Prediction of ROS1 and TRKA/B/C occupancy in plasma and cerebrospinal fluid for entrectinib alone and in DDIs using physiologically based pharmacokinetic (PBPK) modeling approach

Prediction for Plasma Trough Concentration and Optimal Dosing of Imatinib under Multiple Clinical Situations Using Physiologically Based Pharmacokinetic Modeling

(2023) Dongmei Gao et al.   ACS Omega

Efficacy and safety exposure–response analyses of entrectinib in patients with advanced or metastatic solid tumors

(2022) Francois Mercier et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Pre‐ and post‐treatment blood‐based genomic landscape of patients with ROS1 or NTRK fusion‐positive solid tumours treated with entrectinib

(2022) Rafal Dziadziuszko et al.   Molecular Oncology

Alectinib versus crizotinib in ALK ‐positive advanced non‐small cell lung cancer and comparison of next‐generation TKIs after crizotinib failure: Real‐world evidence

(2022) Yurong Wang et al.   Cancer Medicine

Physiologically based pharmacokinetic combined BTK occupancy modeling for optimal dosing regimen prediction of acalabrutinib in patients alone, with different CYP3A4 variants, co-administered with CYP3A4 modulators and with hepatic impairment

(2022) Lifang Xu et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Physiologically based pharmacokinetic combined JAK2 occupancy modelling to simulate PK and PD of baricitinib with kidney transporter inhibitors and in patients with hepatic/renal impairment

(2022) Zhongjian Wang et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Characterization of the pharmacokinetics of entrectinib and its active M5 metabolite in healthy volunteers and patients with solid tumors

(2021) Georgina Meneses-Lorente et al.   INVESTIGATIONAL NEW DRUGS

Physiologically‐based pharmacokinetic model for alectinib, ruxolitinib, and panobinostat in the presence of cancer, renal impairment, and hepatic impairment

(2021) Mo'tasem M. Alsmadi et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

The European Medicines Agency review of entrectinib for the treatment of adult or paediatric patients with solid tumours who have a neurotrophic tyrosine receptor kinase gene fusions and adult patients with non-small-cell lung cancer harbouring ROS1 rearrangements

(2021) J. Delgado et al.   ESMO Open

Physiologically‐based pharmacokinetic model predictions of inter‐ethnic differences in imatinib pharmacokinetics and dosing regimens

(2021) Jeffry Adiwidjaja et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Physiologically-Based Pharmacokinetic Modelling of Entrectinib Parent and Active Metabolite to Support Regulatory Decision-Making

(2021) Nassim Djebli et al.   EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS

In vitro and clinical investigations to determine the drug-drug interaction potential of entrectinib, a small molecule inhibitor of neurotrophic tyrosine receptor kinase (NTRK)

(2021) Georgina Meneses-Lorente et al.   INVESTIGATIONAL NEW DRUGS

Pharmacokinetic Drug-Drug Interactions with Drugs Approved by the US Food and Drug Administration in 2020: Mechanistic Understanding and Clinical Recommendations

(2021) Jingjing Yu et al.   DRUG METABOLISM AND DISPOSITION

Clinical Biomarkers for Early Identification of Patients with Intracranial Metastatic Disease

(2021) Karolina Gaebe et al.   Cancers

Beyond epidermal growth factor receptor: MET amplification as a general resistance driver to targeted therapy in oncogene-driven non-small-cell lung cancer

(2021) N. Coleman et al.   ESMO Open

Physiologically Based Absorption Modelling to Explore the Impact of Food and Gastric pH Changes on the Pharmacokinetics of Entrectinib

(2020) Neil Parrott et al.   AAPS Journal

Clinical and biological implications of target occupancy in CLL treated with the BTK inhibitor acalabrutinib

(2020) Clare CHUI LING Sun et al.   BLOOD

Physiologically‐Based Pharmacokinetic Modeling Characterizes the CYP3A‐Mediated Drug‐Drug Interaction Between Fluconazole and Sildenafil in Infants

(2020) Sara N. Salerno et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Cerebrospinal Fluid Penetration and Combination Therapy of Entrectinib for Disseminated ROS1/NTRK-Fusion Positive Pediatric High-Grade Glioma

(2020) Lisa Mayr et al.   Journal of Personalized Medicine

Entrectinib: First Global Approval

(2019) Zaina T. Al-Salama et al.   DRUGS

Development of a physiologically based pharmacokinetic model for intravenous lenalidomide in mice

(2019) Jim H. Hughes et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Binding Kinetics Survey of the Drugged Kinome

(2018) Victoria Georgi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

In vitro evaluation of the inhibition and induction potential of olaparib, a potent poly(ADP-ribose) polymerase inhibitor, on cytochrome P450

(2017) Alex McCormick et al.   XENOBIOTICA

Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372-001 and STARTRK-1)

(2017) Alexander Drilon et al.   Cancer Discovery

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

Differences in Cytochrome P450-Mediated Pharmacokinetics Between Chinese and Caucasian Populations Predicted by Mechanistic Physiologically Based Pharmacokinetic Modelling

(2013) Zoe E. Barter et al.   CLINICAL PHARMACOKINETICS

Translational Pharmacokinetic-Pharmacodynamic Modeling from Nonclinical to Clinical Development: A Case Study of Anticancer Drug, Crizotinib

(2012) Shinji Yamazaki   AAPS Journal