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EZN-4176
- Development stage
- Phase 1
- Lead developer
- Enzon Pharmaceuticals
- 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
01
Overview
EZN-4176 is a third-generation locked nucleic acid (LNA) antisense oligonucleotide designed to target the androgen receptor (AR) mRNA. It specifically binds to the hinge region (exon 4) of AR mRNA, leading to degradation of full-length AR mRNA and some splice variants, resulting in decreased AR protein expression. This mechanism inhibits AR-induced tumor cell growth and promotes apoptosis in tumor cells that overexpress the androgen receptor. EZN-4176 was developed for the treatment of castration-resistant prostate cancer (CRPC), but clinical activity at tested doses was minimal and associated with reversible liver enzyme elevations[1][2][3][4][5][7].
- Other names
- androgen receptor antisense oligonucleotide ezn-4176
02
Targets
Androgen receptor mRNA (hinge region)
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