TRK inhibitor activity and resistance in TRK fusion-positive cancers in adults

Long-term efficacy and safety of larotrectinib in an integrated dataset of patients with TRK fusion cancer.

(2021) David S. Hong et al.   JOURNAL OF CLINICAL ONCOLOGY

Larotrectinib in patients with TRK fusion-positive solid tumours: a pooled analysis of three phase 1/2 clinical trials

(2020) David S Hong et al.   LANCET ONCOLOGY

Characterization of On-Target Adverse Events Caused by TRK Inhibitor Therapy

(2020) D. Liu et al.   ANNALS OF ONCOLOGY

Preclinical evaluation of SIM1803-1A, a small molecule Trk/ROS1 dual inhibitor for wild and mutate NTRK/ROS1 fusion solid malignancies.

(2020) Jianfei Wang et al.   JOURNAL OF CLINICAL ONCOLOGY

Efficacy and safety of entrectinib in patients (pts) with NTRK-fusion positive (NTRK-fp) solid tumors: An updated integrated analysis.

(2020) Christian Diego Rolfo et al.   JOURNAL OF CLINICAL ONCOLOGY

Activity and safety of larotrectinib in adult patients with TRK fusion cancer: An expanded data set.

(2020) Alexander E. Drilon et al.   JOURNAL OF CLINICAL ONCOLOGY

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

(2020) Holger Fischer et al.   NEURO-ONCOLOGY

U.S. Phase I First-in-human Study of Taletrectinib (DS-6051b/AB-106), a ROS1/TRK Inhibitor, in Patients with Advanced Solid Tumors

(2020) Kyriakos P. Papadopoulos et al.   CLINICAL CANCER RESEARCH

364O Intracranial efficacy of entrectinib in patients with NTRK fusion-positive solid tumours and baseline CNS metastases

(2020) T. John et al.   ANNALS OF ONCOLOGY

TRK xDFG mutations trigger a sensitivity switch from type I to II kinase inhibitors

(2020) Emiliano Cocco et al.   Cancer Discovery

Resistance to TRK inhibition mediated by convergent MAPK pathway activation

(2019) Emiliano Cocco et al.   NATURE MEDICINE

Larotrectinib, a highly selective tropomyosin receptor kinase (TRK) inhibitor for the treatment of TRK fusion cancer

(2019) Noah Federman et al.   Expert Review of Clinical Pharmacology

TRK inhibitors in TRK fusion-positive cancers

(2019) A Drilon   ANNALS OF ONCOLOGY

The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models

(2019) Ryohei Katayama et al.   Nature Communications

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

Basket Studies: Redefining Clinical Trials in the Era of Genome-Driven Oncology

(2018) Jessica J. Tao et al.   Annual Review of Medicine

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

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

Effect of tyrosine kinase inhibitors on renal handling of creatinine by MATE1

(2018) Saki Omote et al.   Scientific Reports

Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations

(2018) Alexander Drilon et al.   Cancer Discovery

NTRK fusion-positive cancers and TRK inhibitor therapy

(2018) Emiliano Cocco et al.   Nature Reviews Clinical Oncology

Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers

(2017) Miho J. Fuse et al.   MOLECULAR CANCER THERAPEUTICS

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

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion–Positive Solid Tumors

(2017) Alexander Drilon et al.   Cancer Discovery

Precision oncology: Charting a path forward to broader deployment of genomic profiling

(2017) Alison M. Schram et al.   PLOS MEDICINE

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

Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes

(2016) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer

(2016) J. F. Gainor et al.   Cancer Discovery

First-Line Erlotinib Therapy Until and Beyond Response Evaluation Criteria in Solid Tumors Progression in Asian Patients With Epidermal Growth Factor Receptor Mutation–Positive Non–Small-Cell Lung Cancer

(2016) Keunchil Park et al.   JAMA Oncology

An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101

(2015) R. C. Doebele et al.   Cancer Discovery

Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer

(2013) Aria Vaishnavi et al.   NATURE MEDICINE

Acquired Resistance to Crizotinib from a Mutation in CD74–ROS1

(2013) Mark M. Awad et al.   NEW ENGLAND JOURNAL OF MEDICINE

Administration of a Tropomyosin Receptor Kinase Inhibitor Attenuates Sarcoma-Induced Nerve Sprouting, Neuroma Formation and Bone Cancer Pain

(2010) Joseph R Ghilardi et al.   Molecular Pain

Appetite Enhancement and Weight Gain by Peripheral Administration of TrkB Agonists in Non-Human Primates

(2008) John C. Lin et al.   PLoS One