Drug intelligence / Profile preview

lapatinib + aromatase inhibitor

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

A combination regimen of **lapatinib**, a small molecule dual tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR, also known as ErbB1) and human epidermal growth factor receptor 2 (HER2/ErbB2), with an **aromatase inhibitor** (such as letrozole, anastrozole, or exemestane) is used for the treatment of hormone receptor-positive, HER2-positive metastatic breast cancer in postmenopausal women. Lapatinib blocks HER2 and EGFR signaling pathways, inhibiting cell proliferation and survival, while aromatase inhibitors block the conversion of androgens to estrogens, decreasing estrogen levels and thereby limiting estrogen-driven tumor growth. This combination is typically used in patients suitable for hormonal therapy, especially after prior exposure to chemotherapies or anti-HER2 agents[1][5][8][9].

Brand names
Tykerb (for lapatinib)
Other names
lapatinib plus aromatase inhibitorlapatinib + AITykerb plus aromatase inhibitor
02

Targets

CYP19A1 (Aromatase)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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