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LErafAON-ETU
- Development stage
- Phase 1
- Lead developer
- INSYS Therapeutics
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
LErafAON-ETU is a liposome-entrapped antisense oligonucleotide (ASO) designed to target and inhibit the expression of the c-raf (Raf-1) protein. Raf-1 is a serine/threonine protein kinase that acts as a key mediator in the MAPK/ERK signaling pathway, which is frequently overactive in various cancers, driving tumor cell proliferation and survival. By binding to c-raf mRNA, the ASO triggers its degradation or prevents translation, thereby reducing Raf-1 protein levels and potentially inhibiting tumor growth. The "ETU" (Easy-to-Use) designation refers to a specific intravenous formulation developed by Insys Therapeutics to simplify clinical administration. This therapeutic candidate was evaluated in Phase I clinical trials for patients with advanced solid tumors that were unresponsive to standard treatments.
- Other names
- Liposome Entrapped c-raf Antisense Oligonucleotide Easy-to-UseLiposome Entrapped c-raf Antisense Oligonucleotide
02
Targets
RAF1 (c-Raf-1 (Y340D/Y341D))
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