Drug intelligence / Profile preview

anti-miR-21 oligonucleotides

Development stage
Preclinical
Lead developer
Regulus Therapeutics
Modality
Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intravenous, Subcutaneous
01

Overview

Anti-miR-21 oligonucleotides are synthetic, chemically modified single-stranded RNA molecules designed to target and inhibit microRNA-21 (miR-21). miR-21 is an oncogenic and pro-fibrotic microRNA that is consistently upregulated in various cancers and fibrotic diseases. By binding to mature miR-21 through sequence complementarity, these oligonucleotides prevent miR-21 from interacting with its target mRNAs, thereby derepressing key tumor suppressor and metabolic genes such as PTEN, PDCD4, and PPARα. This inhibition leads to reduced cell proliferation, increased apoptosis, and attenuated tissue fibrosis. Preclinical and clinical development of anti-miR-21 oligonucleotides, such as lademirsen (RG-012), has focused on indications like Alport syndrome, myocardial fibrosis, and various malignancies, although clinical translation has faced challenges regarding efficacy.

Other names
anti-microRNA-21 oligonucleotidesanti-microRNA21 oligonucleotidesanti-microRNA 21 oligonucleotidesanti-miR-21anti-miR21anti-miR 21anti-miR-21 oligonucleotideanti-miR21 oligonucleotideanti-miR 21 oligonucleotidemicroRNA-21 inhibitorsmicroRNA21 inhibitorsmicroRNA 21 inhibitorsmiR-21 inhibitorsmiR21 inhibitorsmiR 21 inhibitors
02

Targets

miR-21 (MicroRNA-21)

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