Abstract |
Targeted therapy has shown to be a very effective treatment in tumors with specific genomic drivers. Trk has proven to be one such target. Efforts to target the Trk fusion with specific inhibitors have shown remarkable responses in a tumor agnostic fashion, with responses seen even in patients with intracranial metastasis. Entrectinib is a first-generation Trk inhibitor with impressive activity in early phase trials performed in patients with NTRK fusion positive solid tumors and ROS1 positive non-small-cell lung cancers with subsequent approval for those indications. Entrectinib was also found to be effective in treatment of brain metastasis and generally well tolerated.
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Authors | Neal Chawla, Nam Q Bui, Mahesh Seetharam |
Journal | Future oncology (London, England)
(Future Oncol)
Vol. 17
Issue 22
Pg. 2835-2846
(Aug 2021)
ISSN: 1744-8301 [Electronic] England |
PMID | 33896226
(Publication Type: Journal Article, Review)
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Chemical References |
- Benzamides
- Indazoles
- Membrane Glycoproteins
- NTRK1 protein, human
- NTRK3 protein, human
- Oncogene Proteins, Fusion
- Protein Kinase Inhibitors
- Pyrazoles
- Pyrimidines
- Receptor, trkA
- Receptor, trkB
- Receptor, trkC
- tropomyosin-related kinase-B, human
- entrectinib
- larotrectinib
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Topics |
- Animals
- Benzamides
(pharmacology, therapeutic use)
- Cell Line, Tumor
- Clinical Trials as Topic
- Disease Models, Animal
- Drug Approval
- Drug Evaluation, Preclinical
- Humans
- Indazoles
(pharmacology, therapeutic use)
- Membrane Glycoproteins
(antagonists & inhibitors, genetics)
- Molecular Targeted Therapy
(methods, trends)
- Neoplasms
(drug therapy, genetics, mortality, pathology)
- Oncogene Proteins, Fusion
(antagonists & inhibitors, genetics)
- Progression-Free Survival
- Protein Kinase Inhibitors
(pharmacology, therapeutic use)
- Pyrazoles
(pharmacology, therapeutic use)
- Pyrimidines
(pharmacology, therapeutic use)
- Receptor, trkA
(antagonists & inhibitors, genetics)
- Receptor, trkB
(antagonists & inhibitors, genetics)
- Receptor, trkC
(antagonists & inhibitors, genetics)
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