Phase 2 (Data)
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Catalyst Info & Data Links
TITLE: Neratinib (HKI-272) for HER2-positive breast cancer and Brain Metastases
ClinicalTrials.gov (NCT01494662): HKI-272 for HER2-Positive Breast Cancer and Brain Metastases
WHAT IS THE CATALYST EVENT?
Phase 2 Data
WHEN WILL THE EVENT (OR DID THE EVENT) OCCUR?
MECHANISM OF ACTION
Neratinib is an intracellular kinase inhibitor that irreversibly binds to epidermal growth factor receptor (EGFR), HER2, and HER4. In vitro, neratinib reduces EGFR and HER2 autophosphorylation, downstream MAPK and AKT signaling pathways, and showed antitumor activity in EGFR and/or HER2 expressing carcinoma cell lines. Neratinib human metabolites M3, M6, M7 and M11 inhibited the activity of EGFR, HER2, and HER4 in vitro. In vivo, oral administration of neratinib inhibited tumor growth in mouse xenograft models with tumor cell lines expressing HER2 and EGFR.
Approximately 20 to 25 percent of breast cancer tumors over-express the HER2 protein. HER2-positive breast cancer is often more aggressive than other types of breast cancer, increasing the risk of disease progression and death. Although research has shown that trastuzumab can reduce the risk of early stage HER2-positive breast cancer returning after surgery, up to 25% of patients treated with trastuzumab experience recurrence.
Updated by HC
PBYI, HER2-positive breast cancer and brain Metastases, brain tumor cancer, NERLYNX, Neratinib (HKI-272)
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