Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors

Entrectinib is a potent small-molecule tyrosine kinase inhibitor that targets oncogenic rearrangements in NTRK, ROS1, and ALK. The consolidated results of 2 Phase I trials demonstrated activity in tyrosine kinase inhibitor-naïve patients along with substantial intracranial activity. In ROS1-rearrang...

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Detalles Bibliográficos
Autores principales: Liu, Dazhi, Offin, Michael, Harnicar, Stephen, Li, Bob T, Drilon, Alexander
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2018
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6055893/
https://www.ncbi.nlm.nih.gov/pubmed/30050303
http://dx.doi.org/10.2147/TCRM.S147381
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author Liu, Dazhi
Offin, Michael
Harnicar, Stephen
Li, Bob T
Drilon, Alexander
author_facet Liu, Dazhi
Offin, Michael
Harnicar, Stephen
Li, Bob T
Drilon, Alexander
author_sort Liu, Dazhi
collection PubMed
description Entrectinib is a potent small-molecule tyrosine kinase inhibitor that targets oncogenic rearrangements in NTRK, ROS1, and ALK. The consolidated results of 2 Phase I trials demonstrated activity in tyrosine kinase inhibitor-naïve patients along with substantial intracranial activity. In ROS1-rearranged lung cancers, entrectinib results in durable disease control and prolonged progression-free survival. The drug is well tolerated and has a safety profile that includes adverse events mediated by on-target tropomyosin-related kinase A/B/C inhibition.
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spelling pubmed-60558932018-07-26 Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors Liu, Dazhi Offin, Michael Harnicar, Stephen Li, Bob T Drilon, Alexander Ther Clin Risk Manag Review Entrectinib is a potent small-molecule tyrosine kinase inhibitor that targets oncogenic rearrangements in NTRK, ROS1, and ALK. The consolidated results of 2 Phase I trials demonstrated activity in tyrosine kinase inhibitor-naïve patients along with substantial intracranial activity. In ROS1-rearranged lung cancers, entrectinib results in durable disease control and prolonged progression-free survival. The drug is well tolerated and has a safety profile that includes adverse events mediated by on-target tropomyosin-related kinase A/B/C inhibition. Dove Medical Press 2018-07-20 /pmc/articles/PMC6055893/ /pubmed/30050303 http://dx.doi.org/10.2147/TCRM.S147381 Text en © 2018 Liu et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Review
Liu, Dazhi
Offin, Michael
Harnicar, Stephen
Li, Bob T
Drilon, Alexander
Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors
title Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors
title_full Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors
title_fullStr Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors
title_full_unstemmed Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors
title_short Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors
title_sort entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of ntrk, ros1, and alk fusion-positive solid tumors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6055893/
https://www.ncbi.nlm.nih.gov/pubmed/30050303
http://dx.doi.org/10.2147/TCRM.S147381
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