Drug intelligence / Profile preview

lapatinib + vinorelbine

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

Overview

Lapatinib + vinorelbine is a combination therapy used primarily for the treatment of metastatic HER2-positive breast cancer, particularly in patients who have previously received other treatments. Lapatinib is a small molecule tyrosine kinase inhibitor that targets the intracellular domains of both epidermal growth factor receptor (EGFR/HER1/ERBB1) and human epidermal growth factor receptor 2 (HER2/ERBB2), thereby inhibiting tumor cell proliferation driven by these receptors[8]. Vinorelbine is a semi-synthetic vinca alkaloid that disrupts microtubule formation by binding to tubulin, leading to mitotic arrest and apoptosis in rapidly dividing cells[6]. The combination has demonstrated efficacy and manageable toxicity profiles in phase I/II clinical trials, offering an all-oral regimen option for patients with HER2-positive metastatic breast cancer who may have been heavily pretreated[1][3][4][5].

Brand names
TykerbNavelbine
Other names
lapatinib + vinorelbine
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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