Drug intelligence / Profile preview

doxorubicin + lapatinib

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Doxorubicin + lapatinib is a combination therapy used primarily in the treatment of HER2-positive metastatic breast cancer. Doxorubicin is an anthracycline antibiotic that acts as a cytotoxic agent by intercalating into DNA and inhibiting topoisomerase II activity, leading to DNA strand breaks and apoptosis. It also generates reactive oxygen species that contribute to its antitumor effects[2]. Lapatinib is a small molecule tyrosine kinase inhibitor developed by GlaxoSmithKline (GSK) that targets both epidermal growth factor receptor (EGFR/HER1/ERBB1) and human epidermal growth factor receptor type 2 (HER2/ERBB2), blocking their intracellular phosphorylation domains to prevent downstream signaling involved in tumor cell proliferation[4][6]. The combination has shown efficacy in patients with HER2-positive metastatic breast cancer who have progressed on trastuzumab-based therapies and may be particularly suitable for those at risk of cardiotoxicity or with brain metastases due to its ability to cross the blood-brain barrier[3].

Brand names
DoxilCaelyx
Other names
pegylated liposomal doxorubicin
02

Targets

TOP2A (DNA topoisomerase II)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ABCB1 (P-glycoprotein)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)ABCG2 (Breast cancer resistance protein)

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