Zelnorm (tegaserod) / Novartis - LARVOL DELTA

The Safety of Pharmacotherapy for Irritable Bowel Syndrome: A Systematic Review and Meta-Analysis. (PubMed, Am J Gastroenterol) - "Among pharmacotherapies for IBS, tricyclics (especially at elevated doses), tenapanor, and alosetron have the highest absolute risk of discontinuation due to an AE when compared to rifaximin, the safest pharmacotherapy studied."

Journal • Retrospective data • Gastrointestinal Disorder

Assessing the association between drug use and ischaemic colitis: a retrospective pharmacovigilance study using FDA Adverse Event data. (PubMed, BMJ Open) - "This study identified key drugs associated with ischaemic colitis, particularly alosetron, tegaserod, osmoprep, naratriptan and kayexalate. Notably, two-thirds of these drugs lacked ischaemic colitis warnings in their package inserts. These findings underscore the need for greater clinical vigilance, improved regulatory oversight and further research to clarify underlying mechanisms and support safer medication use."

Adverse events • Journal • Retrospective data • Gastroenterology • Gastrointestinal Disorder • Immunology

EVALUATING THE SAFETY OF PHARMACOTHERAPY FOR IRRITABLE BOWEL SYNDROME: A META-ANALYSIS (DDW 2025) - "AEs were more varied for tricyclics (indicated for IBS global symptoms); for example, compared to placebo the three most common AEs with associated risk increases were drowsiness (14%), dry mouth (12%), and weight gain (9%) for amitriptyline, dry mouth (22%), flushing (18%), and constipation (17%) for desipramine, and fatigue (15%), dry mouth (3%) and blurry vision (1.5%) for doxepin...The NNH for linaclotide, lubiprostone, plecanatide, tegaserod, and tenapanor (indicated for IBS-C) was 27 (p < 0.01), 53 (p = 0.59), 58 (p < 0.01), 59 (p = 0.03), and 17 (p <0.01) respectively. The NNH for alosetron and eluxadoline (indicated for IBS-D) was 16 (p < 0.01) and 32 (p < 0.01). Ramosetron and rifaximin (indicated for IBS-D) had a negative risk difference, with the rate of withdrawal due to AEs higher in the placebo arm, so NNH was a negative, although statistically insignificant, value... Tricyclics, alosetron, and tenapanor are associated with a higher..."

Retrospective data • Constipation • Fatigue • Gastrointestinal Disorder • Xerostomia

IBS-C PATIENT EXPERIENCES WITH PHARMACOLOGIC THERAPIES: QUALITATIVE ANALYSIS OF ONLINE POSTS FROM (TWITTER) AND E-HEALTH FORUMS (DDW 2025) - "To find relevant posts from IBS-specific subforums, we applied filters targeting FDA-approved IBS-C medications (linaclotide, lubiprostone, plecanatide, tegaserod, tenapanor). Discussions : Our study highlights the diverse real-world experiences of IBS-C patients with FDA-approved therapies, revealing variability in both efficacy and the biopsychosocial impacts associated with each medication. These findings highlight the importance of shared decision making in selecting an IBS-C treatment, including evaluating the need to switch medications or classes, as well as addressing barriers such as cost and side effects to improve adherence and patient outcomes."

Clinical • CNS Disorders • Constipation • Gastrointestinal Disorder • Mood Disorders • Psychiatry

Binding assays enable discovery of Tet(X) inhibitors that combat tetracycline destructase resistance. (PubMed, Chem Sci) - "We report the development of an efficient fluorescence polarisation Tet(X) binding assay employing a tetramethylrhodamine-glycyl-minocycline conjugate that enables inhibitor discovery...Screening of a bioactive molecule library identified novel Tet(X) inhibitors, including psychoactive phenothiazine derivatives and the 5-HT4 agonist tegaserod, the activities of which were validated by turnover assays...In some cases, potentiation of tigecycline activity was observed in bacteria expressing Tet(X4). The combined results provide non-tetracycline scaffolds for development of potent Tet(X) inhibitors and highlight the need to evaluate the impact of non-antibiotics on antimicrobial resistance."

Journal

Pharmacologic Treatment of Irritable Bowel Syndrome with Predominant Constipation (PubMed, Korean J Gastroenterol) - "Guanylate cyclase-C agonists (linaclotide and plecanatide) enhance intestinal fluid secretion and motility, normalize bowel movements, and reduce abdominal pain. Na+/H+ exchanger inhibitors (e.g., tenapanor) decrease sodium absorption, increase fluid secretion, and alleviate visceral pain. Lubiprostone activates the chloride channels to facilitate bowel movements, while polyethylene glycol laxatives regulate osmotic pressure to improve stool consistency and ease defecation. Highly selective 5-HT4 agonists, such as prucalopride, accelerate gastrointestinal and colonic transit and improve stool frequency and consistency without increasing the cardiovascular risks raised in earlier agents such as tegaserod...These pharmacology agents have shown efficacy and safety in clinical studies, but drug availability, adverse effects, and variable patient responses are still challenging. Effective strategies to manage IBS-C require a personalized approach, considering the..."

Journal • Review • Cardiovascular • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology • Pain

Tegaserod maleate exerts anti-tumor effects on prostate cancer via repressing sonic hedgehog signaling pathway. (PubMed, Mol Med) - "Mechanistically, TM exerted anti-tumor effects via downregulating GLI2, and its downtream targets, thus inhibiting the sonic hedgehog (SHH) signaling pathway. In brief, our findings demonstrated that TM effectively inhibited the activities of PCa cells by suppressing the SHH signaling pathway and provided a potential new agent for the treatment of PCa."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • GLI2

Single-Center Experience with Concomitant Use of Novel and Off-Label Prescriptions for Chronic Constipation (ACG 2024) - "Charts were reviewed for prescriptions of at least 1 of 8 pharmacotherapies: linaclotide, lubiprostone , plecanatide , prucalopride, tenapanor , tegaserod, pyridostigmine, and colchicine. 405 patients were evaluated for chronic constipation, of which 138 (34%) received one or more prescription-based therapies. The most common diagnoses supporting these prescriptions are listed in Table 1. 110 patients (79.7%) were prescribed monotherapy, 23 (16.67%) given dual therapy simultaneously, 4 (2.8%) given three agents simultaneously, and only 1 (0.7%) given four agents simultaneously."

Clinical • Constipation • Gastroenterology • Gastrointestinal Disorder

Tegaserod Stimulates 5-HT4 Serotonin Receptors in the Isolated Human Atrium. (PubMed, Int J Mol Sci) - "Tegaserod shifted the concentration-response curve of the force of contraction to serotonin to the right in HAPs, indicating that it is a partial agonist at 5-HT4 serotonin receptors in this model. We propose that the mechanism of action of tegaserod in HAPs involves cAMP-dependent phosphorylation of cardiac regulatory proteins."

Journal • Gastrointestinal Disorder • Inflammatory Bowel Disease

Integrated transcriptomics- and structure-based drug repositioning identifies drugs with proteasome inhibitor properties. (PubMed, Sci Rep) - "Here, we used an integrated drug repositioning approach based on transcriptomics data and structure-based virtual screening to identify compounds with gene signatures similar to three known proteasome inhibitors (PIs; bortezomib, MG-132, and MLN-2238)...Using this approach, we identified six compounds with PI properties ((-)-kinetin-riboside, manumycin-A, puromycin dihydrochloride, resistomycin, tegaserod maleate, and thapsigargin)...As shown with bortezomib, only manumycin-A, puromycin dihydrochloride, and tegaserod maleate resulted in excessive accumulation of ubiquitinated proteins and elevated HMOX1 expression. Taken together, our integrated drug repositioning approach and subsequent in vitro validation studies identified six compounds demonstrating properties similar to proteasome inhibitors."

Journal • Breast Cancer • Melanoma • Oncology • Solid Tumor • Targeted Protein Degradation • HMOX1

Gut Dysbiosis and Alterations of Gastrointestinal Motility as Drivers of Opioid-Induced Hyperalgesia (IASP 2024) - " Male and female C57Bl6J mice were treated with escalating doses of morphine (10-40 mg/kg, i.p.) for 4 days...To assess the role of gut motility, drug-naïve mice were treated with tegaserod, a peripherally-restricted serotonin agonist that increases gut motility, to determine if increasing gut motility was sufficient to replicate opioid-induced dysbiosis and withdrawal symptoms... Opioid withdrawal produces profound and protracted changes in gut microbiota, motility, and permeability in mice, which correlated with the development and duration of withdrawal-induced inflammation and hyperalgesia. Chronic opioid treatment and withdrawal in germ-free mice, lacking a gut microbiome, does not produce spinal inflammation nor does it result in persistent hyperalgesia. Imitating the increase in gut motility during withdrawal via pharmacological means is sufficient to elicit pain and neuroinflammation, while limiting opioid actions to the central nervous system prevents these..."

Dysbiosis • CNS Disorders • Gastrointestinal Disorder • Immunology • Inflammation • Pain

Current and future pharmacotherapies for the management of constipation-predominant irritable bowel syndrome. (PubMed, Expert Opin Pharmacother) - "Therefore, new therapies are being developed to speed up bowel movement and reduce constipation, with drugs such as linaclotide, plecanatide, lubiprostone, or tegaserod available to reduce IBS-C symptoms. Current clinical trials of new therapeutic options are not too successful and it seems that one of the plausible treatment options could be the multi-drug cocktail with some, or perhaps even all its ingredients emerging from drug re-purposing. Another important path that needs to be explored further in IBS-C patients is the adjustment of dietary habits and/or introduction of dietary or nutritional intervention."

Journal • Review • Constipation • Gastroenterology • Gastrointestinal Disorder

RISK OF CONSTIPATION WITH ANTI-OBESITY MEDICATION AND CURRENT PRESCRIBING PATTERN LANDSCAPE IN MANAGING THE SIDE EFFECT (DDW 2024) - "We then determined whether these patients were prescribed a medication for constipation (plecanatide linaclotide tegaserod lubiprostone polyethylene glycol (PEG) magnesium oxide lactulose bisacodyl senna sodium picosulfate tenapanor prucalopride)...8% (7/145) diethylpropion...Liraglutide and phentermine-topiramate had the highest constipation rates. Black patients had higher rate of new constipation diagnosis and treatment compared to White patients. Semaglutide had the least risk for requiring constipation medication."

Adverse events • Constipation • Diabetes • Gastroenterology • Gastrointestinal Disorder • Genetic Disorders • Obesity

IMPLICATIONS OF POPULAR TRENDING ANTI-OBESITY MEDICATIONS - AN INCREASE IN HEALTHCARE COST AND UTILIZATION FOR THE POPULATION WITH CONSTIPATION (DDW 2024) - "Inclusion criteria included obese patients started on an AOM (per the 0 AGA Guideline on the Pharmacological Interventions for Adults with Obesity - semaglutide liraglutide phentermine-topiramate phentermine naltrexone-bupropion diethylpropion) who subsequently developed constipation after one week to twelve months after starting the AOM...The search was then narrowed to patients who were prescribed a constipation medication: plecanatide linaclotide tegaserod lubiprostone polyethylene glycol (PEG) magnesium oxide lactulose bisacodyl senna sodium picosulfate tenapanor prucalopride...Patients on AOM who develop constipation appear to have a threefold increase in ED visits and inpatient admissions. The average annual cost of constipation medication alone is $5 485. 04 per person."

Clinical • HEOR • Constipation • Diabetes • Gastroenterology • Gastrointestinal Disorder • Genetic Disorders • Obesity

CLINICAL EFFICACY AND ELECTROGASTROGRAPHIC CHANGES OF TEGASEROD VS. DOMPERIDONE IN PATIENTS WITH FUNCTIONAL DYSPEPSIA WITH GASTRIC DYSRHYTHMIA (DDW 2024) - "Tegaserod showed a significant improvement both symptomatically and electrogastrographically compared to domperidone in patients with FD presenting with dysrhythmia on EGG. Further studies with a larger number of patients and longer treatment duration are needed to determine its clinical use."

Clinical • Cardiovascular • Celiac Disease • CNS Disorders • Dyspepsia • Immunology

Prevalence and Choice of Pharmacologic Management of Functional Dyspepsia and Irritable Bowel Syndrome During Pregnancy (ACG 2023) - "Pylori Antibiotics = Metronidazole, Clarithromycin, Levofloxacin, Tetracycline, Doxycycline, Tinidazole, Nitazoxanide, Rifabutin. Anti-Diarrheals = Loperamide, Diphenoxylate, Bismuth Salicylate. Bile Acid Sequestrants = Cholestyramine, Colesevelam, Colestipol. Bowel Stimulants = Bisacodyl, Sennosides. Exposure to IBS or FD medications was significantly elevated in IBSFD compared to NONE. 17,984 of 48,208 IBSFD patients (37%) were exposed to proton pump inhibitors compared to 266,835 of 3,046,065 (9%) of NONE (OR 6.20; 95% CI 6.08 - 6.52). 1.4% of IBSFD were exposed to Rifaximin compared to 0.032% of NONE (OR 44.44; CI 40.19 - 49.14)."

Dyspepsia • Gastrointestinal Disorder

Small Organic Compounds Mimicking the Effector Domain of Myristoylated Alanine-Rich C-Kinase Substrate Stimulate Female-Specific Neurite Outgrowth. (PubMed, Int J Mol Sci) - "We found that epigallocatechin, amiodarone, sertraline, tegaserod, and nonyloxytryptamine bind to a monoclonal antibody against the ED peptide, and compounds stimulate neurite outgrowth in cultured cerebellar granule cells of female mice only. Therefore, a search for compounds that act in males appears warranted."

Journal • CNS Disorders • Orthopedics • MARCKS

The RNA m6A reader YTHDF1 is required for acute myeloid leukemia progression. (PubMed, Cancer Res) - "Moreover, tegaserod reduced the viability of patient-derived AML cells in vitro and prolonged survival in patient-derived xenograft models. Together, our study defines YTHDF1 as an integral regulator of AML progression by regulating the expression of m6A-modified mRNAs, which might serve as a potential therapeutic target for AML."

Journal • Acute Myelogenous Leukemia • Hematological Disorders • Hematological Malignancies • Leukemia • Oncology • YTHDF1

Lactobacillus rhamnosus GG supernatant promotes intestinal mucin production through regulating 5-HT4R and gut microbiota. (PubMed, Food Funct) - "Six-week-old C57BL/6J mice were randomized into 3 groups, and were treated with De-Man Rogosa and Sharpe broth (MRS group), tegaserod maleate (tegaserod group) and LGG supernatant (LGGs group) by gavage, respectively...Our results suggested that LGGs could upregulate 5-HT4R to promote MUC2 production, as well as modulate the gut microbiota, thus improving the defecation function in mice. This finding might provide evidence for the application of diet supplementary LGG in relieving gastrointestinal motility disorders."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Inflammatory Bowel Disease • Transplantation • MUC2

Tegaserod maleate exhibits antileukemic activity by targeting TRPM8. (PubMed, Biomed Pharmacother) - "Importantly, TRPM8 is overexpressed in AML patients, indicating that it is a new prognostic factor in AML. Collectively, our work demonstrates the anti-AML effects of tegaserod maleate via targeting TRPM8 and indicates that TRPM8 is a regulator of leukemogenesis with therapeutic potential in AML."

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

Tegaserod Maleate Suppresses the Growth of Gastric Cancer In Vivo and In Vitro by Targeting MEK1/2. (PubMed, Cancers (Basel)) - "We further compared the effect between tegaserod maleate and trametinib, which is a clinical MEK1/2 inhibitor, and confirmed that tegaserod maleate has the same effect as trametinib in inhibiting the growth of GC. Our findings suggest that tegaserod maleate inhibited GC proliferation by targeting MEK1/2."

Journal • Preclinical • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • MAP2K1

Hydrogen Bonding Penalty Used for Virtual Screening to Discover Potent Inhibitors for Papain-Like Cysteine Proteases of SARS-CoV-2. (PubMed, Chem Biol Drug Des) - "Finally, 61 compounds were acquired and 4 of them with IC at micromolar level tested in vitro enzyme activity assay, which include clinical drugs tegaserod...The binding modes of these 4 compounds were further explored with metadynamics simulations. The hits will provide a starting point for future key interactions identified and lead optimisation targetting PLpro."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

AGA Clinical Practice Guideline on the Pharmacological Management of Irritable Bowel Syndrome With Constipation. (PubMed, Gastroenterology) - "The panel agreed on 9 recommendations for the management of patients with IBS-C. The panel made a strong recommendation for linaclotide (high certainty) and conditional recommendations for tenapanor, plecanatide, tegaserod, and lubiprostone (moderate certainty), polyethylene glycol laxatives, tricyclic antidepressants, and antispasmodics (low certainty). The panel made a conditional recommendation against the use of selective serotonin reuptake inhibitors (low certainty)."

Clinical guideline • CNS Disorders • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology

Tenapanor (Ibsrela) for irritable bowel syndrome with constipation. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology

Real-World Treatment Strategies to Improve Outcomes in Patients With Chronic Idiopathic Constipation and Irritable Bowel Syndrome With Constipation. (PubMed, Am J Gastroenterol) - "When these options fail, prescription secretagogues (plecanatide, linaclotide, lubiprostone, and tenapanor [pending commercial availability]), or serotonergic agents (prucalopride and tegaserod) are generally preferred. Given the broad spectrum of available agents, therapy should be tailored by mutual decision-making between the patient and practitioner. Overall, patients need to be actively monitored and managed to maximize clinical outcomes."

HEOR • Journal • Real-world evidence • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology • Pain