Entrectinib, a TRK/ROS1 inhibitor with anti-CNS tumor activity: differentiation from other inhibitors in its class due to weak interaction with P-glycoprotein

Crizotinib in ROS1-rearranged advanced non-small-cell lung cancer (NSCLC): updated results, including overall survival, from PROFILE 1001

(2019) A T Shaw et al.   ANNALS OF ONCOLOGY

Development of Simplified in Vitro P-Glycoprotein Substrate Assay and in Silico Prediction Models To Evaluate Transport Potential of P-Glycoprotein

(2019) Rikiya Ohashi et al.   MOLECULAR PHARMACEUTICS

Entrectinib in ROS1 fusion-positive non-small-cell lung cancer: integrated analysis of three phase 1–2 trials

(2019) Alexander Drilon et al.   LANCET ONCOLOGY

Entrectinib in patients with advanced or metastatic NTRK fusion-positive solid tumours: integrated analysis of three phase 1–2 trials

(2019) Robert C Doebele et al.   LANCET ONCOLOGY

Efficacy of Larotrectinib in TRK Fusion–Positive Cancers in Adults and Children

(2018) Alexander Drilon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels

(2017) Timothy P Heffron   NEURO-ONCOLOGY

Somatic chromosomal engineering identifies BCAN-NTRK1 as a potent glioma driver and therapeutic target

(2017) Peter J. Cook et al.   Nature Communications

Crizotinib resistance: implications for therapeutic strategies

(2016) I. Dagogo-Jack et al.   ANNALS OF ONCOLOGY

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor

(2016) Maria Menichincheri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications

(2016) E. Ardini et al.   MOLECULAR CANCER THERAPEUTICS

Impact of Membrane Drug Transporters on Resistance to Small-Molecule Tyrosine Kinase Inhibitors

(2016) Claudia Neul et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Label-free assay for the assessment of nonspecific binding of positron emission tomography tracer candidates

(2015) Frauke Assmus et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Estimation of Drug Binding to Brain Tissue: Methodology and in Vivo Application of a Distribution Assay in Brain Polar Lipids

(2015) Sara Belli et al.   MOLECULAR PHARMACEUTICS

Crizotinib in ROS1-Rearranged Non–Small-Cell Lung Cancer

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

The landscape of kinase fusions in cancer

(2014) Nicolas Stransky et al.   Nature Communications

CSF Concentration of the Anaplastic Lymphoma Kinase Inhibitor Crizotinib

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

Validation of 96-well Equilibrium Dialysis with Non-radiolabeled Drug for Definitive Measurement of Protein Binding and Application to Clinical Development of Highly-Bound Drugs

(2011) Maciej J. Zamek-Gliszczynski et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Long-term survival in patients with non-small cell lung cancer and synchronous brain metastasis treated with whole-brain radiotherapy and thoracic chemoradiation

(2011) Oscar Arrieta et al.   Radiation Oncology