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Assessment of the Pharmacokinetics, Disposition, and Duration of Action of the Tumour-Targeting Peptide CEND-1

Authors: Harri A Järveläinen, Christian Schmithals, Maike von Harten, Bianca Kakoschky, Thomas J Vogl, Stephen Harris, Claire Henson, Gemma Bullen-Clerkson, Albrecht Piiper

CEND-1 peptide (iRGD) is a bifunctional cyclic peptide that enhances delivery and efficacy of anti-cancer agents by modulating the tumour microenvironment. This study evaluated its pharmacokinetics (PK), tissue distribution, tumour selectivity, and duration of action in animals and humans. Following intravenous administration, CEND-1 showed rapid plasma clearance but sustained tumour retention. Radiolabelled CEND-1 localized to tumours despite rapid systemic and tissue clearance. In hepatocellular carcinoma models, tumour penetration effects lasted at least 24 hours. These findings suggest CEND-1 has a favourable PK profile and prolonged tumour-targeting capability, supporting its potential to improve anti-cancer drug delivery.

Pharmaron radiolabelled the peptide using [3H]-N-succinimidyl propionate and tissue distribution studies in orthotopic 4T1 mammary carcinoma tumour bearing mice were performed using Quantitative Whole Body Autoradiography (QWBA).

International Journal of Molecular Sciences 2023, Mar 16; 24(6)

DOI: 10.3390/ijms24065700

Access the publication at https://pubmed.ncbi.nlm.nih.gov/36982773/