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lapatinib + paclitaxel
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Lapatinib + paclitaxel is a combination therapy used primarily in oncology, particularly for HER2-positive cancers. 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), blocking their autophosphorylation and downstream signaling pathways such as PI3K/Akt and MAPK, leading to tumor cell growth arrest or apoptosis[1][6]. Paclitaxel is a microtubule-stabilizing agent that inhibits cell division by promoting tubulin polymerization and preventing microtubule disassembly. The combination has demonstrated clinical activity in HER2-positive advanced breast cancer after prior therapies, as well as in HER2 FISH-positive IHC3+ advanced gastric cancer[8]. Lapatinib was developed by GlaxoSmithKline.
- Other names
- None
02
Targets
TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)ABCB1 (P-glycoprotein)EGFR T790M (Epidermal growth factor receptor T790M mutant)ABCG2 (Breast cancer resistance protein)
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