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EZN-3042
- Development stage
- Discontinued
- 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-3042 is a locked nucleic acid antisense oligonucleotide (LNA-ON) designed to inhibit the expression of survivin, a protein encoded by the BIRC5 gene that plays an anti-apoptotic role in cancer cells. By hybridizing to survivin mRNA, EZN-3042 blocks its translation, thereby reducing survivin protein levels and promoting apoptosis in tumor cells that overexpress this protein. The drug was developed using third-generation antisense technology to enhance biological stability and potency. It was investigated primarily for use in relapsed or refractory acute lymphoblastic leukemia (ALL), lymphoma, and advanced solid tumors. Clinical development included phase 1 trials as both monotherapy and in combination with chemotherapy; however, further development was discontinued due to tolerability issues at effective doses[1][2][3][4][5].
- Other names
- survivin mRNA antagonist EZN-3042
02
Targets
BIRC5 (Survivin)
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