Clinical data | |
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Trade names | Velsipity |
Other names | APD334, APD-334 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a623050 |
License data | |
Routes of administration | By mouth |
Drug class | Sphingosine-1-phosphate receptor modulator |
ATC code | |
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Pharmacokinetic data | |
Protein binding | 97.9% |
Metabolism | Liver (CYP2C8, 2C9, 3A4) |
Elimination half-life | 30 hours |
Excretion | Feces (82%), kidneys (5%) |
Identifiers | |
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Chemical and physical data | |
Formula | C26H26F3NO3 |
Molar mass | 457.493 g·mol−1 |
3D model (JSmol) | |
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Etrasimod, sold under the brand name Velsipity, is a medication that is used for the treatment of ulcerative colitis. [3] It is a selective sphingosine-1-phosphate (S1P) receptor modulator that modifies the activity of the immune system. [3] It is taken by mouth. [3]
The most common side effects include lymphopenia (low levels of lymphocytes) and headache. [5]
Etrasimod was discovered by Arena Pharmaceuticals, with subsequent development by Pfizer. [7] Etrasimod was approved for medical use in the United States in October 2023, [3] and in the European Union in February 2024. [5]
Etrasimod is used for the treatment of moderate to severe ulcerative colitis. [3] [5]
It works by causing T cells to become trapped in the lymph nodes, preventing them from entering the bloodstream, from where they would travel to other tissues in the body and mediate inflammation. [8] [9] [10] [11] [12] [13]
Velsipity was approved by the US Food and Drug Administration (FDA) in October 2023. [3] [14] [15]
In December 2023, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Velsipity, intended for the treatment of ulcerative colitis. [5] The applicant for this medicinal product is Pfizer Europe MA EEIG. [5] Etrasimod was approved for medical use in the European Union in February 2024. [5]
Etrasimod is the international nonproprietary name. [16]
Ulcerative colitis (UC) is one of the two types of inflammatory bowel disease (IBD), with the other type being Crohn's disease. It is a long-term condition that results in inflammation and ulcers of the colon and rectum. The primary symptoms of active disease are abdominal pain and diarrhea mixed with blood (hematochezia). Weight loss, fever, and anemia may also occur. Often, symptoms come on slowly and can range from mild to severe. Symptoms typically occur intermittently with periods of no symptoms between flares. Complications may include abnormal dilation of the colon (megacolon), inflammation of the eye, joints, or liver, and colon cancer.
Infliximab, a chimeric monoclonal antibody, sold under the brand name Remicade among others, is a medication used to treat a number of autoimmune diseases. This includes Crohn's disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, and Behçet's disease. It is given by slow injection into a vein, typically at six- to eight-week intervals.
Fingolimod, sold under the brand name Gilenya, is an immunomodulating medication, used for the treatment of multiple sclerosis. Fingolimod is a sphingosine-1-phosphate receptor modulator, which sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction. It has been reported to reduce the rate of relapses in relapsing-remitting multiple sclerosis by approximately one-half over a two-year period.
Sphingosine-1-phosphate (S1P) is a signaling sphingolipid, also known as lysosphingolipid. It is also referred to as a bioactive lipid mediator. Sphingolipids at large form a class of lipids characterized by a particular aliphatic aminoalcohol, which is sphingosine.
Ustekinumab, sold under the brand name Stelara among others, is a monoclonal antibody medication developed by Janssen Pharmaceuticals, for the treatment of Crohn's disease, ulcerative colitis, plaque psoriasis and psoriatic arthritis, targeting both IL-12 and IL-23.
Tremelimumab, sold under the brand name Imjudo, is a fully human monoclonal antibody used for the treatment of hepatocellular carcinoma. Tremelimumab is designed to attach to and block CTLA-4, a protein that controls the activity of T cells, which are part of the immune system.
Maraviroc, sold under the brand names Selzentry (US) and Celsentri (EU), is an antiretroviral medication used to treat HIV infection. It is taken by mouth. It is in the CCR5 receptor antagonist class.
Vedolizumab, sold under the brand name Entyvio, is a monoclonal antibody medication developed by Millennium Pharmaceuticals, Inc. for the treatment of ulcerative colitis and Crohn's disease. It binds to integrin α4β7, blocking the α4β7 integrin results in gut-selective anti-inflammatory activity.
Tofacitinib, sold under the brand Xeljanz among others, is a medication used to treat rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, polyarticular course juvenile idiopathic arthritis, and ulcerative colitis. It is a janus kinase (JAK) inhibitor, discovered and developed by the National Institutes of Health and Pfizer.
Tralokinumab sold under the brand names Adtralza (EU/UK) and Adbry (US) among others, is a human monoclonal antibody used for the treatment of atopic dermatitis. Tralokinumab targets the cytokine interleukin 13.
Ponesimod, sold under the brand name Ponvory, is a medication for the treatment of multiple sclerosis. It is a sphingosine-1-phosphate receptor modulator.
Ozanimod, sold under the brand name Zeposia, is an immunomodulatory medication for the treatment of relapsing multiple sclerosis and ulcerative colitis. It acts as a sphingosine-1-phosphate receptor (S1PR) agonist, sequestering lymphocytes to peripheral lymphoid organs and away from their sites of chronic inflammation.
Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist medication which is used in the treatment of prostate cancer in men and uterine fibroids in women. It is taken by mouth.
Siponimod, sold under the brand name Mayzent, is a selective sphingosine-1-phosphate receptor modulator for oral use that is used for multiple sclerosis (MS). It is intended for once-daily oral administration.
Fezolinetant, sold under the brand name Veozah among others, is a medication used for the treatment of hot flashes (vasomotor symptoms) due to menopause. It is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which is under development by for the treatment of sex hormone-related disorders. It is taken by mouth. It is developed by Astellas Pharma which acquired it from Ogeda (formerly Euroscreen) in April 2017.
Rimegepant, sold under the brand name Nurtec ODT among others, is a medication used for the acute treatment of migraine with or without aura in adults and the prophylactic/ preventive treatment of episodic migraine in adults. It is taken by mouth to dissolve on or under the tongue. It works by blocking CGRP receptors.
Sphingosine-1-phosphate receptor modulators are a class of drugs used as immunomodulators, most notably in cases of multiple sclerosis.
Mirikizumab, sold under the brand name Omvoh, is a monoclonal antibody used for the treatment of ulcerative colitis. It is designed to attach to interleukin-23 (IL-23) and block its activity.
Mosunetuzumab, sold under the brand name Lunsumio, is a monoclonal antibody used for the treatment of follicular lymphoma. It bispecifically binds CD20 and CD3 to engage T-cells. It was developed by Genentech.
Edward Roberts FRSC., is a British-born American scientist with expertise in biochemistry and synthetic organic chemistry. He is recognized for his significant contributions to medicinal chemistry, the design and discovery of new medicines in the development of novel therapeutics.