Drug intelligence / Profile preview

NGR-hTNF + pegylated liposomal doxorubicin

Development stage
Discontinued
Lead developer
AGC Biologics
Modality
Bacterial Toxin Conjugates → Immunotoxins → Antibody Conjugates → Antibody-Based Therapeutics, Cytokines & Interferons → Recombinant Proteins and Enzymes, Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

NGR-hTNF + pegylated liposomal doxorubicin is a combination drug regimen consisting of a tumor vessel-targeting fusion protein (NGR-hTNF) and a liposomal formulation of the chemotherapy agent doxorubicin. NGR-hTNF is a recombinant protein in which the human tumor necrosis factor-alpha (hTNF-α) is fused with an NGR (asparagine-glycine-arginine) peptide, directing it specifically to CD13 isoforms overexpressed on tumor endothelium. This targeting increases local cytokine concentrations within tumor vasculature, impairing pro-survival signaling and enhancing tumor vessel permeability, thus promoting intratumoral delivery of therapies[1][3]. Pegylated liposomal doxorubicin (PLD, Caelyx) is doxorubicin encapsulated in pegylated (polyethylene glycol-coated) liposomes, prolonging its circulation time and favoring deposition into tumors by exploiting leaky tumor vasculature. Its antineoplastic activity comes from inhibiting topoisomerase II, leading to DNA strand breaks and cell death[2][4]. The combination is developed to enhance chemotherapy penetration and efficacy by combining vessel-targeted cytokine therapy with cytotoxic chemotherapy.

Brand names
Caelyx
Other names
NGR-hTNF + PLDNGR-hTNF + Caelyx
02

Targets

DNATOP2A (DNA topoisomerase II)TNFRSF1A (Tumor necrosis factor receptor superfamily member 1A)ANPEP (Aminopeptidase N)

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