The Development of AXL Inhibitors in Lung Cancer: Recent Progress and Challenges

Ph I/II study of oral selective AXL inhibitor bemcentinib (BGB324) in combination with erlotinib in patients with advanced EGFRm NSCLC: End of trial update.

(2021) Lauren Averett Byers et al.   JOURNAL OF CLINICAL ONCOLOGY

ONO-7475, a novel AXL inhibitor, suppresses the adaptive resistance to initial EGFR-TKI treatment in EGFR-mutated non-small lung cancer

(2020) Naoko Okura et al.   CLINICAL CANCER RESEARCH

Gas6/Axl Signaling Pathway in the Tumor Immune Microenvironment

(2020) Mai Tanaka et al.   Cancers

570P A first-in-human phase I study of the AXL inhibitor DS-1205c in combination with gefitinib in subjects with EGFR-mutant NSCLC

(2020) M. Nishio et al.   ANNALS OF ONCOLOGY

Immuno-Oncological Efficacy of RXDX-106, a Novel Small Molecule Inhibitor of the TAM (TYRO3, AXL, MER) Family of Kinases

(2019) Yumi Yokoyama et al.   CANCER RESEARCH

A novel human anti‐ AXL monoclonal antibody attenuates tumor cell migration

(2019) Duan Yanting et al.   SCANDINAVIAN JOURNAL OF IMMUNOLOGY

AXL degradation in combination with EGFR-TKI can delay and overcome acquired resistance in human non-small cell lung cancer cells

(2019) Donghwa Kim et al.   Cell Death & Disease

DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model

(2019) Takeshi Jimbo et al.   Oncotarget

AXL Targeting Overcomes Human Lung Cancer Cell Resistance to NK- and CTL-Mediated Cytotoxicity

(2019) Stéphane Terry et al.   Cancer Immunology Research

S100A10 Is a Critical Mediator of GAS6/AXL–Induced Angiogenesis in Renal Cell Carcinoma

(2019) Yiren Xiao et al.   CANCER RESEARCH

AXL receptor tyrosine kinase as a promising anti-cancer approach: functions, molecular mechanisms and clinical applications

(2019) Chenjing Zhu et al.   Molecular Cancer

Cooperative targeting of melanoma heterogeneity with an AXL antibody-drug conjugate and BRAF/MEK inhibitors

(2018) Julia Boshuizen et al.   NATURE MEDICINE

Engineering Axl specific CAR and SynNotch receptor for cancer therapy

(2018) Jang Hwan Cho et al.   Scientific Reports

Abstract 827: Anti-tumor efficacy of BA3011, a novel Conditionally Active Biologic (CAB) anti-AXL-ADC

(2018) Leslie L. Sharp et al.   CANCER RESEARCH

Abstract 3759: Characterization of INCB081776, a potent and selective dual AXL/MER kinase inhibitor

(2018) Margaret Favata et al.   CANCER RESEARCH

Phase II open-label, multi-centre study of bemcentinib (BGB324), a first-in-class selective AXL inhibitor, in combination with pembrolizumab in patients with advanced NSCLC.

(2018) James Lorens et al.   JOURNAL OF CLINICAL ONCOLOGY

1506TiPPhase I study of the AXL inhibitor DS-1205c in combination with osimertinib in subjects with metastatic or unresectable EGFR-mutant NSCLC

(2018) D Planchard et al.   ANNALS OF ONCOLOGY

Activation of AXL as a Preclinical Acquired Resistance Mechanism Against Osimertinib Treatment in EGFR-Mutant Non–Small Cell Lung Cancer Cells

(2018) Kei Namba et al.   MOLECULAR CANCER RESEARCH

Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia

(2017) Masamichi Mori et al.   INVESTIGATIONAL NEW DRUGS

MA 02.01 Evidence of Clinical Activity of Sitravatinib in Combination with Nivolumab in NSCLC Patients Progressing on Prior Checkpoint Inhibitors

(2017) T. Leal et al.   Journal of Thoracic Oncology

Function of Axl receptor tyrosine kinase in non-small cell lung cancer (Review)

(2017) Guoan Zhang et al.   Oncology Letters

Abstract 566: BGB324, a selective small molecule inhibitor of the receptor tyrosine kinase AXL, enhances immune checkpoint inhibitor efficacy

(2016) Gro Gausdal et al.   CANCER RESEARCH

Phenotypic chemical screening using a zebrafish neural crest EMT reporter identifies retinoic acid as an inhibitor of epithelial morphogenesis

(2016) Laura Jimenez et al.   Disease Models & Mechanisms

Anexelekto (AXL) Increases Resistance to EGFR-TKI and Activation of AKT and ERK1/2 in Non-Small Cell Lung Cancer Cells

(2016) Yaqiong Tian et al.   ONCOLOGY RESEARCH

Axl receptor tyrosine kinase is a potential therapeutic target in renal cell carcinoma

(2015) H Yu et al.   BRITISH JOURNAL OF CANCER

Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors

(2015) S. Sinha et al.   CLINICAL CANCER RESEARCH

Preclinical combination of TP-0903, an AXL inhibitor and B-PAC-1, a procaspase-activating compound with ibrutinib in chronic lymphocytic leukemia

(2015) Viralkumar Patel et al.   LEUKEMIA & LYMPHOMA

Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma

(2015) Parag P. Patwardhan et al.   Oncotarget

Abstract 1747: BGB324, a selective small molecule Axl kinase inhibitor to overcome EMT-associated drug resistance in carcinomas: Therapeutic rationale and early clinical studies

(2015) Katarzyna Wnuk-Lipinska et al.   CANCER RESEARCH

Overcoming EMT-associated resistance to anti-cancer drugs via Src/FAK pathway inhibition

(2015) Catherine Wilson et al.   Oncotarget

Axl as a mediator of cellular growth and survival

(2015) Haley Axelrod et al.   Oncotarget

Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

(2014) Zheng Zhao et al.   ACS Chemical Biology

AXL Mediates Resistance to Cetuximab Therapy

(2014) T. M. Brand et al.   CANCER RESEARCH

Axl-altered microRNAs regulate tumorigenicity and gefitinib resistance in lung cancer

(2014) Y Wang et al.   Cell Death & Disease

The receptor tyrosine kinase Axl in cancer: Biological functions and therapeutic implications

(2013) Juliano D. Paccez et al.   INTERNATIONAL JOURNAL OF CANCER

Preclinical validation of AXL receptor as a target for antibody-based pancreatic cancer immunotherapy

(2013) W Leconet et al.   ONCOGENE

Higher Expression of Receptor Tyrosine Kinase Axl, and Differential Expression of its Ligand, Gas6, Predict Poor Survival in Lung Adenocarcinoma Patients

(2012) Masashi Ishikawa et al.   ANNALS OF SURGICAL ONCOLOGY

An Epithelial-Mesenchymal Transition Gene Signature Predicts Resistance to EGFR and PI3K Inhibitors and Identifies Axl as a Therapeutic Target for Overcoming EGFR Inhibitor Resistance

(2012) L. A. Byers et al.   CLINICAL CANCER RESEARCH

Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer

(2012) Zhenfeng Zhang et al.   NATURE GENETICS

Mer or Axl receptor tyrosine kinase inhibition promotes apoptosis, blocks growth and enhances chemosensitivity of human non-small cell lung cancer

(2012) R M A Linger et al.   ONCOGENE

Axl-dependent signalling: a clinical update

(2011) Vyacheslav A. Korshunov   CLINICAL SCIENCE

Design, Synthesis, and Biological Evaluation of a Series of Novel AXL Kinase Inhibitors

(2011) Alexis Mollard et al.   ACS Medicinal Chemistry Letters

Induction, regulation, and biologic function of Axl receptor tyrosine kinase in Kaposi sarcoma

(2010) R. Liu et al.   BLOOD

AXL Is an Essential Factor and Therapeutic Target for Metastatic Ovarian Cancer

(2010) E. B. Rankin et al.   CANCER RESEARCH

R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

(2010) S. J. Holland et al.   CANCER RESEARCH

Taking aim at Mer and Axl receptor tyrosine kinases as novel therapeutic targets in solid tumors

(2010) Rachel MA Linger et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

An anti-Axl monoclonal antibody attenuates xenograft tumor growth and enhances the effect of multiple anticancer therapies

(2010) X Ye et al.   ONCOGENE

Vimentin regulates EMT induction by Slug and oncogenic H-Ras and migration by governing Axl expression in breast cancer

(2010) K Vuoriluoto et al.   ONCOGENE

Axl as a potential therapeutic target in cancer: role of Axl in tumor growth, metastasis and angiogenesis

(2009) Y Li et al.   ONCOGENE

Axl is an essential epithelial-to-mesenchymal transition-induced regulator of breast cancer metastasis and patient survival

(2009) C. Gjerdrum et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

81 POSTER Preclinical pharmacodynamic markers of MGCD265, a potent orally active c-Met/VEGFR multitargeted kinase inhibitor in Phase I clinical trials

(2008) N. Beaulieu et al.   EJC SUPPLEMENTS

Axl promotes cell invasion by inducing MMP-9 activity through activation of NF-κB and Brg-1

(2008) K-Y Tai et al.   ONCOGENE