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folic acid + hydroxyethyl starch + epirubicin + imiquimod
- Development stage
- Preclinical
- Lead developer
- Pfizer
- Modality
- Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravesical
01
Overview
FA-HES-EPI/IMQ is a research-stage nanomedicine formulation designed for the intravesical chemoimmunotherapy of bladder cancer. It consists of folic acid-modified hydroxyethyl starch (FA-HES) conjugated to epirubicin (EPI) via an acid-sensitive hydrazone bond, forming a prodrug (FA-HES-EPI) that encapsulates the Toll-like receptor 7 (TLR7) agonist imiquimod (IMQ) within its hydrophobic core. This system forms micelles that target tumor cells via folate receptor-mediated endocytosis. Once internalized or within the acidic tumor microenvironment, the pH-responsive hydrazone bonds cleave, triggering the controlled release of both the chemotherapeutic epirubicin and the immunomodulator imiquimod. This dual-action approach aims to enhance tumor cell killing while repolarizing tumor-associated macrophages from an M2 to an M1 phenotype, thereby overcoming the immunosuppressive tumor microenvironment.
- Other names
- FA-HES-EPI/IMQ micellesfolate-conjugated hydroxyethyl starch micelles for co-delivery of epirubicin and imiquimod
02
Targets
DNAFOLR1 (FRα)TOP2A (DNA topoisomerase II)TLR7 (Toll-like receptor 7)
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