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isis 5132
- Development stage
- Phase 2
- Lead developer
- Ionis Pharmaceuticals
- Modality
- 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
- Administration
- Intravenous
01
Overview
ISIS 5132 is a synthetic, 20-base phosphorothioate antisense oligodeoxynucleotide designed to specifically hybridize to and down-regulate c-raf kinase (RAF1) messenger RNA. By inhibiting the expression of c-Raf, a key protein kinase in the mitogen-activated protein kinase (MAPK) signaling pathway, ISIS 5132 aims to suppress oncogenic transformation and tumor cell proliferation. It was developed for use as an antineoplastic agent in various solid tumors including ovarian epithelial carcinoma, metastatic breast cancer, colorectal cancer, and non-small cell lung cancer. Clinical studies have shown that it can be administered intravenously with manageable toxicity profiles[1][2][5].
- Other names
- c-Raf antisense oligonucleotide ISIS 5132
02
Targets
RAF1 (c-Raf-1 (Y340D/Y341D))
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