Nerlynx (neratinib) is an oral tyrosine kinase inhibitor (TKI) recently approved by the FDA for extended adjuvant treatment of early-stage human epidermal growth factor receptor 2 (HER2)–positive breast cancer in patients who have completed standard adjuvant therapy with Herceptin (trastuzumab). Neratinib blocks signal transduction through the epidermal growth factor receptors (EGFR) HER1, HER2, and HER4. Small-molecule TKI agents may offer advantages over antibody-based HER2 antagonists like Herceptin, such as the ability to cross the blood-brain barrier.

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