Etrasimod
Velsipity (etrasimod) is a small molecule pharmaceutical. Etrasimod was first approved as Velsipity on 2023-10-12. It is used to treat ulcerative colitis in the USA. The pharmaceutical is active against sphingosine 1-phosphate receptor 1. In addition, it is known to target sphingosine 1-phosphate receptor 4 and sphingosine 1-phosphate receptor 5.
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2Y
5Y
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Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| digestive system diseases | D004066 |
Trade Name
FDA
EMA
Velsipity
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| velsipity | New Drug Application | 2024-09-24 |
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
ETRASIMOD ARGININE, VELSIPITY, PFIZER | |||
| 2028-10-12 | NCE | ||
ATC Codes
No data
HCPCS
No data
Clinical
Clinical Trials
25 clinical trials
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Indications Phases 4
No data
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Ulcerative colitis | D003093 | EFO_0000729 | K51 | — | 5 | 5 | — | 4 | 14 |
| Colitis | D003092 | EFO_0003872 | K52.9 | — | 6 | 5 | — | 3 | 14 |
| Ulcer | D014456 | MPATH_579 | — | — | 5 | 5 | — | 2 | 12 |
| Atopic dermatitis | D003876 | EFO_0000274 | L20 | — | 2 | 1 | — | — | 2 |
| Eczema | D004485 | HP_0000964 | L30.9 | — | 2 | 1 | — | — | 2 |
| Dermatitis | D003872 | HP_0011123 | L30.9 | — | 2 | 1 | — | — | 2 |
| Crohn disease | D003424 | EFO_0000384 | K50 | — | — | 1 | — | 1 | 2 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Inflammatory bowel diseases | D015212 | EFO_0003767 | — | — | 1 | — | — | 1 | 2 |
| Eosinophilic esophagitis | D057765 | EFO_0004232 | K20.0 | — | 1 | — | — | — | 1 |
| Esophagitis | D004941 | HP_0100633 | K20 | — | 1 | — | — | — | 1 |
| Alopecia areata | D000506 | EFO_0004192 | L63 | — | 1 | — | — | — | 1 |
| Alopecia | D000505 | HP_0002293 | L64 | — | 1 | — | — | — | 1 |
| Biliary liver cirrhosis | D008105 | — | K74.3 | — | 1 | — | — | — | 1 |
| Cholangitis | D002761 | HP_0030151 | K83.0 | — | 1 | — | — | — | 1 |
| Intestinal diseases | D007410 | HP_0002242 | K63.9 | — | 1 | — | — | — | 1 |
| Pyoderma gangrenosum | D017511 | EFO_0006835 | L88 | — | 1 | — | — | — | 1 |
| Pyoderma | D011711 | HP_0000999 | L08.0 | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 2 | — | — | — | — | 2 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Etrasimod |
| INN | etrasimod |
| Description | Etrasimod is an organic heterotricyclic compound that is 1,2,3,4-tetrahydrocyclopenta[b]indole substituted by carboxymethyl and [4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy groups at positions 3R and 7, respectively. It is a potent and functional antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50 = 1.88 nM in CHO cells). It has a role as an antibacterial agent, a sphingosine-1-phosphate receptor 1 antagonist, an immunosuppressive agent and an anti-inflammatory drug. It is a member of (trifluoromethyl)benzenes, a member of cyclopentanes, an aromatic ether, a monocarboxylic acid and an organic heterotricyclic compound. It is a conjugate acid of an etrasimod(1-). |
| Classification | Small molecule |
| Drug class | immunomodulators |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | O=C(O)C[C@H]1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 |
Identifiers
| PDB | — |
| CAS-ID | 1206123-37-6 |
| RxCUI | — |
| ChEMBL ID | CHEMBL3358920 |
| ChEBI ID | — |
| PubChem CID | 44623998 |
| DrugBank | DB14766 |
| UNII ID | 6WH8495MMH (ChemIDplus, GSRS) |
Target
Agency Approved
S1PR1
S1PR1
Organism
Homo sapiens
Gene name
S1PR1
Gene synonyms
CHEDG1, EDG1
NCBI Gene ID
Protein name
sphingosine 1-phosphate receptor 1
Protein synonyms
CD363, Endothelial differentiation G-protein coupled receptor 1, endothelial differentiation, sphingolipid G-protein-coupled receptor, 1, S1P receptor 1, S1P receptor Edg-1, Sphingosine 1-phosphate receptor Edg-1, sphingosine 1-phosphate receptor EDG1
Uniprot ID
Mouse ortholog
S1pr1 (13609)
sphingosine 1-phosphate receptor 1 (Q9R235)
Alternate
S1PR4
S1PR4
S1PR5
S1PR5
Organism
Homo sapiens
Gene name
S1PR4
Gene synonyms
EDG6
NCBI Gene ID
Protein name
sphingosine 1-phosphate receptor 4
Protein synonyms
Endothelial differentiation G-protein coupled receptor 6, endothelial differentiation, lysophosphatidic acid G-protein-coupled receptor, 6, S1P receptor 4, S1P receptor Edg-6, Sphingosine 1-phosphate receptor Edg-6
Uniprot ID
Mouse ortholog
S1pr4 (13611)
sphingosine 1-phosphate receptor 4 (Q9Z0L1)
Variants
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 267 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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102 adverse events reported
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