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oblimersen
- Development stage
- Phase 3
- Lead developer
- Genta
- Modality
- Small Molecules, MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, 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, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
01
Overview
Oblimersen is a phosphorothioate antisense oligonucleotide designed to target the initiation codon region of Bcl-2 mRNA. By binding to this region, it inhibits the translation of Bcl-2 mRNA and reduces expression of the anti-apoptotic Bcl-2 protein. This mechanism promotes tumor cell apoptosis and may enhance the efficacy of standard cytotoxic chemotherapy. Oblimersen was developed primarily for use in hematologic malignancies such as chronic lymphocytic leukemia (CLL) and has also been studied in advanced melanoma and acute myeloid leukemia (AML). Despite showing promise in preclinical studies, clinical trials did not demonstrate significant improvement in survival outcomes when added to standard therapies[1][3][4][6].
- Brand names
- Genasense
- Other names
- oblimersen sodiumoblimersenGenasense
02
Targets
TLR9 (Toll-like receptor 9)BCL-2 (BCL-2 family)
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