Abstract
Brigatinib (ALUNBRIG™) is a small molecule antineoplastic anaplastic lymphoma kinase (ALK) inhibitor being developed by ARIAD Pharmaceuticals (a wholly-owned subsidiary of Takeda Pharmaceutical Company). In April 2017 brigatinib received accelerated approval in the USA for the treatment of patients with ALK-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. The development of resistance to crizotinib is a therapeutic challenge that has led to the development of second-generation ALK-inhibitors such as brigatinib, which have activity against treatment-resistant ALK mutants. This article summarizes the milestones in the development of brigatinib leading to this first global approval for the treatment of patients with ALK-positive metastatic NSCLC who have progressed on or are intolerant to crizotinib.
MeSH terms
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Anaplastic Lymphoma Kinase
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Antineoplastic Agents / adverse effects
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / therapeutic use*
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Carcinoma, Non-Small-Cell Lung / drug therapy*
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Carcinoma, Non-Small-Cell Lung / secondary
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Clinical Trials as Topic
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Drug Approval*
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Humans
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Lung Neoplasms / drug therapy*
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Organophosphorus Compounds / adverse effects
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Organophosphorus Compounds / chemistry
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Organophosphorus Compounds / pharmacokinetics
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Organophosphorus Compounds / therapeutic use*
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Pyrimidines / adverse effects
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Pyrimidines / chemistry
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Pyrimidines / pharmacokinetics
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Pyrimidines / therapeutic use*
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Receptor Protein-Tyrosine Kinases / antagonists & inhibitors
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Receptor Protein-Tyrosine Kinases / chemistry
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United States
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United States Food and Drug Administration
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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Receptor Protein-Tyrosine Kinases
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brigatinib