Drug intelligence / Profile preview

lapatinib + chemotherapy

Development stage
Unknown
Lead developer
GSK
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Lapatinib + chemotherapy refers to the use of **lapatinib**, a small molecule tyrosine kinase inhibitor targeting both epidermal growth factor receptor (EGFR/HER1) and human epidermal growth factor receptor type 2 (HER2), in combination with a chemotherapeutic agent, most commonly **capecitabine**. This combination is primarily utilized for patients with advanced or metastatic HER2-positive breast cancer who have progressed on prior therapies including anthracyclines, taxanes, and trastuzumab. Lapatinib blocks the intracellular tyrosine kinase domains of EGFR and HER2, thereby inhibiting tumor cell growth. Clinical studies have demonstrated that adding lapatinib to capecitabine significantly improves progression-free survival and reduces the risk of disease progression versus chemotherapy alone[2][3][4][1]. The combination may also include other chemotherapy agents, such as paclitaxel, depending on the specific protocol[1].

02

Targets

DDB2 (Damage-specific DNA-binding protein 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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