Drug intelligence / Profile preview

lapatinib + letrozole

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

Overview

Lapatinib + letrozole is a combination therapy used for the treatment of postmenopausal women with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-positive (HER2+) metastatic breast cancer. Lapatinib is a small molecule tyrosine kinase inhibitor that targets both HER1/EGFR and HER2 receptors, inhibiting intracellular signaling pathways involved in tumor cell proliferation and survival. Letrozole is an aromatase inhibitor that reduces estrogen production, thereby suppressing the growth of hormone-sensitive breast cancer cells. The combination has demonstrated significantly improved progression-free survival, objective response rate, and clinical benefit rate compared to letrozole alone in this patient population[1][5][6].

Brand names
FemaraTykerb
Other names
lapatinib and letrozoleletrozole plus lapatinib
02

Targets

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

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