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<\/a><\/p>\n1. Acalabrutinib<\/p>\n
On October 31, 2017, the FDA granted accelerated approval to acalabrutinib<\/a> for treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy. B-cell receptor (BCR) signalling is central to\u00a0the survival and proliferation of malignant B cells, and\u00a0Bruton tyrosine kinase<\/a> (BTK), an integral member of the\u00a0BCR pathway, is a clinically validated\u00a0target in mantle\u00a0cell lymphoma.<\/p>\n Acalabrutinib (ACP-196) is a highly selective, potent\u00a0BTK inhibitor developed to minimise off-target activity.\u00a0Findings from in-vitro studies showed that acalabrutinib\u00a0has more selective\u00a0BTK inhibition and higher in-vivo\u00a0potency than ibrutinib. The phase 1\/2 ACE-CL-001\u00a0trial of\u00a0acalabrutinib monotherapy in patients with\u00a0relapsed chronic lymphocytic leukaemia showed that\u00a0acalabrutinib has rapid oral absorption and a short\u00a0plasma half-life.<\/p>\n 2. Neratinib<\/p>\n On July 17, 2017,\u00a0the FDA\u00a0approved Nerlynx (neratinib<\/a>) for the extended adjuvant treatment of early-stage, HER2-positive breast cancer. Neratinib is a kinase inhibitor that irreversibly binds to epidermal growth factor receptor<\/a>\u00a0(EGFR), human epidermal growth factor receptor 2 (HER2), and HER4. In vitro, neratinib\u00a0inhibited cell proliferation, EGFR and HER2 autophosphorylation, downstream MAPK and AKT\u00a0signaling pathways, and cell cycle regulatory pathway activities in HER2- and EGFR-dependent\u00a0cancer cell lines. Neratinib human metabolites M3, M6, M7, and M11 inhibited the activity of\u00a0EGFR, HER2, and HER4 in vitro. In vivo, oral administration of\u00a0neratinib inhibited tumor\u00a0growth in mouse xenograft models with tumor cell lines expressing HER2 and EGFR.<\/p>\n 3. Brigatinib<\/p>\n On April 28, 2017, the FDA\u00a0granted accelerated approval to brigatinib<\/a> for the treatment of patients with metastatic anaplastic lymphoma kinase<\/a> (ALK)-positive non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib.\u00a0Brigatinib acts as both a anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR) inhibitor.<\/p>\n 4. Midostaurin<\/p>\n Midostaurin<\/a> (CGP41251; PKC412) is a multikinase inhibitor recently approved for 2 indications in adult patients: (1) newly diagnosed acute myeloid leukemia (AML) with fms-like tyrosine kinase 3 (FLT3) mutations and (2) advanced systemic mastocytosis (SM).<\/p>\n 5. Ribociclib<\/p>\n On March 13, 2017, the FDA\u00a0approved ribociclib<\/a>, a cyclin-dependent kinase 4\/6 inhibitor, in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.<\/p>\n 6.\u00a0Abemaciclib<\/p>\n On September 28, 2017, the FDA\u00a0approved abemaciclib<\/a> in combination with fulvestrant for women with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy. In addition, abemaciclib was approved as monotherapy for women and men with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.<\/p>\n 7.\u00a0Copanlisib<\/p>\n On September 14, 2017, the FDA\u00a0granted accelerated approval to copanlisib<\/a> for the treatment of adult patients with relapsed follicular lymphoma who have received at least two prior systemic therapies.<\/p>\n<\/a><\/p>\n<\/a><\/p>\n<\/a><\/p>\n<\/a><\/p>\n<\/a><\/p>\n