Drug intelligence / Profile preview

iRGD-10R-siRNA

Development stage
Preclinical
Lead developer
Carnegie Mellon University Qatar
Modality
Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Peptides, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intravenous
01

Overview

iRGD-10R-siRNA is a preclinical, research-stage cell-penetrating peptide (CPP)-based siRNA delivery complex. It is a bifunctional nanocomplex consisting of the internalizing RGD (iRGD) tumor-penetrating peptide coupled with a polyarginine (10R) cell-penetrating peptide, which together form a positively charged carrier that electrostatically complexes with negatively charged siRNA targeting Lactate Dehydrogenase C (LDHC). The iRGD motif targets integrin αvβ3 to facilitate tumor-selective uptake and penetration, while the 10R peptide facilitates cellular internalization. Once inside the cell, the siRNA silences LDHC, a cancer-associated gene involved in the DNA damage response and tumor mitotic fidelity. This compound has been investigated primarily for the treatment of triple-negative breast cancer (TNBC), with anti-tumor effects assessed in TNBC xenograft zebrafish models.

Other names
iRGD-10R:siLDHCiRGD-10R:siLDHC#2iRGD-10R:siRNA
02

Targets

αVβ3 (Integrin αVβ3)LDH (L-lactate dehydrogenase A chain)

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