Crizotinib resistance: implications for therapeutic strategies

Activity and safety of ceritinib in patients with ALK -rearranged non-small-cell lung cancer (ASCEND-1): updated results from the multicentre, open-label, phase 1 trial

(2016) Dong-Wan Kim et al.   LANCET ONCOLOGY

Alectinib in ALK -positive, crizotinib-resistant, non-small-cell lung cancer: a single-group, multicentre, phase 2 trial

(2016) Alice T Shaw et al.   LANCET ONCOLOGY

Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F

(2016) Alice T. Shaw et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Functional Landscape of Resistance to ALK Inhibition in Lung Cancer

(2015) Frederick H. Wilson et al.   CANCER CELL

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models

(2015) Helen Y. Zou et al.   CANCER CELL

Induction of PD-L1 Expression by the EML4-ALK Oncoprotein and Downstream Signaling Pathways in Non-Small Cell Lung Cancer

(2015) K. Ota et al.   CLINICAL CANCER RESEARCH

Progression-Free and Overall Survival in ALK-Positive NSCLC Patients Treated with Sequential Crizotinib and Ceritinib

(2015) J. F. Gainor et al.   CLINICAL CANCER RESEARCH

Clinical Experience With Crizotinib in Patients With Advanced ALK-Rearranged Non–Small-Cell Lung Cancer and Brain Metastases

(2015) Daniel B. Costa et al.   JOURNAL OF CLINICAL ONCOLOGY

Analysis of ERBB Ligand-Induced Resistance Mechanism to Crizotinib by Primary Culture of Lung Adenocarcinoma with EML4-ALK Fusion Gene

(2015) Madoka Kimura et al.   Journal of Thoracic Oncology

I1171 missense mutation (particularly I1171N) is a common resistance mutation in ALK-positive NSCLC patients who have progressive disease while on alectinib and is sensitive to ceritinib

(2015) Sai-Hong Ignatius Ou et al.   LUNG CANCER

Brain metastases in patients with EGFR -mutated or ALK -rearranged non-small-cell lung cancers

(2015) Deepa Rangachari et al.   LUNG CANCER

RAS-MAPK dependence underlies a rational polytherapy strategy in EML4-ALK–positive lung cancer

(2015) Gorjan Hrustanovic et al.   NATURE MEDICINE

Pembrolizumab for the Treatment of Non–Small-Cell Lung Cancer

(2015) Edward B. Garon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK

(2015) Diletta Fontana et al.   Cancer Medicine

Receptor ligand-triggered resistance to alectinib and its circumvention by Hsp90 inhibition in EML4-ALK lung cancer cells

(2015) Azusa Tanimoto et al.   Oncotarget

ALK Mutations Confer Differential Oncogenic Activation and Sensitivity to ALK Inhibition Therapy in Neuroblastoma

(2014) Scott C. Bresler et al.   CANCER CELL

Two Novel ALK Mutations Mediate Acquired Resistance to the Next-Generation ALK Inhibitor Alectinib

(2014) R. Katayama et al.   CLINICAL CANCER RESEARCH

U.S. Food and Drug Administration Approval: Crizotinib for Treatment of Advanced or Metastatic Non-Small Cell Lung Cancer That Is Anaplastic Lymphoma Kinase Positive

(2014) S. M. Malik et al.   CLINICAL CANCER RESEARCH

Stereotactic Radiation Therapy can Safely and Durably Control Sites of Extra-Central Nervous System Oligoprogressive Disease in Anaplastic Lymphoma Kinase-Positive Lung Cancer Patients Receiving Crizotinib

(2014) Gregory N. Gan et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations

(2014) Ted W. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Next-Generation Sequencing Reveals a Novel NSCLC ALK F1174V Mutation and Confirms ALK G1202R Mutation Confers High-Level Resistance to Alectinib (CH5424802/RO5424802) in ALK-Rearranged NSCLC Patients Who Progressed on Crizotinib

(2014) Sai-Hong Ignatius Ou et al.   Journal of Thoracic Oncology

Secondary Mutations at I1171 in the ALK Gene Confer Resistance to Both Crizotinib and Alectinib

(2014) Gouji Toyokawa et al.   Journal of Thoracic Oncology

Rationale for co-targeting IGF-1R and ALK in ALK fusion–positive lung cancer

(2014) Christine M Lovly et al.   NATURE MEDICINE

Ceritinib in ALK-Rearranged Non–Small-Cell Lung Cancer

(2014) Alice T. Shaw et al.   NEW ENGLAND JOURNAL OF MEDICINE

First-Line Crizotinib versus Chemotherapy in ALK-Positive Lung Cancer

(2014) Benjamin J. Solomon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Patient-derived models of acquired resistance can identify effective drug combinations for cancer

(2014) Adam S. Crystal et al.   SCIENCE

The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non-Small Cell Lung Cancer

(2014) L. Friboulet et al.   Cancer Discovery

A Multicenter Phase II Study of Ganetespib Monotherapy in Patients with Genotypically Defined Advanced Non-Small Cell Lung Cancer

(2013) M. A. Socinski et al.   CLINICAL CANCER RESEARCH

ALK Rearrangements Are Mutually Exclusive with Mutations in EGFR or KRAS: An Analysis of 1,683 Patients with Non-Small Cell Lung Cancer

(2013) J. F. Gainor et al.   CLINICAL CANCER RESEARCH

Co-Clinical Trials Demonstrate Superiority of Crizotinib to Chemotherapy inALK-Rearranged Non–Small Cell Lung Cancer and Predict Strategies to Overcome Resistance

(2013) Zhao Chen et al.   CLINICAL CANCER RESEARCH

Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar

(2013) Seng Chuan Tang et al.   INTERNATIONAL JOURNAL OF CANCER

Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

(2013) Thomas H. Marsilje et al.   JOURNAL OF MEDICINAL CHEMISTRY

Clinical Impact of Continued Crizotinib Administration after Isolated Central Nervous System Progression in Patients with Lung Cancer Positive for ALK Rearrangement

(2013) Masayuki Takeda et al.   Journal of Thoracic Oncology

The Central Nervous System as a Sanctuary Site in ALK-Positive Non–Small-Cell Lung Cancer

(2013) Justin F. Gainor et al.   Journal of Thoracic Oncology

Transformation to Sarcomatoid Carcinoma in ALK-Rearranged Adenocarcinoma, Which Developed Acquired Resistance to Crizotinib and Received Subsequent Chemotherapies

(2013) Yoshihisa Kobayashi et al.   Journal of Thoracic Oncology

Epithelial-mesenchymal transition leads to crizotinib resistance in H2228 lung cancer cells with EML4-ALK translocation

(2013) Hyeong Ryul Kim et al.   Molecular Oncology

Crizotinib versus Chemotherapy in Advanced ALK-Positive Lung Cancer

(2013) Alice T. Shaw et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Comprehensive Comparative Analysis of the Histomorphological Features of ALK-Rearranged Lung Adenocarcinoma Based on Driver Oncogene Mutations: Frequent Expression of Epithelial-Mesenchymal Transition Markers than Other Genotype

(2013) Hyojin Kim et al.   PLoS One

Targeted Inhibition of the Molecular Chaperone Hsp90 Overcomes ALK Inhibitor Resistance in Non–Small Cell Lung Cancer

(2013) Jim Sang et al.   Cancer Discovery

Oncogene status predicts patterns of metastatic spread in treatment-naive nonsmall cell lung cancer

(2012) Robert C. Doebele et al.   CANCER

Isolated central nervous system progression on Crizotinib

(2012) Stephen G. Chun et al.   CANCER BIOLOGY & THERAPY

Paracrine Receptor Activation by Microenvironment Triggers Bypass Survival Signals and ALK Inhibitor Resistance in EML4-ALK Lung Cancer Cells

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

Mechanisms of Resistance to Crizotinib in Patients withALKGene Rearranged Non–Small Cell Lung Cancer

(2012) Robert C. Doebele et al.   CLINICAL CANCER RESEARCH

Activation of HER Family Signaling as a Mechanism of Acquired Resistance to ALK Inhibitors in EML4-ALK-Positive Non-Small Cell Lung Cancer

(2012) J. Tanizaki et al.   CLINICAL CANCER RESEARCH

Local Ablative Therapy of Oligoprogressive Disease Prolongs Disease Control by Tyrosine Kinase Inhibitors in Oncogene-Addicted Non–Small-Cell Lung Cancer

(2012) Andrew J. Weickhardt et al.   Journal of Thoracic Oncology

Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study

(2012) D Ross Camidge et al.   LANCET ONCOLOGY

Crizotinib for the Treatment of ALK -Rearranged Non-Small Cell Lung Cancer: A Success Story to Usher in the Second Decade of Molecular Targeted Therapy in Oncology

(2012) Sai-Hong Ignatius Ou et al.   ONCOLOGIST

A Novel ALK Secondary Mutation and EGFR Signaling Cause Resistance to ALK Kinase Inhibitors

(2011) T. Sasaki et al.   CANCER RESEARCH

CSF Concentration of the Anaplastic Lymphoma Kinase Inhibitor Crizotinib

(2011) Daniel B. Costa et al.   JOURNAL OF CLINICAL ONCOLOGY

Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK

(2011) R. Katayama et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

EML4-ALK Mutations in Lung Cancer That Confer Resistance to ALK Inhibitors

(2010) Young Lim Choi et al.   NEW ENGLAND JOURNAL OF MEDICINE

Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer

(2010) Eunice L. Kwak et al.   NEW ENGLAND JOURNAL OF MEDICINE

Clinical Features and Outcome of Patients With Non–Small-Cell Lung Cancer Who Harbor EML4-ALK

(2009) Alice T. Shaw et al.   JOURNAL OF CLINICAL ONCOLOGY

Multiplex Reverse Transcription-PCR Screening for EML4-ALK Fusion Transcripts

(2008) K. Takeuchi et al.   CLINICAL CANCER RESEARCH