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Tonix Pharmaceuticals Announces the Isolation and Characterization of the (S)-Isomer of Tianeptine, TNX-4300 (Estianeptine), Now Under Development for Psychiatric and Neurodegenerative Diseases
TNX-4300 is a Dual PPAR-β/δ and PPAR-γ Agonist, Free from µ-Opioid Receptor Activity TNX-4300’s Mechanism of Restoring Neuroplasticity Supports Development as
About this update from Tonix Pharmaceuticals Holding Corp.
[{"type":"text","content":"TNX-4300 is a Dual PPAR-β/δ and PPAR-γ Agonist, Free from µ-Opioid Receptor Activity TNX-4300’s Mechanism of Restoring Neuroplasticity Supports Development as a First-in-Class Oral Therapy for Depression, Bipolar Disorder, Alzheimer’s Disease and Parkinson’s Disease Restoring Atrophied Neuronal Connections in Psychiatric and Neurological Diseases Seen as Paramount to Achieving Better and More Durable Outcomes CHATHAM, N.J., May 23, 2023 (GLOBE NEWSWIRE) -- Tonix Pharmaceuticals Holding Corp. (Nasdaq: TNXP) (Tonix or the Company), a clinical-stage biopharmaceutical company, today announced the isolation and functional characterization of the two mirror image isomers of racemic tianeptine, which is marketed outside the U.S. as a treatment for major depressive disorder (MDD). Tonix scientists discovered that the (S)-isomer of tianeptine activates PPAR-β/δ, restores neuroplasticity in neuronal tissue culture and is free of µ-opioid receptor activity. In contrast, (R)-tianeptine activates the µ-opioid receptor and lacks PPAR-β/δ activity. Based on these discoveries, Tonix has begun preclinical development of the (S)-isomer, TNX-4300 (estianeptine)*, as a treatment for MDD, bipolar disorder, Alzheimer’s disease, and Parkinson’s disease. Tonix is planning to submit data supporting tianeptine’s mechanism of action for presentation at upcoming scientific conferences and for publication in peer reviewed journals. Tonix recently announced that tianeptine, a drug marketed outside the U.S. for more than 30 years, is a plastogen1 that acts on nuclear PPAR-β/δ and PPAR-γ in neurons and glia to restore neuronal connectivity in depression and has direct applicability in a number of neurodegenerative diseases in which neuronal connections are atrophying.2 The newly reported mechanism also provided clarity on why tianeptine does not cause sexual dysfunction, weight gain or several other treatment-limiting toxicities frequently associated with antidepressants. “The tianeptine marketed outside the U.S. for treating depression is a 1:1 racemic mixture of two mirror image isomers,” said Seth Lederman, M.D., Chief Executive Officer of Tonix Pharmaceuticals. “The discovery reported today is that the (S)-isomer is responsible for tianeptine’s activity on PPAR-β/δ and restoring neuroplasticity, and the (R)-isomer for its off-target activity on the µ-opioi...