Type

Journal Article

Authors

John Crown
Alshad S Lalani
Lisa D Eli
Chandra S Verma
Srinivasaraghavan Kannan
Neil T. Conlon
Denis M Collins

Subjects

Pharmacology

Topics
implications year 1 her2 positive tyrosine kinase this review breast cancer treatment epidermal growth factor receptor egfr

Preclinical Characteristics of the Irreversible Pan-HER Kinase Inhibitor Neratinib Compared with Lapatinib: Implications for the Treatment of HER2-Positive and (2019)

Abstract An estimated 15-20% of breast cancers overexpress human epidermal growth factor receptor 2 (HER2/ERBB2/neu). Two small-molecule tyrosine kinase inhibitors (TKIs), lapatinib and neratinib, have been approved for the treatment of HER2-positive (HER2+) breast cancer. Lapatinib, a reversible epidermal growth factor receptor (EGFR/ERBB1/HER1) and HER2 TKI, is used for the treatment of advanced HER2+ breast cancer in combination with capecitabine, in combination with trastuzumab in patients with hormone receptor-negative metastatic breast cancer, and in combination with an aromatase inhibitor for the first-line treatment of HER2+ breast cancer. Neratinib, a next-generation, irreversible pan-HER TKI, is used in the US for extended adjuvant treatment of adult patients with early-stage HER2+ breast cancer following 1 year of trastuzumab. In Europe, neratinib is used in the extended adjuvant treatment of adult patients with early-stage hormone receptor-positive HER2+ breast cancer who are less than 1 year from the completion of prior adjuvant trastuzumab-based therapy. Preclinical studies have shown that these agents have distinct properties that may impact their clinical activity. This review describes the preclinical characterization of lapatinib and neratinib, with a focus on the differences between these two agents that may have implications for patient management.
Collections Ireland -> Dublin City University -> PubMed

Full list of authors on original publication

John Crown, Alshad S Lalani, Lisa D Eli, Chandra S Verma, Srinivasaraghavan Kannan, Neil T. Conlon, Denis M Collins

Experts in our system

1
John Crown
Dublin City University
Total Publications: 104
 
2
Neil T. Conlon
Dublin City University
Total Publications: 10
 
3
Denis M Collins
Dublin City University
Total Publications: 26