Lipid antisens oligonucleotide targeting fxyd2 as a therapeutic agent for pain management

The present invention relates to an inhibitor of FXYD2 gene expression for use in a method for treating neuropathic pain in a patient in need thereof. The invention also relates to a pharmaceutical composition comprising an inhibitor of FXYD2 gene expression, wherein said pharmaceutical composition is formulated for a direct administration into the peripheral nervous system (PNS) of a patient (e.g., formulated for intrathecal administration).rnThe invention also relates to an inhibitor of FXYD2 wherein said inhibitor reduces the expression and/or activity of FXYD2 in a subject in need thereof and targets at least the region comprising or consisting of the nucleotides 219-229 of SEQ ID NO: 3. rnInventors have shown that targeting a region of FXYD2 can be used to inhibit and/or reduce the expression and/or activity of FXYD2. They have designed and synthesized an antisense oligonucleotide (SEQ ID NO: 4) targeting the rat and human FXYD2 gene. The have performed intrathecal injection of FXYD2 optimized ASO in two rat models of pain (neuropathic and inflammatory pain). They have shown that FXYD2 ASO efficiently reduces its expression in rat Dorsal root ganglion (DRG). The have demonstrated that FXYD2 ASO dramatically reduces neuropathic pain in the Spinal Nerve Ligation (SNL) rat model and analgesic effect of FXYD2 ASO on neuropathic pain is greater than that of Ziconotide, the current market leader. They also have shown that FXYD2 ASO dramatically reduces inflammatory pain in Complete Freund’s Adjuvant (CFA)-induced rat model. rn

Patent Application number: European Procedure (Patents) (EPA) - 09 Juil. 2014 - 14 306 114.1
PATTYN AlexandreVENTEO StéphanieVENTEO Stéphanie
Sci Rep. 2016 Nov 2;6:36407. doi: 10.1038/srep36407.PLoS One. 2012;7(1):e29852. doi: 10.1371/journal.pone.0029852. Epub 2012 Jan 13.



    Business Developper
    Anne COCHI
    Business Development Manager
    Patent filling date: 09-07-2014
    Rare disease: No
    Second indication: No

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