Etrasimod

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Etrasimod is an onp drug catalogued in DrugCentral. It was first approved by the FDA in 2023. DrugCentral lists 5 molecular targets, including S1PR1, S1PR5 and S1PR4. Recorded indications include Moderately to severely active ulcerative colitis.

• Approval status: onp (first approved 2023 by the FDA).
• Molecular targets: S1PR1, S1PR5, S1PR4 and ADORA3 (5 listed in DrugCentral).
• Indications: Moderately to severely active ulcerative colitis.
• ATC code: L04AE05 (Sphingosine-1-phosphate (S1P) receptor modulators).
• Molecular formula: C26H26F3NO3; molecular weight 457.49 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Moderately to severely active ulcerative colitis

Contraindications (7)

• Angina pectoris
• Cerebrovascular accident
• Decompensated cardiac failure
• Mobitz type II atrioventricular block
• Myocardial infarction
• Sick sinus syndrome
• Transient ischemic attack

Mechanism & targets

Molecular targets (5)

Target	Gene	Action	Activity
Sphingosine 1-phosphate receptor 1	S1PR1	agonist	EC50 7.36
Sphingosine 1-phosphate receptor 5	S1PR5	agonist	EC50 7.20
Sphingosine 1-phosphate receptor 4	S1PR4	agonist	EC50 6.85
Adenosine receptor A3	ADORA3	unknown	IC50 5.48
Sphingosine 1-phosphate receptor 3	S1PR3	partial agonist	EC50 5.22

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2023-12-10	FDA	—	PFIZER INC

ATC classification

ATC code	Therapeutic hierarchy
L04AE05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Sphingosine-1-phosphate (S1P) receptor modulators

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2C9 · Actionable PGx
• FDA label: CYP2C9 · Informative PGx
• HCSC label: CYP2C9 · Informative PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Diabetic eye disease	441.6
Drug ineffective	147.3
Condition aggravated	144.7
Type 2 diabetes mellitus	144.3
Haematochezia	87.5
Colitis	81.7
Colitis ulcerative	80.9
Rectal haemorrhage	65.1
Large intestine erosion	56.4
Defaecation urgency	51.1
Faecal calprotectin increased	48.7

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Etrasimod is on its molecule page.

• Molecular formula: C₂₆H₂₆F₃NO₃
• Molecular weight: 457.49 g/mol
• CAS number: —
• InChIKey: MVGWUTBTXDYMND-QGZVFWFLSA-N
• PubChem CID: 44623998

OC(=O)C[C@H]1CCC2=C1NC1=CC=C(OCC3=CC=C(C4CCCC4)C(=C3)C(F)(F)F)C=C21

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Etrasimod used for?

DrugCentral lists the following indications for Etrasimod: Moderately to severely active ulcerative colitis.

How does Etrasimod work?

Its molecular targets in DrugCentral include S1PR1 (agonist), S1PR5 (agonist), S1PR4 (agonist) and ADORA3.

When was Etrasimod first approved?

Etrasimod was first approved by the FDA in 2023.

What is the chemical formula of Etrasimod?

Etrasimod has the molecular formula C26H26F3NO3 and a molecular weight of 457.49 g/mol.

Sources

• DrugCentral drug card 5747 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3358920 — compound record and bioactivity
• PubChem CID 44623998 — chemical identifiers
• DrugBank DB14766 — drug record
• FDA UNII 6WH8495MMH — substance identity
• DailyMed: FDA labels for Etrasimod — current prescribing information (label search)
• UniProt P21453 (S1PR1) — target protein
• UniProt Q9H228 (S1PR5) — target protein
• UniProt O95977 (S1PR4) — target protein
• UniProt P0DMS8 (ADORA3) — target protein
• UniProt Q99500 (S1PR3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.