tranylcypromine / Generic mfg. - LARVOL DELTA

Drug-associated hypertensive crisis: a disproportionality analysis of the FAERS database. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Ramipril (282 cases) and valsartan (192 cases) ranked as the second and third medications, respectively. The top 5 drugs associated with the risk of hypertensive crisis under the ROR algorithm were amlodipine perindopril (ROR = 136.64), methyl aminolevulinate (ROR = 122.78), tranylcypromine (ROR = 105.15), rifapentine (ROR = 39.46), and amiloride hydrochlorothiazide (ROR = 39.36)...Our study showed that numerous medications carry potential risks for drug-associated hypertensive crisis. Further investigation is required to establish causality and inform clinical decision-making."

Journal

NLRP3 inflammasome and hearing loss: from mechanisms to therapies. (PubMed, J Neuroinflammation) - "Experimental studies have demonstrated that pharmacological inhibition of NLRP3 via agents such as MCC950, oridonin and tranylcypromine can preserve auditory function...Clinically, IL-1B signaling blockers such as anakinra and canakinumab have shown efficacy in CAPS patients, stabilizing or improving hearing outcomes...Future translational research should focus on validating NLRP3-targeting compounds in human trials, identifying biomarkers for early diagnosis, and exploring combination therapies that integrate anti-inflammatory, antioxidant, and regenerative strategies. Targeting NLRP3 may ultimately redefine treatment paradigms for preventing or halting progressive hearing loss."

Journal • Review • Inflammation • Otorhinolaryngology • Rare Diseases • IL18 • IL1B • NLRP3

Tranylcypromine-derived LSD1 inhibitors: Synthetic strategies, structure-activity relationships, and anticancer potential. (PubMed, Eur J Med Chem) - "Clinically evaluated candidates like TCP, ORY-1001, and INCB059872; administered alone or in combination; irreversibly inhibit LSD1 by binding its FAD cofactor. Collectively, these inhibitors demonstrate significant therapeutic promise. We further discuss challenges (e.g., selectivity, resistance), opportunities, and future directions for optimizing LSD1-targeted cancer therapies."

Journal • Review • Breast Cancer • Oncology • Solid Tumor

Quercetin and Tranylcypromine Improve Memory, Behavioral Performance, and Cholinergic Function in Male Rats Subjected to Chronic Restraint Stress. (PubMed, Brain Sci) - "Overall, quercetin and TCP proved to reverse CRS-induced alterations in these parameters. Quercetin mitigated cognitive deficits, behavioral impairments, and neurochemical alterations induced by the CRS model, especially in association with TCP, supporting its potential as a promising therapeutic agent for depression."

Journal • Preclinical • CNS Disorders • Cognitive Disorders • Depression • Major Depressive Disorder • Mood Disorders • Pain • Psychiatry

MAO inhibitors for treatment-resistant depression: bringing an updated perspective on pioneering drugs. (PubMed, Pharmacol Res) - "These now have well-recognized mechanisms of action, making them much less common and potentially preventable. It is important to study and teach the pharmacology of monoamine oxidase inhibitors again in order to revive their use in severely depressed patients, as well as in those who have experienced multiple treatment failures."

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

Tangeretin protects the kidney from ischemia-reperfusion injury by inhibiting inflammatory response through downregulation of MAOA. (PubMed, Int Immunopharmacol) - "Tangeretin attenuates RIRI-induced renal injury by inhibiting the MAOA/NF-κB pathway and exerting anti-inflammatory and anti-apoptotic effects. These findings highlight its potential as a promising therapeutic candidate for ischemia-associated AKI."

Journal • Acute Kidney Injury • Cardiovascular • Inflammation • Nephrology • Renal Disease • Reperfusion Injury

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

Unravelling the target landscape of tranylcypromines for new drug discovery. (PubMed, Acta Pharm Sin B) - "Tranylcypromine (TCP) is a widely acknowledged scaffold with diverse pharmacological activities...Notably, the first reversible oral P2Y12 receptor antagonist, ticagrelor, is currently used to prevent future myocardial infarction, stroke, and cardiovascular death...This review aims to explore the target landscape of TCPs, highlight key structure-activity relationships (SARs), and emphasize the therapeutic potential of TCPs for treating various diseases. Finally, the lessons learned from our medicinal chemistry practice, challenges and future directions of TCP-based drug discovery are briefly discussed."

Journal • Review • Acute Coronary Syndrome • Cardiovascular • Human Immunodeficiency Virus • Infectious Disease • Myocardial Infarction • Oncology

Tranylcypromine-Based LSD1 Inhibitors as Useful Agents to Reduce Viability of Schistosoma mansoni. (PubMed, ACS Infect Dis) - "Schistosoma infections remain a major public health issue mainly in tropical and subtropical regions. While Praziquantel is the primary treatment for schistosomiasis, its limitations include resistance development and poor efficacy against juvenile worms. Given the biological similarities between tumor and parasite-infected cells, LSD1 inhibitors─primarily explored as anticancer agents─have been investigated for their antiparasitic potential."

Journal • Infectious Disease • Oncology

Triflupromazine and tranylcypromine alleviate primary cisplatin resistance in lung adenocarcinoma by promoting LDHA-mediated AMBRA1 ubiquitination. (PubMed, Biochem Pharmacol) - "Importantly, we identified two LDHA inhibitors, triflupromazine (TRI) and tranylcypromine (TRA), that significantly improve cisplatin efficacy both in vitro and in vivo. These findings highlight a critical role of LDHA in promoting cisplatin resistance, and suggest that targeting LDHA may represent a promising therapeutic strategy for patients with advanced LUAD."

IO biomarker • Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • AMBRA1 • BCL2 • CCND1 • LDHA

Sensitization of Non-M3 Acute Myeloid Leukemia Blasts to All-Trans Retinoic Acid by the LSD1 Inhibitor Tranylcypromine: TRANSATRA Phase I Study. (PubMed, Eur J Haematol) - "As histone demethylase LSD1 (KDM1A) is a rational therapeutic target in AML, we conducted a phase I trial ("rolling-six design") with the LSD1 inhibitor tranylcypromine (TCP, dose levels [DL] 20, 40, 60, 80 mg p.o. d1-28) combined with fixed-dose ATRA (45 mg/m2 p.o. d10-28) and low-dose cytarabine (LDAC, 40 mg s.c. Trial Registration: German Clinical Trials Register (DRKS): DRKS00006055. For further Information see https://drks.de/search/en/trial/DRKS00006055."

Journal • P1 data • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Myelodysplastic Syndrome • Oncology

Consistent differential effects of bupropion and mirtazapine in major depression. (PubMed, J Affect Disord) - "Bupropion is most effective for hypersomnia, increased weight, increased appetite, or fatigue, while mirtazapine is preferable for insomnia, decreased weight, or decreased appetite. SV enables statistically rigorous, symptom-level differentiation using only treatment assignment, offering a scalable and clinically aligned framework for guiding antidepressant selection from individual clinical trials."

Journal • CNS Disorders • Depression • Fatigue • Insomnia • Major Depressive Disorder • Mood Disorders • Psychiatry • Sleep Disorder

The Combination of Two Small Molecules Improves Neurological Parameters and Extends the Lifespan of C3H Strain Female Mice. (PubMed, Brain Behav) - "Chemical cocktails like RepSox and tranylcypromine (TCP) may induce beneficial age-related changes without the risks of full reprogramming...Histological findings revealed localized adaptive changes rather than major toxic effects. These results suggest that the combination of RepSox and TCP exerts protective effects on aging phenotypes and may potentially slow systemic aging processes in C3H mice."

Journal • Preclinical • Osteoporosis • Rheumatology

Atypical Antipsychotics in Mood and Other Disorders: Are We Too Quick on the Draw? - A Panel Discussion (APA 2025) - "Following the 1989 advent of SGAs when clozapine was launched, these medications began their triumphant march across the pages of the DSM: prescribed on-label for Schizophrenia, Schizoaffective Disorder, Bipolar Disorder, Major Depression augmentation, irritability associated with Autism Spectrum Disorder, suicidal risk reduction; off-label for PTSD, sleep disorders, ADHD, Tourettes Disorder, OCD, panic disorder, eating disorders, and both on label and off label - depending on which SGA - agitation associated with Alzheimer's.`...In the 1960s and 70s there were several formulations which combined first generation antipsychotics with antidepressants in a single pill (e.g., amitriptyline+perphenazine, tranylcypromine+trifluoperazine.) Although these combinations are still available, they seemed to fall out of favor in the 1980s, perhaps as a result of increasing attention to the challenge of tardive dyskinesia and the increasing faith in newer antidepressants. (We..."

ADHD (Impulsive Aggression) • Alzheimer's Disease • Attention Deficit Hyperactivity Disorder • Autism Spectrum Disorder • Bipolar Disorder • CNS Disorders • Depression • Genetic Disorders • Major Depressive Disorder • Mood Disorders • Movement Disorders • Post-traumatic Stress Disorder • Psychiatry • Schizophrenia • Sleep Disorder • Tourette Syndrome

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

Exploring the Addictive Potential of Tranylcypromine: A Case Report. (PubMed, J Clin Psychopharmacol) - No abstract available

Journal

Forced intracellular degradation of xenoantigens as a modality for cell-based cancer immunotherapy. (PubMed, iScience) - "Where MSC-UBvR-OVA vaccination successfully controlled tumor growth in cancer-bearing mice, the effect is further enhanced using tranylcypromine-stimulated MSCs and anti-PD-1 combination. Such anti-tumoral response relies on efferocytosis by endogenous phagocytes. Altogether, UBvR facilitated forced antigen degradation represents a plausible modality for future development of tumor antigen-expressing MSC-based vaccine."

IO biomarker • Journal • Hematological Malignancies • Lymphoma • Oncology • T Cell Non-Hodgkin Lymphoma

Dynamics of Cell Fate Decisions during Chemically Induced Multi-Lineage Trans-Differentiation at Single-Cell Level. (PubMed, Adv Sci (Weinh)) - "The time-course trajectory is demonstrated for trans-differentiation of mouse embryonic fibroblasts (MEFs) into multiple cell lineages including epithelial, neural, extraembryonic endoderm like (XEN-like) cells, and endothelial cells, when induced by SMs cocktail 6TCF (E616452, tranylcypromine, CHIR99021, and forskolin)...This study combines high-resolution landscape with comparative analyses of trans-differentiation dynamics, providing new insights into the complex mechanisms driving cell fate determination in vitro. Future study shall explore the applicability of the model in human cell trans-differentiation."

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Discovery of novel tranylcypromine-indazole-based derivatives as LSD1 inhibitors for acute myeloid leukemia treatment. (PubMed, Eur J Med Chem) - "In addition, compound 9e was found to induce apoptosis and upregulate of CD86-expression in MV-4-11 cells. All these findings indicated that compound 9e, a tranylcypromine-indazole derivative, provided a structural basis for LSD1 inhibitors in the treatment of acute myeloid leukemia."

Journal • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • CD86

An Exploration of the Interplay Between Caffeine and Antidepressants Through the Lens of Pharmacokinetics and Pharmacodynamics. (PubMed, Eur J Drug Metab Pharmacokinet) - "The interaction between fluvoxamine and caffeine resulted in increased concentrations of caffeine in the body and lowered the renal clearance of fluvoxamine. Other SSRIs such as fluoxetine and escitalopram had augmented antidepressant effects by decreasing their renal clearance and prolonging their effects in the body when coadministered with caffeine. Caffeine may also increase the concentration of paroxetine, potentially affecting its pharmacodynamic effects. TCAs such as clomipramine, imipramine, desipramine, and sertraline, were found to reduce the metabolism of caffeine...The inhibition of caffeine at high doses when used with MAOIs such as tranylcypromine and phenelzine was found to lead to a higher likelihood of experiencing hypertension. Coadministration of caffeine with venlafaxine (SNRIs) suggests minimal interactions between the two substances and the pharmacodynamic effects of venlafaxine were unlikely to be impacted by caffeine consumption. Miscellaneous..."

Journal • PK/PD data • Review • Cardiovascular • CNS Disorders • Hypertension • Psychiatry

Histone lysine demethylase 1A inhibitors, seclidemstat and tranylcypromine, induce astrocytogenesis in rat neural stem cells. (PubMed, Biochem Biophys Res Commun) - "Therefore, we show that the KDM1A inhibitors, SP-2577 and TCP, induce astrocytogenesis in rat NSCs. These findings suggest that KDM1A is a target for regulating NSCs fate and provide insights into the molecular mechanisms underlying neurodevelopmental processes and epigenetics."

Journal • Preclinical • CNS Disorders • Hematological Malignancies • Leukemia • Oncology • FAP • FGF2 • GFAP • IL6 • KDM1A • LIF • STAT3 • TUBB3

Development of BACE2-IN-1/tranylcypromine-based compounds to induce steroidogenesis-dependent neuroprotection. (PubMed, Biomed Pharmacother) - "Taken together, the outcomes of this study validate the favorable effects of inhibiting LSD1 and beta-secretase in mitigating mitochondrial stress and promoting neurometabolic recovery in TBI. These findings pave the way for the development of rationally designed inhibitors as promising neuroprotective agents, potentially addressing unmet clinical needs in TBI treatment."

Journal • CNS Disorders • Vascular Neurology

BMB-101 and Biased 5-HT2C Agonism: A Novel Approach for Sustained Epilepsy Management (AES 2024) - "BMB-101 is a novel 5-HT2C agonist developed by Bright Minds Biosciences Inc (USA) that belongs to a well-characterized class of tranylcypromine scaffold...BMB-101 shows a greater preference for Gq dissociation agonist activity versus β-arr1 and β-arr2 recruitment activity compared to Lorcaserin, thus demonstrating Gq-biased agonism. Based on the currently available data, BMB-101 is the only compound in clinical development (phase II anticipated Q4 2024) that has shown to be a "biased" or "functionally selective" 5-HT2C agonist, which means that it only targets one of the GPCR pathways... Based on the currently available data, BMB-101 is the only compound in clinical development (phase II anticipated Q4 2024) that has shown to be a "biased" or "functionally selective" 5-HT2C agonist, which means that it only targets one of the GPCR pathways. This is of utmost importance since βArr activation is associated with steric hindrance of..."

CNS Disorders • Epilepsy

An extended substrate spectrum of the proton organic cation antiporter and relation to other cation transporters. (PubMed, Basic Clin Pharmacol Toxicol) - "They included antidepressants (like tranylcypromine or nortriptyline), antipsychotics (like levomepromazine) and local anaesthetics. The substrate overlap between the H+/OC antiporter and OCTN1, OCTN2 or OCT3 was minimal, indicating that the latter three are not the proteins underlying the H+/OC antiporter activity. Overall, about 50% of positively charged drugs may be substrates of the antiporter, which may be the most important membrane transport protein for many drugs."

Journal • Anesthesia • CNS Disorders

Functional efficacy of the MAO-B inhibitor safinamide in murine substantia nigra pars compacta dopaminergic neurons in vitro: A comparative study with tranylcypromine. (PubMed, Parkinsonism Relat Disord) - "In patch-clamp recordings, we found that SAF (30 μM) significantly reduced the number of spikes evoked by depolarizing currents in SNpc DAergic neurons, in a sulpiride (1 μM) independent manner. According to our results, SAF marginally potentiates the DA signal in SNpc DAergic neurons, while exerting an inhibitory effect on the postsynaptic excitability acting on membrane conductances. Thus, we propose that the therapeutic effects of SAF in PD patients partially depends on MAO inhibition, while other MAO-independent sites of action could be more relevant."

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