2021
DOI: 10.1007/s40265-021-01503-3
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Entrectinib: A Review in NTRK+ Solid Tumours and ROS1+ NSCLC

Abstract: Entrectinib (Rozlytrek ® ) is an orally active, CNS-penetrant, small-molecule, selective inhibitor of the tropomyosin receptor tyrosine kinases TRKA/B/C [encoded by the neurotrophic tyrosine receptor kinase (NTRK) genes NTRK1/2/3 , respectively], the proto-oncogene tyrosine-protein kinase ROS1 ( ROS1 ) and the anaplastic lymphoma kinase gene ( ALK ). It is approved for the treatment of adults and paediatric patients age… Show more

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Cited by 35 publications
(25 citation statements)
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“…In the early-to-mid 2000s, the first approvals of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) combined with a better understanding of the role of "driver" mutations in the pathogenesis and progression of NSCLC marked the start of the targeted therapy era [4,5]. Subsequently, TKIs targeting other driver mutations, such as anaplastic lymphoma kinase (ALK), ROS1, BRAF V600E, or NTRK1/2/3 alterations have been approved for patients with NSCLC tumors harboring these mutations [6][7][8][9][10]. More recently, immuno-oncology (I-O) therapies, primarily immune checkpoint inhibitors targeting the programmed death-1 (PD-1)/programmed death ligand 1 (PD-L1) pathway, have demonstrated improved survival outcomes versus standard chemotherapy in randomized clinical trials and have emerged as recommended first-and second-line treatments in Europe and North America for patients with advanced NSCLC without actionable driver mutations [3,[11][12][13][14][15].…”
Section: Introductionmentioning
confidence: 99%
“…In the early-to-mid 2000s, the first approvals of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) combined with a better understanding of the role of "driver" mutations in the pathogenesis and progression of NSCLC marked the start of the targeted therapy era [4,5]. Subsequently, TKIs targeting other driver mutations, such as anaplastic lymphoma kinase (ALK), ROS1, BRAF V600E, or NTRK1/2/3 alterations have been approved for patients with NSCLC tumors harboring these mutations [6][7][8][9][10]. More recently, immuno-oncology (I-O) therapies, primarily immune checkpoint inhibitors targeting the programmed death-1 (PD-1)/programmed death ligand 1 (PD-L1) pathway, have demonstrated improved survival outcomes versus standard chemotherapy in randomized clinical trials and have emerged as recommended first-and second-line treatments in Europe and North America for patients with advanced NSCLC without actionable driver mutations [3,[11][12][13][14][15].…”
Section: Introductionmentioning
confidence: 99%
“…Since the NTRK basket trial demonstrates the efficacy of entrectinib as a monotherapy in metastatic NTRK rearranged solid tumors ( 26 ). Basket trails can be attempted for ROS1 rearranged or ROS1 fusion tumors, in which ROS1 inhibitors such as crizotinib are used whenever ROS1 rearranged or ROS1 fusion is detected, regardless of tumor types, for a broader tumor agnostic approval.…”
Section: Discussionmentioning
confidence: 99%
“…Entrectinib ( 45 ) is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine protein kinase ROS1 (ref. 98) and anaplastic lymphoma kinase (ALK) inhibitor for the treatment of ROS1-positive metastatic non-small cell lung cancer with NTRK gene fusion-positive solid tumors (Fig. 27a).…”
Section: Pyrazole-containing Drugs Targeting Central Nervous System D...mentioning
confidence: 99%