Certepetide

Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].

O=C1[C@@]2([H])N(C(CNC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@H](CSSC[C@H](NC([C@@H](N1)CC(O)=O)=O)C(N)=O)NC(C)=O)=O)CCCNC(N)=N)=O)=O)CC(O)=O)=O)CCCCN)=O)=O)CCC2

[1]International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022 |[2]Ruoslahti Erkki, et al. Methods for treating pancreatic cancer and other solid tumors. WO2021226148.|[3]Andrew Peter Dean, et al. Updated single institution outcome data from the first-in-human CEND-1 trial in metastatic pancreatic cancer. Journal of Clinical Oncology 2021 39:15_suppl, e16274-e16274|[4]Harri A Järveläinen, et al. Assessment of the Pharmacokinetics, Disposition, and Duration of Action of the Tumour-Targeting Peptide CEND-1. Int J Mol Sci. 2023 Mar 16;24(6):5700.|[5]Schmithals, C, et al. Improving Drug Penetrability with iRGD Leverages the Therapeutic Response to Sorafenib and Doxorubicin in Hepatocellular Carcinoma. Cancer Res. 2015 Aug 1;75(15):3147-54.