Sediel (tandospirone) / Sumitomo Pharma, Pfizer - LARVOL DELTA

Severe bradycardia triggered by repetitive transcranial magnetic stimulation in a patient with major depressive disorder and premature ventricular contractions: a case report. (PubMed, BMC Psychiatry) - "The influence of rTMS on heart rate (HR) is likely mediated through the autonomic nervous system (ANS). Currently, severe arrhythmias are not widely recognized as adverse effects of rTMS. While the exact mechanisms by which rTMS affects the cardiovascular system remain unclear, this case underscores the necessity for caution when using rTMS to treat psychiatric patients with arrhythmias."

Journal • Cardiovascular • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry

A Real-world Study on the Effectiveness and Safety of Tandospirone in Treating Patients with Anxiety. (ChiCTR) - P4 | N=2000 | Recruiting | Sponsor: Shanghai Tongji Hospital; Shanghai Tongji Hospital

New P4 trial • Mood Disorders • Psychiatry

Deep eutectic solvent combined with permeation enhancer strategy to convert tandospirone from oral to transdermal formulations improving drug bioavailability. (PubMed, Eur J Pharm Biopharm) - "The results of the mechanistic study showed that levulinic acid(LeA) acted as a bridge to increase the interaction between the Tan and the matrix and inhibited the crystallization of the drug in the patch, and THEDES together with CPE improved the matrix fluidity and skin permeability. This study provides a reference for the joint application of THEDES and CPEs in patch development."

Journal • Mood Disorders • Psychiatry

Autism spectrum disorder-like behaviors induced by hyper-glutamatergic NMDA receptor signaling through hypo-serotonergic 5-HT1A receptor signaling in the prefrontal cortex in mice exposed to prenatal valproic acid. (PubMed, Neuropsychopharmacology) - "Treatment with a low-affinity NMDA receptor antagonist (memantine), a selective 5-HT reuptake inhibitor (fluoxetine), and a 5-HT1A receptor agonist (tandospirone) attenuated both the increase in CaMKII phosphorylation and ASD-like behavior of prenatal VPA mice. WAY-100635-a 5-HT1A receptor antagonist-antagonized the effect of fluoxetine on impaired social behavior and object recognition memory. These results suggest that E/I imbalance and ASD-like behavior are associated with hypo-serotonergic receptor signaling through 5-HT1A receptors in prenatal VPA mice."

Journal • Preclinical • Alzheimer's Disease • Autism Spectrum Disorder • CNS Disorders • Cognitive Disorders • Developmental Disorders • Genetic Disorders • Psychiatry

Ameliorating effect of chotosan and its active component, Uncaria hook, on lipopolysaccharide-induced anxiety-like behavior in mice. (PubMed, Front Pharmacol) - "Furthermore, treatment with tandospirone, a 5-HT1A receptor agonist, alleviated anxiety-like behavior in mice, whereas treatment with DOI, a 5-HT2A receptor agonist, enhanced anxiety-like behavior in mice...These findings indicate that chotosan exerts anxiolytic-like effects in the context of inflammation-induced anxiety, potentially mediated by the inhibition of 5-HT2A receptor hyperfunction in LPS-treated mice. Consequently, we postulate that chotosan may be effective in managing inflammation-induced anxiety-like behaviors."

Journal • Preclinical • Inflammation • Mood Disorders • Psychiatry

Unexplained recurrent high fever observed in a depressed adolescent. (PubMed, BMC Psychiatry) - "Depression should be considered a potential cause of unexplained recurrent fevers in adolescents, even when the temperature is significantly outside the normal range."

Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry

Efficacy and safety of venlafaxine hydrochloride combined with tandospirone citrate for patients with vascular depression accompanied by somatic symptoms: An open-labeled randomized control trial. (PubMed, CNS Neurosci Ther) - "The combined therapy rapidly acts on VaDep comorbid with anxiety and somatic symptoms and significantly alleviates the anxiety and somatic symptoms. The plasma levels of 5-HT may serve as potential objective candidates in evaluating VaDep severity and the efficacy of the undertaken treatment regimen."

Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry

Neonatal hypoxia impairs serotonin release and cognitive functions in adult mice. (PubMed, Neurobiol Dis) - "Finally, chronic treatment of adult MPA mice with fluoxetine, an inhibitor of 5-HT reuptake transporter, or the 5-HT1A receptor agonist tandospirone rescues cognitive flexibility and memory impairments. All together, these data demonstrate that the development of 5-HT system function is vulnerable to moderate perinatal asphyxia. 5-HT hypofunction might in turn contribute to long-term cognitive impairment in adulthood, indicating a potential target for pharmacological therapies."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Developmental Disorders • Epilepsy

Pharmacokinetics and absorption mechanism of tandospirone citrate. (PubMed, Front Pharmacol) - "The low absolute bioavailability of TDS may be attributed to its rapid metabolism. The pharmacokinetic data and absorption characteristics obtained in this study provide fundamental information for the further development and utilization of TDS."

Journal • PK/PD data • CNS Disorders • General Anxiety Disorder • Mood Disorders • Psychiatry

Comparison of tandospirone and escitalopram as a symptomatic treatment in Multiple System Atrophy-cerebellar ataxia: An open-label, non-controlled, 4 weeks observational study. (PubMed, J Psychiatr Res) - "Tandospirone citrate was more effective in improving depression/anxiety and some cerebellar ataxia symptoms, whereas escitalopram was more effective in improving some autonomic symptoms in MSA-C patients over a short-term period in an open-label observational study without a control group. Further research is needed to evaluate the long-term effects of tandospirone and escitalopram in MSA-C in long-term placebo controlled trials."

Journal • Observational data • Ataxia • CNS Disorders • Depression • Dermatology • Mood Disorders • Movement Disorders • Multiple System Atrophy • Parkinson's Disease • Psychiatry

Augmentation therapy with serotonin receptor partial agonists on neurocognitive function in schizophrenia: A systematic review and meta-analysis. (PubMed, Schizophr Res Cogn) - "5-HT partial agonists (buspirone or tandospirone) did not have a significant effect on verbal learning (SMD = 0.08, 95 % CI = -0.31 to 0.47) or working memory (SMD = 0.15, 95 % CI = -0.09 to 0.39)...The absence of any significant benefits in the cognitive domains studied here may have been due to the variance in the concomitant medication (typical vs atypical antipsychotic drugs), the level of cognition at baseline, or other factors. Further studies with various types of 5-HT agonists are warranted to examine the potential cognitive efficacy of stimulating these receptors."

Journal • Retrospective data • Review • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

The Serotonin 1A (5-HT) Receptor as a Pharmacological Target in Depression. (PubMed, CNS Drugs) - "Stimulation of the 5-HT receptor is an existing therapeutic target for treating depression and anxiety, using drugs such as buspirone and tandospirone...The development of 5-HT 'biased agonism', using compounds such as NLX-101, offers the opportunity to further elucidate the roles of pre- and post-synaptic 5-HT receptors. We describe how experimental medicine approaches can be helpful in profiling the effects of 5-HT receptor modulation on the different clinical domains of depression, and outline some potential neurocognitive models that could be used to test the effects of 5-HT biased agonists."

Journal • Review • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry

5 - HT1A Receptor Agonists in the Treatment of Psychopathology and Cognitive Impairment of Schizophrenia; An Avenue to Disease - Modifying Therapy (CINP 2023) - "It is of note that SEP-363856, a non-D2-receptor-binding drug that selectively acts on 5-HT1A receptors, in addition to trace amine-associated receptors, has been shown to ameliorate psychotic symptoms...Specifically, up-to-date information will be provided on the recent meta-analysis to confirm beneficial effects of augmentation with buspirone or tandospirone, azapirone derivatives usually prescribed as anxiolytics, on positive symptoms and attention/processing speed. The advantage of such add-on therapy raises the possibility that some marketed antipsychotic drugs, e.g., brexpiprazole and lurasidone, show part of their antipsychotic and cognition-enhancing efficacy via. actions on 5-HT1A receptors. These considerations will help refine the strategy to overcome unmet needs (e.g., cognitive impairment) in the treatment of psychotic disorders, and promote further endeavor to develop novel pharmacotherapy."

Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

Augmentation Therapy with 5 - HT1A Partial Agonists In Schizophrenia: A Meta - analysis (CINP 2023) - " Random-effects model meta-analyses revealed significant favorable effects on overall psychotic symptoms (SMD = -1.13, 95% CI = -1.98 to -0.27) and positive symptoms (SMD = -0.72, 95% CI = -1.31 to - 0.12) for add-on therapy with buspirone or tandospirone , while the effect on negative symptoms did not reach significance (SMD = -0.93, 95% CI = -1.90 to 0.04). These findings support the idea that some compounds that stimulate 5-HT1A receptors can provide an effective pharmacologic enhancer in the treatment of schizophrenia. Further clinical trials are warranted to determine the benefits of the adjunctive use of 5-HT1A partial agonists in ameliorating symptoms and improving functional outcomes in patients with schizophrenia."

CNS Disorders • Psychiatry • Schizophrenia

5-HT agonists for levodopa-induced dyskinesia in Parkinson's disease. (PubMed, Neurodegener Dis Manag) - "Clinical trials testing 5-HT agonists have yielded inconsistent results in alleviating dyskinesia, especially that the antidyskinetic benefit observed was often accompanied by an adverse effect on motor function. In this article, we summarize and analyze the various clinical trials performed with 5-HT agonists in PD patients with dyskinesia and offer perspectives on the future of this class of agents in PD."

Journal • Review • CNS Disorders • Movement Disorders • Parkinson's Disease

Early outcomes, associated factors and predictive values of clinical outcomes of tandospirone in generalized anxiety disorder: a post-hoc analysis of a randomized, controlled, multicenter clinical trial. (PubMed, Curr Med Res Opin) - P4 | "Patients with younger age at onset, milder anxiety symptoms and better physiological functions administered high-dose tandospirone showed rapid onset, great early outcomes, high recovery rate and good prognosis. Drug onset time had a good predictive effect on treatment outcome."

Clinical data • Journal • Retrospective data • CNS Disorders • General Anxiety Disorder • Mood Disorders • Psychiatry

Augmentation therapy with tandospirone citrate in vascular depression patients with mild cognitive impairment: A prospective randomized clinical trial. (PubMed, J Psychiatr Res) - "In this single-blind, randomized controlled study, 116 participants were randomly assigned to the tandospirone (tandospirone citrate-escitalopram) and control (escitalopram) groups. Additionally, plasma 5-HT levels may serve as a potential biomarker of VaDep severity. These findings may provide clinical insights into the treatment of vascular depression."

Clinical • Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Depression • Mood Disorders • Psychiatry

Effect of 5-HT1A receptor partial agonists of the azapirone class as an add-on therapy on psychopathology and cognition in schizophrenia: A systematic review and meta-analysis. (PubMed, Int J Neuropsychopharmacol) - "These findings support the idea that some compounds that stimulate 5-HT1A receptors might provide an effective pharmacologic enhancer in the treatment of schizophrenia. Further clinical trials are warranted to determine the benefits of the adjunctive use of 5-HT1A partial agonists in ameliorating symptoms and improving functional outcomes in patients with schizophrenia or other psychiatric disorders."

Journal • Retrospective data • Review • CNS Disorders • Cognitive Disorders • Mental Retardation • Psychiatry • Schizophrenia

5-HT Receptor Agonist Treatment Partially Ameliorates Rett Syndrome Phenotypes in mecp2-Null Mice by Rescuing Impairment of Neuron Transmission and the CREB/BDNF Signaling Pathway. (PubMed, Int J Mol Sci) - "Moreover, RNA-sequencing analysis found that tandospirone modulates the RTT phenotype, partially through the CREB1/BDNF signaling pathway in Mecp2-KO mice. These findings provide a new option for clinical treatment."

Journal • Preclinical • CNS Disorders • Developmental Disorders • Movement Disorders • Psychiatry • CLSPN, • CREB1

Clinical Efficacy of Tandospirone on Functional Dyspepsia Patients with Anxiety: A Randomized, Placebo-Controlled Study. (PubMed, Dig Dis Sci) - "Tandospirone effectively improved both anxiety and gastrointestinal symptoms of patients with FD, and these therapeutic effects may be associated with the modulation of BDNF and inflammatory cytokines."

Journal • CNS Disorders • Dyspepsia • Gastrointestinal Disorder • General Anxiety Disorder • Mood Disorders • Oncology • Psychiatry • BDNF • IL10 • IL1B • IL4 • IL6 • TNFA

Befiradol treatment ameliorated the motor dysfunction of Spinocerebellar Ataxia Type 3 mouse model (ECNP 2022) - "elegans) SCA3 model [4], using as reference drug tandospirone (TD), a partial 5-HT1AR agonist, previously described to have transient anti-ataxia effects in SCA3 patients [5]. Contrarily, TD exhibited no therapeutic effect on motor function. Post-symptomatically, befiradol-treated animals’ coordination was improved in the MST early on the disease (lower dose - p=0.053), while minor impact was observed in other motor parameters. Conclusion : Overall, befiradol showed a beneficial effect in SCA3 mice motor function, reinforcing the potential role of serotonergic signaling modulation as a promising therapeutic target for SCA3, though further experiments should be conducted to clarify the optimal doses and the route of administration to be utilized for this drug."

Preclinical • Ataxia • CNS Disorders • Parkinson's Disease • ATXN3

Befiradol treatment ameliorated the motor dysfunction of Spinocerebellar Ataxia Type 3 mouse model (ECNP 2022) - "elegans) SCA3 model [4], using as reference drug tandospirone (TD), a partial 5-HT1AR agonist, previously described to have transient anti-ataxia effects in SCA3 patients [5]. Contrarily, TD exhibited no therapeutic effect on motor function. Post-symptomatically, befiradol-treated animals’ coordination was improved in the MST early on the disease (lower dose - p=0.053), while minor impact was observed in other motor parameters. Conclusion : Overall, befiradol showed a beneficial effect in SCA3 mice motor function, reinforcing the potential role of serotonergic signaling modulation as a promising therapeutic target for SCA3, though further experiments should be conducted to clarify the optimal doses and the route of administration to be utilized for this drug."

Preclinical • Ataxia • CNS Disorders • Parkinson's Disease • ATXN3

Clinical Analysis on the Effects of Tandospirone Citrate Assisted by Drawing Therapy on Medication Compliance and Sleep Quality in Patients with Anxiety Disorders. (PubMed, Emerg Med Int) - "During treatment, there was no significant difference in the incidence of adverse reactions between the two groups (P > 0.05). DT-assisted tandospirone citrate can effectively improve the clinical symptoms of patients with anxiety disorders, improve medication compliance, sleep quality, and quality of life, and have a certain degree of safety."

Journal • CNS Disorders • Mood Disorders • Psychiatry

Tandospirone prevents stress-induced anxiety-like behavior and visceral hypersensitivity by suppressing theta oscillation enhancement via 5-HT receptors in the anterior cingulate cortex in rats. (PubMed, Front Cell Neurosci) - "Tandospirone reduced the enhancement of theta band power in ACC in vitro and in vivo, thus alleviating anxiety-like behavior and visceral hypersensitivity through 5-HT receptors in stressed rats. These results suggest a novel mechanism by which tandospirone activates 5-HT receptors to relieve stress-induced anxiety and visceral hypersensitivity by suppressing theta oscillation enhancement in ACC."

Journal • Preclinical • Gastrointestinal Disorder • Immunology • Mood Disorders • Psychiatry

Relative Safety and Efficacy of Two Doses of Tandospirone Citrate for Generalized Anxiety Disorder: A Multicenter Randomized Controlled Trial. (PubMed, Neuropsychiatr Dis Treat) - P4 | "The trial registration no. was NCT01614041."

Clinical • Cardiovascular • CNS Disorders • Depression • Gastrointestinal Disorder • General Anxiety Disorder • Mood Disorders • Psychiatry