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Drug intelligence / Profile preview
lapatinib + pegylated liposomal doxorubicin
- Development stage
- Phase 1
- Lead developer
- GSK
- Modality
- Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Oral, Intravenous
01
Overview
Lapatinib + pegylated liposomal doxorubicin is a combination therapy used primarily in the treatment of HER2-positive metastatic breast cancer, especially in patients who have progressed on trastuzumab or are at increased risk for cardiotoxicity. Lapatinib is an oral small molecule tyrosine kinase inhibitor targeting both the human epidermal growth factor receptor 2 (HER2/ERBB2) and epidermal growth factor receptor (EGFR/ERBB1), thereby inhibiting downstream signaling pathways involved in tumor cell proliferation and survival. Pegylated liposomal doxorubicin (PLD) is a formulation of the anthracycline antibiotic doxorubicin encapsulated within polyethylene glycol-coated liposomes, which prolongs circulation time, enhances tumor delivery via the enhanced permeability and retention effect, and reduces cardiotoxicity compared to conventional doxorubicin. The combination offers a cardiosparing alternative that can cross the blood-brain barrier—an important consideration since brain metastases are common in this patient population[1][2][6].
- Brand names
- Lipo-Dox
- Other names
- lapatinib plus pegylated liposomal doxorubicinlapatinib + PLD
02
Targets
DNAEGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP2A (DNA topoisomerase II)
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