Abstract
Despite the benefits of first and second generation anaplastic lymphoma kinase (ALK) inhibitors in the management of ALK-rearranged advanced non-small-cell lung cancer (NSCLC), the development of acquired resistance poses an ongoing dilemma. Brigatinib has demonstrated a wider spectrum of preclinical activity against crizotinib-resistant ALK mutant advanced NSCLC. The current review narrates a brief history of tyrosine kinases, the development and clinical background of brigatinib (including its pharmacology and molecular structure) and its use in ALK-positive NSCLC.
Keywords:
ALK inhibitors; ALK positive; TKI; brigatinib; non-small cell lung cancer.
MeSH terms
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Anaplastic Lymphoma Kinase / antagonists & inhibitors*
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Anaplastic Lymphoma Kinase / genetics
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Anaplastic Lymphoma Kinase / metabolism
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Carcinoma, Non-Small-Cell Lung / drug therapy*
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Carcinoma, Non-Small-Cell Lung / metabolism
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Carcinoma, Non-Small-Cell Lung / pathology
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Cell Proliferation / drug effects
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Drug Design*
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Humans
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Lung Neoplasms / drug therapy*
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Lung Neoplasms / metabolism
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Lung Neoplasms / pathology
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Mutation
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Organophosphorus Compounds / chemical synthesis
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Organophosphorus Compounds / chemistry
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Organophosphorus Compounds / pharmacology*
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
Substances
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Antineoplastic Agents
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Organophosphorus Compounds
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Pyrimidines
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ALK protein, human
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Anaplastic Lymphoma Kinase
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brigatinib