Velsipity (etrasimod)

To treat moderately to severely active ulcerative colitis in adults Drug Trials Snapshot

FDA Approval: 10/12/2023

Research Synopsis

  • Velsipity, known generically as etrasimod, is an investigational oral medication currently being researched for the treatment of inflammatory bowel diseases (IBD), particularly ulcerative colitis.
  • Etrasimod selectively modulates sphingosine-1-phosphate (S1P) receptors, which play a key role in regulating lymphocyte trafficking, thus potentially reducing inflammation associated with these conditions.
  • Recent studies indicate that etrasimod shows promise in improving clinical scores and endoscopic findings in patients with ulcerative colitis compared to placebo, with most side effects reported as mild to moderate.
  • Long-term studies suggest that etrasimod maintains efficacy beyond initial treatment phases, with a favorable safety profile observed in extended trials.
  • Etrasimod's effectiveness in regulating lymphocyte movement positions it as a potential breakthrough in IBD treatment, especially for patients who have not responded well to existing therapies.
  • The drug has been shown to exhibit strong bactericidal properties against Gram-positive bacteria, indicating the potential for repurposing it as an antibacterial agent.
  • Ongoing phase 3 trials are expected to further clarify etrasimod's role and benefits in IBD, expanding the therapeutic landscape as new small molecules for treatment emerge.
  • Continuing research into S1P modulators like etrasimod reflects a shift away from traditional biologic therapies, with small molecule drugs offering easier administration routes and reduced immunogenicity risks.
  • Overall, sentiment around etrasimod is cautiously optimistic, bolstered by its promising clinical trial outcomes and adaptability in treating various immune-mediated disorders, including IBD and potential infectious diseases.

Related articles

Research articles about Velsipity (etrasimod)

Velsipity (etrasimod)

Modulation of sphingosine-1-phosphate in inflammatory bowel disease.

London, UK

2 hours ago

1 Received

  • Inflammatory bowel diseases (IBD), like ulcerative colitis and Crohn's disease, are caused by inappropriate immune responses in the digestive system, leading to severe symptoms and complications.
  • Monoclonal antibodies have transformed IBD treatment but come with high costs, risk of losing effectiveness, and potential for harmful immune reactions over time.
  • New Sphingosine-1-phosphate (S1P) receptor modulators, like ozanimod and etrasimod, show promise for IBD treatment in ongoing clinical trials, offering an oral alternative that may reduce the risk of anti-drug antibodies.

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Targeting Cytokine Signaling and Lymphocyte Traffic via Small Molecules in Inflammatory Bowel Disease: JAK Inhibitors and S1PR Agonists.

London, UK

2 hours ago

1 Received

  • Inflammatory Bowel Diseases (IBDs) are chronic conditions affecting the gastrointestinal tract, with treatments like biological therapies showing varied effectiveness due to their complexity and immunogenicity.
  • Recent advancements in understanding IBD mechanisms have led to new treatment options, particularly focusing on small molecules (SMs) which are easier to administer and less likely to provoke immune responses.
  • Janus Kinase (JAK) inhibitors and Sphingosine-1-Phosphate Receptor (S1PR) agonists are emerging as promising SM treatments for IBD, targeting specific pathways that contribute to the disease's pathology.

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The Selective Sphingosine 1-Phosphate Receptor Modulator Etrasimod Regulates Lymphocyte Trafficking and Alleviates Experimental Colitis.

London, UK

2 hours ago

1 Received

  • Lymphocyte movement from secondary lymphoid organs is influenced by the interaction between sphingosine 1-phosphate (S1P) and its receptor, which operates through concentration gradients.
  • Etrasimod, a new oral drug currently being tested, targets S1P receptors and is developed for treating immune-mediated inflammatory disorders like ulcerative colitis.
  • In studies, etrasimod acted effectively on various S1P receptors in different animals, showing a dose-dependent impact on lymphocyte levels and reducing inflammation in a mouse model of colitis.

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Interfering with leukocyte trafficking in Crohn's disease.

London, UK

2 hours ago

1 Received

  • The discovery of gut-specific leukocytes has revolutionized the treatment of inflammatory bowel disease by allowing for targeted therapies that modulate immune cell function.* -
  • New drugs like vedolizumab enable gut-specific immunosuppression and focus on targeting specific molecules involved in leukocyte trafficking to enhance treatment effectiveness.* -
  • Current and future therapies include oral and subcutaneous options, with ongoing discussions about safety, efficacy, and initial trial results guiding clinical practice.*

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Sphingosine-1-Phosphate Lyase Inhibition Alters the S1P Gradient and Ameliorates Crohn's-Like Ileitis by Suppressing Thymocyte Maturation.

London, UK

2 hours ago

1 Received

  • - The study explores the role of sphingosine-1-phosphate lyase (SPL) in the intestine, particularly its impact on S1P levels and lymphocyte behavior in both healthy and inflamed conditions like inflammatory bowel disease (IBD).
  • - Researchers conducted experiments using specific SPL inhibitors on mice with Crohn's-like chronic ileitis to observe changes in lymphocyte circulation, inflammation levels, and tissue S1P concentrations.
  • - Results showed that SPL is widely expressed in the gut, primarily in intestinal epithelial cells, and its inhibition significantly raised local S1P levels, suggesting a potential therapeutic avenue for managing gut inflammation without common side effects linked to S1P receptor targeting.

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Efficacy and Safety of Etrasimod in a Phase 2 Randomized Trial of Patients With Ulcerative Colitis.

London, UK

2 hours ago

1 Received

  • Etrasimod is an oral medication being tested for treating ulcerative colitis, a serious inflammatory bowel disease, in a phase 2 study.
  • The study involved 156 patients, who were given either 1 mg or 2 mg of etrasimod or a placebo for 12 weeks, measuring improvements in symptoms and endoscopic findings.
  • Results showed that the 2 mg dose of etrasimod significantly improved clinical scores and endoscopic outcomes compared to placebo, with most side effects being mild or moderate.

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Modulation of sphingosine-1-phosphate in ulcerative colitis.

London, UK

2 hours ago

1 Received

  • - Sphingosine-1-phosphate (S1P) is a crucial signaling molecule involved in various bodily functions and conditions, including immune response and potential cancer risks, by activating S1P receptors 1 through 5.
  • - Researchers are exploring S1P receptor agonists, like fingolimod and ozanimod, as new treatments for ulcerative colitis (UC) by preventing lymphocytes from leaving lymph nodes.
  • - Selective S1P modulators are being developed to improve the effectiveness and safety of S1P-based treatments, with ongoing Phase 3 trials expected to provide further evidence of their benefits for UC management.

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Small molecule drugs in the treatment of inflammatory bowel diseases: which one, when and why? - a systematic review.

London, UK

2 hours ago

1 Received

  • In the management of inflammatory bowel disease (IBD), small molecule drugs (SMDs) are emerging as effective alternatives to conventional biomolecular treatments, especially due to the rising failure rates of anti-tumor necrosis factor α agents.
  • This review assesses the role of various SMDs in treating Crohn's disease (CD) and ulcerative colitis (UC), highlighting the results of 15 clinical trials that demonstrate their efficacy and safety.
  • The findings suggest that while SMDs show promising safety and efficacy profiles, their clinical application will necessitate a personalized, mechanism-based approach for optimal treatment outcomes.

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PK, PD, and interactions: the new scenario with JAK inhibitors and S1P receptor modulators, two classes of small molecule drugs, in IBD.

London, UK

2 hours ago

1 Received

  • Inflammatory bowel diseases (IBDs) are chronic conditions affecting the gastrointestinal tract with unclear causes, and current treatments do not always ensure sustained remission for patients.
  • Small molecule drugs (SMDs) are emerging as a new treatment option for IBDs, showing promise in clinical trials and differing in pharmacodynamics and pharmacokinetics from traditional biologic agents.
  • These SMDs offer advantages like oral administration and fewer immune-related side effects, but they may also pose risks of drug-drug interactions due to their metabolic processing.

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P045 Effect of Etrasimod on Circulating Lymphocyte Subsets: Data From a Randomized Phase 1 Study in Healthy Japanese and Caucasian Men.

London, UK

2 hours ago

1 Received

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Sphingosine 1-phosphate Receptor Modulator Therapy for Multiple Sclerosis: Differential Downstream Receptor Signalling and Clinical Profile Effects.

London, UK

2 hours ago

1 Received

  • Lysophospholipids, especially sphingosine 1-phosphate (S1P), play a significant role in cell signaling through G protein-coupled receptors (GPCRs) and are important in various physiological and disease processes.
  • The S1P pathway has led to the approval of three medications for multiple sclerosis (MS)—fingolimod, siponimod, and ozanimod—while new modulators like ponesimod and etrasimod are in clinical development.
  • S1PR modulators vary in how they affect receptor activity, acting as both agonists and functional antagonists, influencing their clinical effectiveness, safety profiles, and pharmacokinetics, which is crucial for treating

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Targeting Sphingosine-1-Phosphate Signaling in Immune-Mediated Diseases: Beyond Multiple Sclerosis.

London, UK

2 hours ago

1 Received

  • Sphingosine-1-phosphate (S1P) is a lipid metabolite that interacts with 5 G-protein-coupled receptors to regulate lymphocyte trafficking, impacting immune responses and diseases.
  • An S1P gradient (low in tissues, high in blood) is crucial for lymphocyte movement; modulating this pathway can therapeutically affect conditions like multiple sclerosis and other immune-mediated diseases.
  • While some S1PR modulators show promise in treating autoimmune diseases and COVID-19, they come with potential side effects such as leukopenia and elevated transaminases, requiring careful administration.

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Long-term Safety and Efficacy of Etrasimod for Ulcerative Colitis: Results from the Open-label Extension of the OASIS Study.

London, UK

2 hours ago

1 Received

  • Etrasimod is a selective oral medication that showed significant effectiveness in treating moderately-to-severely active ulcerative colitis during a phase 2 clinical trial.
  • In the open-label extension study, 118 patients continued treatment with etrasimod for up to 52 weeks, with the majority completing the study and reporting mild to moderate adverse effects.
  • The results indicated that a large percentage of patients maintained clinical improvement, remission, or endoscopic improvement after the extended treatment period, demonstrating the medication's favorable safety profile.

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Targeting Chronic Inflammation of the Digestive System in Cancer Prevention: Modulators of the Bioactive Sphingolipid Sphingosine-1-Phosphate Pathway.

London, UK

2 hours ago

1 Received

  • Incidence of gastrointestinal (GI) cancers is rising, often diagnosed at later stages, making treatment challenging; chronic inflammation is a recognized risk factor.
  • The bioactive sphingolipid sphingosine-1-phosphate (S1P) is crucial for maintaining a balanced immune response in the GI tract, and disturbances in its signaling may contribute to chronic inflammatory disorders and GI cancers.
  • The text reviews S1P's role in GI cancers, highlighting current clinical trials for S1P receptor modulators like ozanimod and etrasimod, which show promise in treating inflammation and potentially reducing GI cancer risk long-term.

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Current options and investigational drugs for the treatment of eosinophilic esophagitis.

London, UK

2 hours ago

1 Received

  • * Established therapies include dietary modifications, proton pump inhibitors, and topical corticosteroids, with ongoing research into novel treatments like monoclonal antibodies and other targeted therapies aimed at reducing inflammation.
  • * Future strategies should focus on personalized care while considering cost-effectiveness, as many new therapies could address overlapping conditions related to EoE.

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Drug treatment strategies for eosinophilic esophagitis in adults.

London, UK

2 hours ago

1 Received

  • Eosinophilic esophagitis (EoE) is a disorder that leads to inflammation in the esophagus, causing symptoms related to esophageal dysfunction, with treatment focusing on symptom relief and improved quality of life through dietary changes, medications, and endoscopic procedures.
  • The text reviews current treatments for EoE in adults, emphasizing the role of proton pump inhibitors (PPIs) and swallowed topical corticosteroids (STCs), while also discussing new therapy developments like targeted STC formulations and monoclonal antibodies.
  • Emerging treatments using viscose STCs that coat the esophagus and investigational therapies targeting Th2 pathways may enhance effectiveness, and further studies

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Emerging therapies for ulcerative colitis.

London, UK

2 hours ago

1 Received

  • Despite improvements in treating ulcerative colitis (UC), some patients do not respond to existing therapies, leading to the development of new drug options.
  • The review highlights three key classes of drugs nearing approval: IL-23 antibodies, S1PR modulators, and JAK inhibitors, discussing how they work and their effectiveness and safety.
  • Although these drugs show promise, the need for reliable biomarkers for treatment selection and the lack of direct comparative trials remain challenges in effectively managing UC patients.

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Competitive Binding of Ozanimod and Other Sphingosine 1-Phosphate Receptor Modulators at Receptor Subtypes 1 and 5.

London, UK

2 hours ago

1 Received

  • * Research shows that ozanimod and several other S1P receptor modulators bind to the same sites on S1P receptors, indicating that they can compete for these binding sites.
  • * Since these modulators exhibit similar pharmacological properties and binding characteristics, they are considered interchangeable, allowing patients to switch between them based on individual treatment benefits without worrying about compounded effects.

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Repurposing the Sphingosine-1-Phosphate Receptor Modulator Etrasimod as an Antibacterial Agent Against Gram-Positive Bacteria.

London, UK

2 hours ago

1 Received

  • New antibiotics are urgently needed to combat drug-resistant bacteria, and drug repurposing may help speed up this process.
  • The study identified etrasimod, an existing investigational drug for ulcerative colitis, as an effective antibacterial agent, particularly against Gram-positive bacteria, including resistant strains.
  • Etrasimod not only exhibited strong bactericidal properties but also inhibited biofilm formation and showed potential for use in combination therapies without harming mammalian cells.

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