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ARC183

Development stage: Discontinued
Lead developer: Takeda
Modality: miRNA Mimics → MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Natural RNA Aptamers → RNA Aptamers → RNA Therapeutics → Nucleic Acid Therapeutics, DNA Vaccines → Plasmid DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Spiegelmers → RNA Aptamers → RNA Therapeutics → Nucleic Acid Therapeutics, Unmodified DNA Aptamers → DNA Aptamers → DNA Therapeutics → Nucleic Acid Therapeutics, Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Gene Editing mRNA → mRNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Vaccine mRNA → mRNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Long Non-coding RNA (lncRNA) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Aptamers → DNA Aptamers → DNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Protein Replacement mRNA → mRNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, miRNA Inhibitors → MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Gene Therapy Plasmids → Plasmid DNA → DNA Therapeutics → Nucleic Acid Therapeutics
Administration: Intravenous

Overview

ARC183 is a DNA aptamer—a single-stranded DNA oligonucleotide of 15 deoxynucleotides—that forms a specific three-dimensional structure enabling high-affinity and selective binding to thrombin. Developed as an anticoagulant for acute cardiovascular settings such as coronary artery bypass graft (CABG) surgery and other procedures requiring rapid-onset and reversible anticoagulation, ARC183 acts by inhibiting thrombin’s pro-exosite I functions. This results in the inhibition of fibrinogen cleavage and platelet activation. The drug was designed for rapid onset and short half-life to allow quick reversal of its effects after medical procedures. Despite promising early results in Phase I trials demonstrating stable dose-dependent anticoagulation with rapid onset, development was discontinued due to suboptimal dosing profiles that limited clinical utility compared to newer agents[1][2][3][5][6][7][8].

Targets

F2 (Thrombin)

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