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vintafolide + pegylated liposomal doxorubicin
- Development stage
- Phase 2
- Lead developer
- Merck
- Modality
- Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
This agent is a **combination of vintafolide (EC145)**, a folate receptor-targeted small molecule-drug conjugate, and **pegylated liposomal doxorubicin (PLD)**, a liposome-formulated anthracycline chemotherapeutic. **Vintafolide targets the folate receptor alpha (FRα) expressed on many epithelial ovarian cancers, delivering the vinca alkaloid desacetylvinblastine monohydrazide (DAVLBH) directly into FR-expressing tumor cells, thereby increasing cytotoxicity to cancer cells while reducing exposure to normal tissues. PLD is a pegylated, liposomal formulation of doxorubicin with established cytotoxic effects via topoisomerase II inhibition and intercalation into DNA.** This combination showed statistically significant improvement in progression-free survival over PLD monotherapy in phase II trials for platinum-resistant ovarian cancer, particularly among patients with high folate receptor expression[1][4][5][7][9]. The combination was developed with the aim to selectively target and kill FR-positive cancer cells while minimizing toxicity compared to untargeted chemotherapies. Development of the combination was discontinued after failure to demonstrate sufficient benefit in late-stage studies[9].
- Other names
- vintafolide plus pegylated liposomal doxorubicinvintafolide + PLDEC145 + DOXIL
02
Targets
FOLR1 (FRα)TOP2A (DNA topoisomerase II)
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