Drug intelligence / Profile preview

TC14012

Development stage
Preclinical
Lead developer
Kyoto University
Modality
Peptides
Administration
Intravenous, Subcutaneous, Intraperitoneal
01

Overview

TC14012 is a cyclic peptide that serves as a potent agonist of the atypical chemokine receptor 3 (ACKR3), also known as CXCR7, and as an antagonist of the C-X-C chemokine receptor type 4 (CXCR4). It is specifically recognized as a $\beta$-arrestin-biased agonist of CXCR7, meaning it selectively activates the $\beta$-arrestin signaling pathway over G-protein-mediated pathways. Preclinical research has demonstrated that TC14012 possesses anti-metastatic, anti-fibrotic, and cardioprotective properties. It has been shown to inhibit lung cancer metastasis by preventing endothelial necroptosis, ameliorate liver fibrosis by enhancing the therapeutic effects of mesenchymal stem cells, and improve cardiac function following myocardial infarction by promoting angiogenesis and reducing apoptosis. Additionally, TC14012 has been utilized in the development of radiolabeled PET imaging tracers for the detection of CXCR4 expression in various cancers.

02

Targets

CXCR7 (CXC chemokine receptor 7)CXCR4 (C-X-C motif chemokine receptor 4)

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