Marplan (isocarboxazid) / Validus - LARVOL DELTA

Modulating monoaminergic systems: A study on 3,5-dimethyl-1-phenyl-4-(phenylselenyl)-1H-pyrazole in lipopolysaccharide-induced depressive-like symptoms in mice. (PubMed, Eur J Pharmacol) - "In silico docking indicated high affinity of SePy for catalytic residues of both MAO isoforms, comparable to the reference inhibitor isocarboxazide...Taken together, the results suggest that SePy may exert antidepressant-like effects via monoaminergic modulation and displays a favorable hepatic safety profile. Additional studies are warranted to confirm its renal safety and further explore its pharmacological potential under inflammatory conditions."

Journal • Preclinical

Efficient photocatalytic synthesis of benzylhydrazine. (PubMed, Org Biomol Chem) - "At the same time, it was also proved that a wide range of phenylethanol analogues and azodicarboxylates can be successfully applied in this fragment coupling transformation. Moreover, this method can be applied to the synthesis of active molecules of isocarboxazid."

Journal

Rapid Monoamine Oxidase Inhibitor Switches in Treatment-Resistant Depression: Safety Evaluation in 3 Cases. (PubMed, J Psychiatr Pract) - "Case 1: A 25-year-old female on selegiline for 2 months was switched to phenelzine with only 1 medication-free day, then switched to tranylcypromine 2 weeks later with 1 medication-free day...Case 3: A 41-year-old female on isocarboxazid was switched to phenelzine with a 1-day washout period. The switch was well tolerated without any adverse events. These findings suggest MAOIs can be safely switched with a washout period of 2 days or less, although this should be reserved for specific clinical situations where the expected benefits outweigh the potential risks associated with any direct antidepressant switch."

Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry

Pharmacological treatments for atypical depression: A systematic review and network meta-analysis of randomized controlled trials. (PubMed, Eur Neuropsychopharmacol) - "Phenelzine might perform better than other compounds, but several drugs outperformed placebo in response. Nortriptyline performed worse than other treatments. High-quality studies are needed."

Journal • Retrospective data • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry • Sleep Disorder

SELECTIVE SEROTONIN REUPTAKE INHIBITORS AND TRICYCLIC ANTIDEPRESSANTS USE IN INFLAMMATORY BOWEL DISEASE PATIENTS MAY BE ASSOCIATED WITH POOR CLINICAL OUTCOMES (DDW 2025) - "Subjects were stratified into groups using commonly prescribed selective serotonin reuptake inhibitors (SSRI) (fluoxetine, citalopram, escitalopram, paroxetine, sertraline), tricyclic antidepressants (TCA) (amitriptyline, doxepin, imipramine, nortriptyline, desipramine), or monoamine oxidase inhibitors (MAOI) (selegiline, isocarboxazid, phenelzine, tranylcypromine) for at least one year. Herein we showed that SSRI and TCA use in IBD patients is associated with poor clinical outcomes in terms of requiring steroid therapy, hospitalization, and death. Some studies have suggested that this may be due to SSRI-induced dysbiosis which may lead to gut inflammation. MAOI use was not associated with statistically significant worsened outcomes however this may be due to insufficient power."

Clinical • Clinical data • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Pain • Psychiatry • Ulcerative Colitis

Antidepressant-Like Activity and Molecular Docking Analysis of a Sesquiterpene Lactone Isolated from the Root Bark of Ximenia americana (L.). (PubMed, Evid Based Complement Alternat Med) - "Dehydrocostus lactone (400 mg/kg) demonstrated a 46.50 s reduction in immobility time in the FST, which was comparable to the positive control, imipramine (30 mg/kg). With a highly favorable docking score of -8.365 kcal/mol on an antidepressant target, monoamine oxidase A (MAO-A; pdb ID: 2BXS), dehydrocostus lactone (1) potentially outperforms the standard MAO-A inhibitor drug, isocarboxazid (-5.847 kcal/mol)...These findings highlight that the antidepressant-like activity of X. americana is partly attributed to the presence of dehydrocostus lactone. Additionally, it also supports the traditional medicinal use of the plant for treating depression."

Journal • Review • CNS Disorders • Depression • Psychiatry

Efficacy and tolerability of monoamine oxidase inhibitors for the treatment of depressive episodes in mood disorders: A systematic review and network meta-analysis. (PubMed, Acta Psychiatr Scand) - "MAOIs are similar in efficacy to other antidepressants for the treatment of depression. However, more studies are needed comparing MAOI treatment in people with treatment-resistant, atypical and bipolar depression."

Journal • Retrospective data • Review • Bipolar Disorder • CNS Disorders • Depression • Mood Disorders • Psychiatry

Drugs for depressionr. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry

Classics in Chemical Neuroscience: Selegiline, Isocarboxazid, Phenelzine, and Tranylcypromine. (PubMed, ACS Chem Neurosci) - "It is therefore timely to review key aspects of the four "classic" MAOIs: high-dose selegiline, isocarboxazid, phenelzine, and tranylcypromine. This review discusses their chemical synthesis, metabolism, pharmacology, adverse effects, and the history and importance of these drugs within the broader field of chemical neuroscience."

Journal • Review • Alzheimer's Disease • CNS Disorders • Depression • Mood Disorders • Movement Disorders • Oncology • Parkinson's Disease • Psychiatry

Serotonin syndrome: A pharmacovigilance comparative study of drugs affecting serotonin levels. (PubMed, Eur J Clin Pharmacol) - "Prescribers need to be vigilant about drugs that can raise serotonin concentration or influence serotonergic neurotransmission, also when using drugs with less well-known risk for serotonin syndrome, like linezolid and triptans."

Adverse events • Journal

Final analysis of a phase II study of MRI based functional imaging of bone metastases in men with metastatic castrate-resistant prostate cancer (mCRPC) receiving Cabozantinib. (ASCO-GU 2019) - P2; "...The most common grades 3/4 toxicities were fatigue (24%) and palmarplantar erythrodysesthesia (12%)... Ktrans decreased significantly after 2 wks of treatment, consistent with antiangiogenic properties of C. Compared to wk 2, K trans at disease progression is unchanged, which could signify that adaptive vascular change is not the primary mechanism of tumor resistance to the drug. Contrary to our hypothesis, ADC increased during the trial, which perhaps correlates with the short median time to progression. Still, MRI of bone metastases could benefit drug development for other agents in mCRPC or interrogation of bone metastases, notoriously challenging for disease response analysis, in other cancers."

P2 data

Green Chemistry Approach for the Synthesis of Isoxazole Derivatives and Evaluation of Their Anti-epileptic Activity. (PubMed, Curr Drug Discov Technol) - "The use of microwave radiation enhances the rate of the reaction which leads to high selectivity with improved product yields in comparison with the traditional heating methods. The tested compounds exhibited promising antiepileptic activity as compared to the standard drug (Phenytoin)."

Journal • CNS Disorders • Epilepsy • Oncology

The prescriber's guide to classic MAO-inhibitors (phenelzine, tranylcypromine, isocarboxazid) for treatment-resistant depression. (PubMed, CNS Spectr) - No abstract available

Journal • Review • CNS Disorders • Depression • Mood Disorders • Psychiatry

The Prescriber's Guide to the MAOI Diet-Thinking Through Tyramine Troubles. (PubMed, Psychopharmacol Bull) - "This review article features comprehensive discussions on the dietary restrictions issued to patients taking a classic monoamine oxidase inhibitor (phenelzine, tranylcypromine, isocarboxazid), or high-dose (oral or transdermal) selegiline. Minimizing the intake of the small number of risky foods is all that is required. Many patients may hardly need to change their diet at all."

Journal • Review

"And yeah: Luvox has a bunch of contraindications, such as - alosetron, dihydroergotamine isocarboxazid, Lonafarnib, ramelteon, selegiline, citalopram - uk what? Lemme just post the link bc its a lot: https://t.co/miBZdmTVV6" (@Syfx18637973)

Treatment History Characteristics Associated With Use of Isocarboxazid: A Nationwide Register-Based Study. (PubMed, J Clin Psychopharmacol) - "Forty percent of those initiating isocarboxazid had received treatment with drugs from 5 or more different psychopharmacological classes in the 5 preceding years. These findings suggest that isocarboxazid is typically used for treatment-resistant depression, consistent with guideline recommendations."

Journal • CNS Disorders • Depression • Psychiatry

Neuronal Monoaminergic Antidepressant Response Signatures in the L1000 Database (ACNP 2021) - "To date, we have analyzed the following antidepressants within a given class: TCAs (9) – amitriptyline, amoxapine, clomipramine, desipramine, dibenzepin, doxepin (3 datasets), maprotiline, nortriptyline, and trimipramine; SSRIs (5) – escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline; serotonin norepinephrine reuptake inhibitors (SNRIs) (2) – duloxetine and venlafaxine; and monoamine oxidase inhibitors (MAOIs) (2) – bifemelane and isocarboxazid...Potential next steps include the identification of gene expression signatures of other antidepressant “perturbagens” in the L100, including those with different mechanisms, e.g. bupropion, a norepinephrine-dopamine reuptake inhibitor and nicotine receptor antagonist. Most of the gene expression profiles were non-overlapping across monoaminergic antidepressant classes. However, in the NPC line, HLA-DMA [major histocompatibility complex class II alpha chain, catalyzing the release of class II-associated invariant..."

IO biomarker • Alzheimer's Disease • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry • CD40 • EPHA3 • GJA1 • HLA-DRB1 • SSBP2 • TSPAN8

Neuronal Monoaminergic Antidepressant Response Signatures in the L1000 Database (ACNP 2021) - "To date, we have analyzed the following antidepressants within a given class: TCAs (9) – amitriptyline, amoxapine, clomipramine, desipramine, dibenzepin, doxepin (3 datasets), maprotiline, nortriptyline, and trimipramine; SSRIs (5) – escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline; serotonin norepinephrine reuptake inhibitors (SNRIs) (2) – duloxetine and venlafaxine; and monoamine oxidase inhibitors (MAOIs) (2) – bifemelane and isocarboxazid...Potential next steps include the identification of gene expression signatures of other antidepressant “perturbagens” in the L100, including those with different mechanisms, e.g. bupropion, a norepinephrine-dopamine reuptake inhibitor and nicotine receptor antagonist. Most of the gene expression profiles were non-overlapping across monoaminergic antidepressant classes. However, in the NPC line, HLA-DMA [major histocompatibility complex class II alpha chain, catalyzing the release of class II-associated invariant..."

IO biomarker • Alzheimer's Disease • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry • CD40 • EPHA3 • GJA1 • HLA-DRB1 • SSBP2 • TSPAN8

Final analysis of a phase II study of MRI based functional imaging of bone metastases in men with metastatic castrate-resistant prostate cancer (mCRPC) receiving Cabozantinib. (ASCO-GU 2019) - P2; "...The most common grades 3/4 toxicities were fatigue (24%) and palmarplantar erythrodysesthesia (12%)... Ktrans decreased significantly after 2 wks of treatment, consistent with antiangiogenic properties of C. Compared to wk 2, K trans at disease progression is unchanged, which could signify that adaptive vascular change is not the primary mechanism of tumor resistance to the drug. Contrary to our hypothesis, ADC increased during the trial, which perhaps correlates with the short median time to progression. Still, MRI of bone metastases could benefit drug development for other agents in mCRPC or interrogation of bone metastases, notoriously challenging for disease response analysis, in other cancers."

P2 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A review on post-traumatic stress disorder (PTSD): "Symptoms, Therapies and Recent Case Studies". (PubMed, Curr Mol Pharmacol) - "Various drugs which are used for the treatment of PTSD include selective serotonin reuptake inhibitors (SSRIs) (citalopram, fluvoxamine, fluoxetine, etc.); tricyclic antidepressants (amitriptyline and isocarboxazid); mood stabilizers (Divalproex and lamotrigine); atypical antipsychotics (aripiprazole and quetiapine), etc. In this review, we have covered the different risk factors, case studies related to various treatment options with different age group peoples in PTSD and their effects on them. We have also covered the symptoms and associated disorders which can play a key role in the development of PTSD."

Clinical • Journal • Review • CNS Disorders • Fatigue • Mental Retardation • Mood Disorders • Post-traumatic Stress Disorder • Psychiatry

Characterization of Novel Lytic Bacteriophages of Achromobacter marplantensis Isolated from a Pneumonia Patient. (PubMed, Viruses) - "The possibility exists for future testing of such bacteriophages in the control of Achromobacter infections such as those seen in CF and other infections of the lungs. The incidence of antibiotic resistance in this genus highlights the importance of seeking adjuncts and alternatives in CF and other lung infections."

Clinical • Journal • Cystic Fibrosis • Fibrosis • Genetic Disorders • Immunology • Infectious Disease • Pneumonia • Respiratory Diseases

Drugs for Depression. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • CNS Disorders • Depression • Mood Disorders

Despite calls to lower drug prices, more than 600 medications saw increases in January (BioSpace) - "...since the start of the year, prices have increased on more than 600 prescription drugs by an average of 5.2%...Among those is Humira...which saw a price hike of 7.4% this year...However, there were also a couple of outlier drugs that saw price increases above 10% this year, GoodRx said. The group pointed to the antidepressant Marplan, which saw a 14.9%..." "

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