title: Neratinib (HKI-272) in the treatment of breast cancer.
abstract: Neratinib is an orally available, small, irreversible, pan-HER kinase inhibitor. HER-2-positive breast cancer is a breast cancer subtype with an increasing body of knowledge regarding potential targeted drug combinations that are significantly improving outcomes through a biologically tailored therapy approach; neratinib emerges as a promising tool in this context. This article reviews the molecular and clinical development of neratinib, an example of a covalent drug, from preclinical models to Phase III clinical trials, focusing on breast cancer treatment. The potential combinations of neratinib with chemotherapy in the metastatic, adjuvant and even neoadjuvant settings are appraised. These results and future perspectives will be discussed.
authors: Medical Oncology Service, Instituto de Investigación Sanitaria Gregorio Marañón, Universidad Complutense, Calle Dr Esquerdo 46, 28007, Madrid, Spain.
authors: Sara
authors: S
authors: López-Tarruella
authors: Yolanda
authors: Y
authors: Jerez
authors: Iván
authors: I
authors: Márquez-Rodas
authors: Miguel
authors: M
authors: Martín
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D005260:Female; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D011804:Quinolines / Q000494:pharmacology / Q000627:therapeutic use*; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011804:Quinolines; D018719:Erb-b2 Receptor Tyrosine Kinases; C487932:neratinib