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PEG-E-TC11
- Development stage
- Preclinical
- Lead developer
- Keio University
- Modality
- Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intraperitoneal
01
Overview
PEG-E-TC11 is a novel, water-soluble, PEGylated phenylphthalimide derivative developed by researchers at Keio University Faculty of Pharmacy and IDAC Theranostics. It is a polymer-drug conjugate consisting of the active ingredient TC11 (2-(2,6-diisopropylphenyl)-5-amino-1H-isoindole-1,3-dione) linked to polyethylene glycol (PEG) via an ester bond. This modification significantly improves the water solubility of TC11 from 0.02 mg/mL to 88.9 mg/mL and enhances its pharmacokinetic profile, including increased peak blood concentration and extended half-life. Unlike conventional immunomodulatory drugs (IMiDs) such as thalidomide and lenalidomide, PEG-E-TC11 does not bind to cereblon (CRBN). Instead, it exerts its anti-tumor effects by binding to α-tubulin and nucleophosmin-1 (NPM1), leading to G2/M cell cycle arrest and apoptosis. It is being investigated as a potential therapeutic for high-risk multiple myeloma, particularly in patients with poor-prognosis cytogenetic abnormalities such as t(4;14) and del17p.
- Other names
- polyethylene glycol-linked TC11
02
Targets
NPM1 (Nucleophosmin)TUBA (Tubulin alpha/beta dimer)
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