Drug intelligence / Profile preview

Por-HDL-NPs

Development stage
Preclinical
Lead developer
South Australia Health and Medical Research Institute
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Por-HDL-NPs (Porphyrin-lipid HDL mimetic nanoparticles) are biomimetic theranostic agents designed for the multimodal imaging and treatment of atherosclerotic cardiovascular disease. These nanoparticles consist of a porphyrin-lipid conjugate core and an outer shell functionalized with the R4F peptide, a mimetic of apolipoprotein A-I (ApoA-I). The porphyrin component allows for near-infrared fluorescence (NIRF) imaging and positron emission tomography (PET) when chelated with Copper-64 (64Cu). The R4F peptide targets the scavenger receptor class B type I (SR-BI) on macrophages, facilitating cholesterol efflux. Beyond cholesterol transport, Por-HDL-NPs exhibit potent anti-inflammatory effects by inhibiting the NLRP3 inflammasome and the NF-κB signaling pathway, leading to reduced secretion of pro-inflammatory cytokines like IL-1β and CCL5. Preclinical studies in Apoe-/- mice have demonstrated that Por-HDL-NPs can effectively localize to atherosclerotic plaques, detect increases in plaque size, and significantly reduce plaque area and inflammation.

Other names
Porphyrin-lipid HDL mimetic nanoparticles64Cu-Por-HDL-NPs
02

Targets

NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)SCARB1 (Scavenger receptor class B member 1)NF-κB

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