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Drug intelligence / Profile preview
iRGD-2DG-NanoHT
- Development stage
- Preclinical
- Lead developer
- Kanazawa University
- Modality
- Small Molecules, Peptides, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
iRGD-2DG-NanoHT (iRGD-2DG-nanoheater) is a photothermally modulated liposomal drug delivery system designed for the targeted treatment of liver cancer (hepatocellular carcinoma). The formulation consists of liposomes encapsulating the glycolysis inhibitor 2-deoxy-D-glucose (2DG) and embedding a near-infrared (NIR) absorbing photothermal dye (nanoheater) within the lipid bilayers. The surface of the liposomes is modified with the tumor-penetrating cyclic peptide iRGD (CRGDKGPDC) to target integrins and neuropilin-1 (NRP-1) overexpressed on tumor cells and vasculature. Upon near-infrared light irradiation, the photothermal dye generates localized heat, triggering a phase transition in the lipid bilayer that enables the controlled, efficient release of 2DG. This dual-action approach suppresses the Warburg effect, induces endoplasmic reticulum (ER) stress-induced apoptosis via AMPK phosphorylation, triggers ferroptosis via reduction of the GSH/GPX4 axis, and stimulates HMGB-1-mediated antitumor immunity.
- Other names
- iRGD-2DG-nanoheateriRGD2DG-nanoheateriRGD 2DG-nanoheater
02
Targets
αVβ3 (Integrin αVβ3)αVβ5 (Integrin αVβ5)NRP1 (Neuropilin-1)
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