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Tonix Pharmaceuticals Announces Pharmacology and Medicinal Chemistry Results that Reveal the Molecular Mechanism of Action of Tianeptine, the Active Ingredient of TNX-601 ER, in Treating Depression
Research Supports Direct Role for Restoring Neuroplasticity and Upsets Previously Held Beliefs About the Significance of Neurotransmitters in Treating
About this update from Tonix Pharmaceuticals Holding Corp.
[{"type":"text","content":"Research Supports Direct Role for Restoring Neuroplasticity and Upsets Previously Held Beliefs About the Significance of Neurotransmitters in Treating Depression Findings Explain Why Tianeptine Is Not Associated with Sexual Dysfunction and Weight Gain Mechanism Supports Development of TNX-601 ER for a Broad Range of Neurodegenerative Diseases and Psychiatric Disorders CHATHAM, N.J., May 17, 2023 (GLOBE NEWSWIRE) -- Tonix Pharmaceuticals Holding Corp. (Nasdaq: TNXP) (Tonix or the Company), a clinical-stage biopharmaceutical company, today announced the molecular mechanism of action of tianeptine, the active ingredient of TNX-601 ER (tianeptine hemioxalate extended-release tablets), currently in Phase 2 clinical development for the treatment of major depressive disorder (MDD)*. Based on pharmacology and medicinal chemistry experiments, scientists at Tonix have established that tianeptine is an agonist for the nuclear peroxisome proliferator-activated receptor (PPAR) isoforms PPAR-β/δ and PPAR-γ, and tianeptine’s effects on these PPAR isoforms account for its ability to induce neuroplasticity in cultured neurons. The findings upset a long-held belief that the only way to restore the connectivity of neurons damaged in the state of depression was to increase the synaptic levels or activity of neurotransmitters such as the monoamines serotonin, norepinephrine, and dopamine. The new findings show that selective activation of nuclear PPAR-β/δ and PPAR-γ in neurons and supporting glia appears to be a more direct mechanism to achieve the goal of restoring neuronal connectivity, which is called neuroplasticity. Drugs that restore neuroplasticity are called plastogens.1-3 Consequently, tianeptine is a plastogen that acts directly on nuclear receptors that regulate gene expression in neurons and microglia. “The discovery that tianeptine stimulates neuroplasticity by activating certain PPAR isoforms could lead to a paradigm shift in designing new antidepressants, and change the relative reliance developers place on targeting synaptic neurotransmitter levels and activity,” said Stephen Stahl, M.D., Ph.D., Adjunct Professor of Psychiatry at the University of California San Diego, Chairman of Neuroscience Education Institute, author of the bestselling clinical manual, Essential Psychopharmacology Prescriber’s Guide, and consultant to Tonix. “Thi...