Drug intelligence / Profile preview

lapatinib + letrozole + trastuzumab

Development stage
Unknown
Lead developer
GSK
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

Lapatinib, letrozole, and trastuzumab is a combination therapy used in the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-positive (HER2+) metastatic breast cancer in postmenopausal women. Lapatinib is a small molecule tyrosine kinase inhibitor targeting HER2 and EGFR; letrozole is an aromatase inhibitor that reduces estrogen production; and trastuzumab is a monoclonal antibody targeting HER2. The combination leverages both hormonal blockade and dual HER2 inhibition to improve outcomes compared to single-agent or doublet therapies[6][1][4]. This regimen has been studied in clinical trials for its efficacy in improving progression-free survival (PFS) over single targeted agent plus aromatase inhibitor combinations[6].

Other names
lapatinib/letrozole/trastuzumablapatinib plus letrozole plus trastuzumab
02

Targets

EGFR (Epidermal growth factor receptor)CYP19A1 (Aromatase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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