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apatorsen
- Development stage
- Discontinued
- Lead developer
- Sonus 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
Apatorsen is a second-generation antisense oligonucleotide designed to inhibit the production of heat shock protein 27 (Hsp27), a cytoprotective chaperone protein that is overexpressed in many human cancers, including prostate, lung, breast, ovarian, bladder, renal, pancreatic cancers, multiple myeloma and liver cancer. By binding to Hsp27 mRNA and blocking its translation into functional protein, apatorsen suppresses tumor cell expression of Hsp27. This may induce tumor cell apoptosis and enhance sensitivity to cytotoxic agents by disabling cancer cells' defenses against stressors such as chemotherapy. The drug was developed as an investigational therapy for various solid tumors but has been discontinued in clinical development for all major indications.
- Other names
- apatorsen sodiumApatorsen [USAN]UNII-IFJ6X26JW6UNII-IFJ-6X26JW6UNII-IFJ 6X26JW6OGX 427OGX427OGX-427
02
Targets
HSPB1 (Heat shock protein beta-1)
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