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irinotecan + oblimersen
- Development stage
- Unknown
- Lead developer
- Genta
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous
01
Overview
Irinotecan + oblimersen is an investigational combination therapy studied primarily for metastatic or recurrent colorectal cancer. Irinotecan is a small molecule topoisomerase I inhibitor that interferes with DNA replication in cancer cells, leading to cell death. Oblimersen (also known as G3139 or augmerosen) is an antisense oligonucleotide designed to bind specifically to Bcl-2 mRNA and inhibit its translation; Bcl-2 is a protein that helps tumor cells resist apoptosis. By downregulating Bcl-2 expression with oblimersen, tumor cells may become more sensitive to the cytotoxic effects of chemotherapy agents like irinotecan. The combination has been evaluated in phase I/II clinical trials for safety and preliminary efficacy in patients with advanced colorectal carcinoma[1][2][3].
- Other names
- irinotecan + oblimersen sodiumirinotecan + G3139irinotecan + augmerosen
02
Targets
BCL-2 (BCL-2 family)TOP1 (DNA Topoisomerase I)
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