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| Trade names | Genasense |
| Other names | G3139 |
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| Formula | C172H221N62O91P17S17 |
| Molar mass | 5684.58 g·mol−1 |
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Oblimersen (INN, trade nameGenasense; also known asAugmerosen andbcl-2 antisense oligodeoxynucleotide G3139) is anantisenseoligodeoxyribonucleotide being studied as a possible treatment for several types ofcancer, includingchronic lymphocytic leukemia,B-cell lymphoma, andbreast cancer. It may kill cancer cells by blocking the production ofBcl-2—aprotein that makes cancer cells live longer—and by making them more sensitive to chemotherapy.
The antisenseoligonucleotide drug oblimersen was developed byGenta Incorporated to target Bcl-2. An antisense DNA or RNA strand is non-coding and complementary to the coding strand (which is the template for producing respectively RNA or protein). An antisense drug is a short sequence of RNA which hybridises with and inactivates mRNA, preventing the protein from being formed.[citation needed]
It was shown that the proliferation of humanlymphomacells (with t(14;18) translocation) could be inhibited by antisense RNA targeted at the startcodon region of Bcl-2mRNA.In vitro studies led to the identification of oblimersen, which is complementary to the first 6 codons of Bcl-2 mRNA.[1]
These have shown successful results in Phase I/II trials for lymphoma, and a large Phase III trial was launched in 2004.[2]
By the first quarter 2010, the drug had not receivedFDA approval due to disappointing results in a melanoma trial. Although its safety and efficacy have not been established for any use, Genta Incorporated still[when?] claims on its website that studies are currently under way to examine the potential role of oblimersen in a variety of clinical indications.
Recent studies in 2023 continue to explore the potential of oblimersen in combination with other therapies. Preclinical models have demonstrated that oblimersen, when combined with vinorelbine, significantly inhibits tumor growth and prolongs survival in NSCLC. These findings suggest that combining oblimersen with other chemotherapeutic agents could enhance its efficacy and potentially overcome previous clinical challenges.[1]
