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A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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Identification of potent Yes1 kinase inhibitors using a library screening approach.
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Biochemical pharmacology 20120801
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A double-blind, randomized, multiple-dose, parallel-group study to characterize the occurrence of diarrhea following two different dosing regimens of neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor.
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Neratinib reverses ATP-binding cassette B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivo.
Molecular pharmacology 20120701
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Structural analysis of the EGFR TK domain and potential implications for EGFR targeted therapy.
International journal of oncology 20120601
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Future oncology (London, England) 20120601
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Safety, efficacy and pharmacokinetics of neratinib (HKI-272) in Japanese patients with advanced solid tumors: a Phase 1 dose-escalation study.
Japanese journal of clinical oncology 20120401
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A genome-wide RNAi screen identifies novel targets of neratinib resistance leading to identification of potential drug resistant genetic markers.
Molecular bioSystems 20120401
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Preformulation stability study of the EGFR inhibitor HKI-272 (Neratinib) and mechanism of degradation.
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Comprehensive analysis of kinase inhibitor selectivity.
Nature biotechnology 20111030
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Beyond trastuzumab: new treatment options for HER2-positive breast cancer.
Breast (Edinburgh, Scotland) 20111001
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A genome-wide RNAi screen identifies novel targets of neratinib sensitivity leading to neratinib and paclitaxel combination drug treatments.
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Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects.
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Reversible covalent binding of neratinib to human serum albumin in vitro.
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Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
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A single-dose, crossover, placebo- and moxifloxacin-controlled study to assess the effects of neratinib (HKI-272) on cardiac repolarization in healthy adult subjects.
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Characterization of HKI-272 covalent binding to human serum albumin.
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Neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancer.
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The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.
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Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
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The development of HKI-272 and related compounds for the treatment of cancer.
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Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.
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Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
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Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.
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Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
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Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.
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