Eletriptan
Serotonin-1b and Serotonin-1d Receptor Agonist — NERVOUS SYSTEM
Also known as: eletriptan hydrobromide, relpax, UK 116044-04, UK-116,044
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Eletriptan is an ofp drug in the Serotonin-1b and Serotonin-1d Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2002. Its mechanism of action is classified as Serotonin 1b Receptor Agonists and Serotonin 1d Receptor Agonists. DrugCentral lists 5 molecular targets, including HTR1D, HTR1B and HTR1F. Recorded indications include Migraine.
- Approval status: ofp (first approved 2002 by the FDA).
- Drug class: Serotonin-1b and Serotonin-1d Receptor Agonist.
- Mechanism of action: Serotonin 1b Receptor Agonists; Serotonin 1d Receptor Agonists.
- Molecular targets: HTR1D, HTR1B, HTR1F and HTR1A (5 listed in DrugCentral).
- Indications: Migraine.
- ATC code: N02CC06 (Selective serotonin (5HT1) agonists).
- Molecular formula: C22H26N2O2S; molecular weight 382.53 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (1)
- Migraine
Contraindications (24)
- Angina pectoris
- Cardiovascular event risk
- Cerebral ischemia
- Cerebrovascular accident
- Coronary artery spasm
- Diabetes mellitus
- Disease of liver
- Disorder of coronary artery
- Familial History of Cardiovascular Disease
- Hemiplegic migraine
- Hepatic failure
- Hypercholesterolemia
- Hypertensive disorder
- Hypertensive urgency
- Myocardial infarction
- Myocardial ischemia
- Obesity
- Peripheral vascular disease
- Prinzmetal angina
- Raynaud's phenomenon
- Serotonin syndrome
- Smokes tobacco daily
- Transient ischemic attack
- Vascular insufficiency of intestine
Mechanism & targets
| Mechanism of action (MoA) | Serotonin 1b Receptor Agonists; Serotonin 1d Receptor Agonists |
|---|---|
| Established pharmacologic class | Serotonin-1b and Serotonin-1d Receptor Agonist |
Molecular targets (5)
| Target | Gene | Action | Activity |
|---|---|---|---|
| 5-hydroxytryptamine receptor 1D | HTR1D | agonist | Kd 9.05 |
| 5-hydroxytryptamine receptor 1B | HTR1B | agonist | Kd 8.52 |
| 5-hydroxytryptamine receptor 1F | HTR1F | agonist | Ki 8.00 |
| 5-hydroxytryptamine receptor 1A | HTR1A | agonist | Ki 7.40 |
| 5-hydroxytryptamine receptor 1E | HTR1E | agonist | Ki 7.20 |
Regulatory approvals (1)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 2002-12-26 | FDA | — | PFIZER IRELAND |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
N02CC06 | NERVOUS SYSTEM › ANALGESICS › ANTIMIGRAINE PREPARATIONS › Selective serotonin (5HT1) agonists |
Pharmacogenomics
Drug-label and guideline annotations from PharmGKB and CPIC.
- Swissmedic label: CYP2D6 · 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 |
|---|---|
| Migraine | 268.8 |
| Medication overuse headache | 257.3 |
| Headache | 119.2 |
| Drug ineffective | 107.0 |
| Drug dependence | 99.1 |
| Paraesthesia | 94.4 |
| Drug abuse | 93.3 |
| Rheumatoid factor negative | 70.3 |
| Intentional product misuse | 69.7 |
| Recalled product administered | 68.0 |
| Rubber sensitivity | 52.6 |
| Feeling abnormal | 49.4 |
Chemical structure
| Molecular formula | C22H26N2O2S |
|---|---|
| Molecular weight | 382.53 g/mol |
| CAS number | — |
| InChIKey | PWVXXGRKLHYWKM-LJQANCHMSA-N |
| PubChem CID | 77993 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Eletriptan used for?
DrugCentral lists the following indications for Eletriptan: Migraine.
How does Eletriptan work?
Eletriptan is classified as Serotonin 1b Receptor Agonists and Serotonin 1d Receptor Agonists; its molecular targets in DrugCentral include HTR1D (agonist), HTR1B (agonist), HTR1F (agonist) and HTR1A (agonist).
When was Eletriptan first approved?
Eletriptan was first approved by the FDA in 2002.
What drug class does Eletriptan belong to?
Eletriptan is in the Serotonin-1b and Serotonin-1d Receptor Agonist class.
What is the chemical formula of Eletriptan?
Eletriptan has the molecular formula C22H26N2O2S and a molecular weight of 382.53 g/mol.
Browse: all drugs starting with E · drug guides by category · protein targets A–Z.
Sources
- DrugCentral drug card 995 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL1201003 — compound record and bioactivity
- PubChem CID 77993 — chemical identifiers
- DrugBank DB00216 — drug record
- FDA UNII 22QOO9B8KI — substance identity
- DailyMed: FDA labels for Eletriptan — current prescribing information (label search)
- UniProt P28221 (HTR1D) — target protein
- UniProt P28222 (HTR1B) — target protein
- UniProt P30939 (HTR1F) — target protein
- UniProt P08908 (HTR1A) — target protein
- UniProt P28566 (HTR1E) — target protein
- FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
- PharmGKB / CPIC — pharmacogenomic label annotations
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