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CPP-PMO antimiR-218
- Development stage
- Preclinical
- Lead developer
- INCLIVA Biomedical Research Institute
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous
01
Overview
CPP-PMO antimiR-218 is a **peptide-conjugated phosphorodiamidate morpholino oligomer (PMO)** designed to target and inhibit microRNA-218 (miR-218). It consists of a PMO antisense oligonucleotide sequence directed against miR-218, chemically conjugated to a cell-penetrating peptide (CPP) such as 9b2, 9b2KC, or 6aKC, which enables efficient intracellular delivery. The drug acts as an antimiR, blocking miR-218 activity and thereby upregulating MBNL1 protein, which is beneficial for the treatment of **myotonic dystrophy type 1 (DM1)**. In preclinical models, intravenous administration improved molecular, tissue, and functional parameters in DM1 mouse models. CPP conjugation markedly increased delivery efficiency and therapeutic index versus previous antagomiRs, with R-to-K amino acid substitutions (e.g. in 9b2KC) decreasing cellular toxicity while maintaining high potency[1].
- Other names
- cell penetrating peptide phosphorodiamidate morpholino oligomer antimiR-218CPP-PMO anti-miR-218
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