Drug intelligence / Profile preview

177Lu-FA-DOTA-PEG-PLGA

Development stage
Unknown
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intraperitoneal
01

Overview

177Lu-FA-DOTA-PEG-PLGA is a nanoparticle-based radiopharmaceutical designed as a targeted, sustained-release drug delivery system for cancer therapy—specifically for ovarian cancer. It consists of a poly(lactic-co-glycolic acid) (PLGA) nanoparticle core functionalized with polyethylene glycol (PEG), equipped with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) as a chelator for the radioactive isotope lutetium-177 (^177Lu), and conjugated to folic acid (FA) as a targeting ligand. The radiolabeled nanoparticles exhibit long circulation times and low renal clearance, and are administered via intraperitoneal injection to exploit folate receptor-mediated uptake by ovarian cancer cells. The mechanism of action combines targeted beta-radiation therapy (via ^177Lu emission causing localized cell death) with increased tumor specificity from FA targeting. Preclinical studies have shown antitumor efficacy in relevant mouse models[1][3][4][5].

02

Targets

DNAFOLR1 (FRα)

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