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etrasimod (Velsipity)

Indications: - investigational treatment of atopic dermatitis - ulcerative colitis (FDA-approved) Contraindications: - myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or heart failure class III or IV - history of Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker. Dosage: - 2 mg PO QD Adverse effects: - may increase risk of infections - unintended additive immune system effects from prior treatment with immunosuppressives or immunomodulators - immune system effects after stopping etrasimod - bradyarrhythmia & atrioventricular conduction delays - hepatotoxicity: increase in serum transaminases - may increase risk of macular edema - hypertension - skin cancer - posterior reversible encephalopathy syndrome - may cause a decline in pulmonary function [3] Mechanism of action: - sphingosine 1-phosphate receptor 1 (S1PR1) modulator - activates S1PR subtypes S1PR1, S1PR4 & S1PR5 - with no detectable activity on S1PR2 or S1PR3 - prevents immune cells or lymphocytes from getting into skin

General

dermatologic agent receptor antagonist

Database Correlations

PUBCHEM cid=44623998

References

  1. Laub G Etrasimod Shows Promise for Atopic Dermatitis New safety and efficacy data highlight potential, Emma Guttman-Yassky explains. MedPage Today May 24, 2021 https://www.medpagetoday.com/meetingcoverage/aadvideopearls/92764
  2. Brooks M FDA Approves New Drug for Ulcerative Colitis. Medscape. Oct 13, 2023 https://www.medscape.com/viewarticle/997350 - Sandborn WJ et al Etrasimod as induction and maintenance therapy for ulcerative colitis (ELEVATE): two randomised, double-blind, placebo-controlled, phase 3 studies. Lancet. 2023;401(10383):P1159 April 8. PMID: 36871574 Free article https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(23)00061-2/fulltext
  3. HIGHLIGHTS OF PRESCRIBING INFORMATION Velsipity. tablets, for oral use https://labeling.pfizer.com/ShowLabeling.aspx?id=19776