al.   International Journal of Biological Sciences

FGF2/FGFR1 regulates autophagy in FGFR1-amplified non-small cell lung cancer cells

(2017) Hong Yuan et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors

(2017) Ken A. Brameld et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tumour-associated macrophages as treatment targets in oncology

(2017) Alberto Mantovani et al.   Nature Reviews Clinical Oncology

Treatments for EGFR-mutant non-small cell lung cancer (NSCLC): The road to a success, paved with failures

(2017) Dae Ho Lee   PHARMACOLOGY & THERAPEUTICS

In Vitro and In Vivo Activity of Lucitanib in FGFR1/2 Amplified or Mutated Cancer Models

(2017) Federica Guffanti et al.   NEOPLASIA

Phase 1 study of ODM-203, a selective dual FGFR/VEGFR inhibitor, in patients with advanced solid tumours

(2016) J. Rodón et al.   ANNALS OF ONCOLOGY

FGFR antagonist induces protective autophagy in FGFR1-amplified breast cancer cell

(2016) Yi Chen et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The impact of multiple low-level BCR-ABL1 mutations on response to ponatinib

(2016) W. T. Parker et al.   BLOOD

Inhibition of histone deacetylases in cancer therapy: lessons from leukaemia

(2016) Elena Ceccacci et al.   BRITISH JOURNAL OF CANCER

Dual blockade of vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (FGF-2) exhibits potent anti-angiogenic effects

(2016) Dong Li et al.   CANCER LETTERS

Antitumor effect of FGFR inhibitors on a novel cholangiocarcinoma patient derived xenograft mouse model endogenously expressing an FGFR2-CCDC6 fusion protein

(2016) Yu Wang et al.   CANCER LETTERS

Targeting the fibroblast growth factor receptor family in cancer

(2016) Niamh Hallinan et al.   CANCER TREATMENT REVIEWS

FGFR inhibitors: Effects on cancer cells, tumor microenvironment and whole-body homeostasis (Review)

(2016) MASARU KATOH   INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE

Discovery of 3-(5′-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation

(2016) Wei Yan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cell adhesion and polarity in squamous cell carcinoma of the lung

(2016) Ester Bonastre et al.   JOURNAL OF PATHOLOGY

Immuno-oncologists eye up macrophage targets

(2016) Chris Morrison   NATURE REVIEWS DRUG DISCOVERY

Trichlorobenzene-substituted azaaryl compounds as novel FGFR inhibitors exhibiting potent antitumor activity in bladder cancer cells in vitro and in vivo

(2016) Chun-Han Chen et al.   Oncotarget

Dual Targeting of PDGFRα and FGFR1 Displays Synergistic Efficacy in Malignant Rhabdoid Tumors

(2016) Jocelyn P. Wong et al.   Cell Reports

Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy

(2016) S-M Kim et al.   Oncogenesis

Platelet-Derived Growth Factor Signaling in the Lung. From Lung Development and Disease to Clinical Studies

(2015) Nina Noskovičová et al.   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma

(2015) Shin Saito et al.   BMC CANCER

Phase 2 study of dovitinib in patients with metastatic or unresectable adenoid cystic carcinoma

(2015) Bhumsuk Keam et al.   CANCER

Targeting FGFR Signaling in Cancer

(2015) M. Touat et al.   CLINICAL CANCER RESEARCH

Histone deacetylases: structural determinants of inhibitor selectivity

(2015) Carmina Micelli et al.   DRUG DISCOVERY TODAY

Dovitinib (CHIR258, TKI258): structure, development and preclinical and clinical activity

(2015) Camillo Porta et al.   Future Oncology

Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer

(2015) Chee-Seng Tan et al.   LANCET ONCOLOGY

Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms

(2015) Diarmaid Hughes et al.   NATURE REVIEWS GENETICS

Targeting Angiogenesis in Cancer Therapy: Moving Beyond Vascular Endothelial Growth Factor

(2015) Y. Zhao et al.   ONCOLOGIST

Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold

(2015) Jian Liu et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Phase I/IIa study evaluating the safety, efficacy, pharmacokinetics, and pharmacodynamics of lucitanib in advanced solid tumors

(2014) J.- C. Soria et al.   ANNALS OF ONCOLOGY

Targeting Tumor-Associated Macrophages with Anti-CSF-1R Antibody Reveals a Strategy for Cancer Therapy

(2014) Carola H. Ries et al.   CANCER CELL

A phase II trial of brivanib in recurrent or persistent endometrial cancer: An NRG Oncology/Gynecologic Oncology Group Study

(2014) Matthew A. Powell et al.   GYNECOLOGIC ONCOLOGY

Discoidin Domain Receptor 2 Signaling Networks and Therapy in Lung Cancer

(2014) Leo S. Payne et al.   Journal of Thoracic Oncology

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

(2014) Katrina J. Falkenberg et al.   NATURE REVIEWS DRUG DISCOVERY

Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF, VEGF and PDGF Signaling

(2014) Ikuo Nakamura et al.   PLoS One

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

(2014) Li Tan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Genomic aberrations in the FGFR pathway: opportunities for targeted therapies in solid tumors

(2013) R. Dienstmann et al.   ANNALS OF ONCOLOGY

Discoidin Domain Receptors: Unique Receptor Tyrosine Kinases in Collagen-mediated Signaling

(2013) Hsueh-Liang Fu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phase III Randomized, Placebo-Controlled Study of Cetuximab Plus Brivanib Alaninate Versus Cetuximab Plus Placebo in Patients With Metastatic, Chemotherapy-Refractory, Wild-TypeK-RASColorectal Carcinoma: The NCIC Clinical Trials Group and AGITG CO.20 Trial

(2013) Lillian L. Siu et al.   JOURNAL OF CLINICAL ONCOLOGY

Brivanib Versus Sorafenib As First-Line Therapy in Patients With Unresectable, Advanced Hepatocellular Carcinoma: Results From the Randomized Phase III BRISK-FL Study

(2013) Philip J. Johnson et al.   JOURNAL OF CLINICAL ONCOLOGY

Beneficial effects of dual vascular endothelial growth factor receptor/fibroblast growth factor receptor inhibitor brivanib alaninate in cirrhotic portal hypertensive rats

(2013) Han-Chieh Lin et al.   JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY

Identification of GZD824 as an Orally Bioavailable Inhibitor That Targets Phosphorylated and Nonphosphorylated Breakpoint Cluster Region–Abelson (Bcr-Abl) Kinase and Overcomes Clinically Acquired Mutation-Induced Resistance against Imatinib

(2013) Xiaomei Ren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Personalized therapy on the horizon for squamous cell carcinoma of the lung

(2013) Han Sang Kim et al.   LUNG CANCER

Potential Advantages of CUDC-101, a Multitargeted HDAC, EGFR, and HER2 Inhibitor, in Treating Drug Resistance and Preventing Cancer Cell Migration and Invasion

(2013) J. Wang et al.   MOLECULAR CANCER THERAPEUTICS

The anticancer multi-kinase inhibitor dovitinib also targets topoisomerase I and topoisomerase II

(2012) Brian B. Hasinoff et al.   BIOCHEMICAL PHARMACOLOGY

The Clinical Effect of the Dual-Targeting Strategy Involving PI3K/AKT/mTOR and RAS/MEK/ERK Pathways in Patients with Advanced Cancer

(2012) T. Shimizu et al.   CLINICAL CANCER RESEARCH

Cancer Network Disruption by a Single Molecule Inhibitor Targeting Both Histone Deacetylase Activity and Phosphatidylinositol 3-Kinase Signaling

(2012) C. Qian et al.   CLINICAL CANCER RESEARCH

597 Pharmacokinetics of the Novel FGFR and VEGFR Inhibitor, E-3810, in Patients with Advanced Solid Tumors Participating to a Phase I/II Trial

(2012) M. Zangarini et al.   EUROPEAN JOURNAL OF CANCER

Population Pharmacokinetic/Pharmacodynamic Modeling to Assist Dosing Schedule Selection for Dovitinib

(2012) Xiaofeng Wang et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Identification of Enriched Driver Gene Alterations in Subgroups of Non-Small Cell Lung Cancer Patients Based on Histology and Smoking Status

(2012) She-Juan An et al.   PLoS One

E-3810 Is a Potent Dual Inhibitor of VEGFR and FGFR that Exerts Antitumor Activity in Multiple Preclinical Models

(2011) Ezia Bello et al.   CANCER RESEARCH

Discoidin domain receptor 2 is a critical regulator of epithelial–mesenchymal transition

(2011) Logan A. Walsh et al.   MATRIX BIOLOGY

Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents1

(2010) Aleem Gangjee et al.   BIOORGANIC & MEDICINAL CHEMISTRY

CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity

(2010) Cheng-Jung Lai et al.   CANCER RESEARCH

Macrophages, innate immunity and cancer: balance, tolerance, and diversity

(2010) Alberto Mantovani et al.   CURRENT OPINION IN IMMUNOLOGY

Metabolism, Excretion, and Pharmacokinetics of Oral Brivanib in Patients with Advanced or Metastatic Solid Tumors

(2010) T. Mekhail et al.   DRUG METABOLISM AND DISPOSITION

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

The emerging mechanisms of isoform-specific PI3K signalling

(2010) Bart Vanhaesebroeck et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

FGFR3 mutations in prostate cancer: association with low-grade tumors

(2009) Silvia Hernández et al.   MODERN PATHOLOGY

The regulation and function of Class III PI3Ks: novel roles for Vps34

(2008) Jonathan M. Backer   BIOCHEMICAL JOURNAL

Discovery of Brivanib Alaninate ((S)-((R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinase Inhibitor (BMS-540215)

(2008) Zhen-wei Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY

PI3K pathway alterations in cancer: variations on a theme

(2008) T L Yuan et al.   ONCOGENE