Epinastine

Adrenergic Receptor Agonist — RESPIRATORY SYSTEM

Key facts

Epinastine is an ofp drug in the Adrenergic Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2003. Its mechanism of action is classified as Adrenergic Agonists and Histamine H1 Receptor Antagonists. DrugCentral lists 11 molecular targets, including HRH1, HRH1 and SLC47A1. Recorded indications include Allergic conjunctivitis and Ocular Itching.

• Approval status: ofp (first approved 2003 by the FDA).
• Drug class: Adrenergic Receptor Agonist; Histamine-1 Receptor Inhibitor.
• Mechanism of action: Adrenergic Agonists; Histamine H1 Receptor Antagonists.
• Molecular targets: HRH1, HRH1, SLC47A1 and SLC22A2 (11 listed in DrugCentral).
• Indications: Allergic conjunctivitis and Ocular Itching.
• ATC code: R06AX24 (Other antihistamines for systemic use).
• Molecular formula: C16H15N3; molecular weight 249.32 g/mol.

Indications & contraindications

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

Indications (2)

• Allergic conjunctivitis
• Ocular Itching

Mechanism & targets

• Mechanism of action (MoA): Adrenergic Agonists; Histamine H1 Receptor Antagonists
• Established pharmacologic class: Adrenergic Receptor Agonist; Histamine-1 Receptor Inhibitor

Molecular targets (11)

Target	Gene	Action	Activity
Histamine H1 receptor	HRH1	antagonist	Ki 8.90
Histamine H1 receptor	HRH1	unknown	IC50 8.80
Multidrug and toxin extrusion protein 1	SLC47A1	unknown	IC50 5.96
Solute carrier family 22 member 2	SLC22A2	unknown	IC50 5.37
Multidrug and toxin extrusion protein 2	SLC47A2	unknown	IC50 4.53
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 4.00
Histamine H2 receptor	HRH2	unknown	—
Alpha-2A adrenergic receptor	ADRA2A	unknown	—
Alpha-1A adrenergic receptor	ADRA1A	unknown	—
5-hydroxytryptamine receptor 2A	HTR2A	unknown	—
Multidrug resistance protein 1	ABCB1	unknown	—

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2019-09-20	PMDA	—	Santen Pharmaceutical Co., Ltd.
2003-10-16	FDA	—	ALLERGAN

ATC classification

ATC code	Therapeutic hierarchy
R06AX24	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Other antihistamines for systemic use
S01GX10	SENSORY ORGANS › OPHTHALMOLOGICALS › DECONGESTANTS AND ANTIALLERGICS › Other antiallergics

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
Treatment failure	161.7
Hepatic function abnormal	110.1
Drug eruption	60.8
Interstitial lung disease	55.6
Syphilis	51.2
Pyrexia	50.4
Platelet count decreased	46.1
Pemphigoid	43.9
Decreased appetite	38.2
Alopecia areata	37.5
Cardiac failure	32.8
Enzyme level abnormal	31.2

Chemical structure

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

• Molecular formula: C₁₆H₁₅N₃
• Molecular weight: 249.32 g/mol
• CAS number: 80012-43-7
• InChIKey: WHWZLSFABNNENI-UHFFFAOYSA-N
• PubChem CID: 3241

NC1=NCC2N1C1=C(CC3=C2C=CC=C3)C=CC=C1

Frequently asked questions

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

What is Epinastine used for?

DrugCentral lists the following indications for Epinastine: Allergic conjunctivitis and Ocular Itching.

How does Epinastine work?

Epinastine is classified as Adrenergic Agonists and Histamine H1 Receptor Antagonists; its molecular targets in DrugCentral include HRH1 (antagonist), HRH1, SLC47A1 and SLC22A2.

When was Epinastine first approved?

Epinastine was first approved by the FDA in 2003.

What drug class does Epinastine belong to?

Epinastine is in the Adrenergic Receptor Agonist class.

What is the chemical formula of Epinastine?

Epinastine has the molecular formula C16H15N3 and a molecular weight of 249.32 g/mol.

Sources

• DrugCentral drug card 1027 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1106 — compound record and bioactivity
• PubChem CID 3241 — chemical identifiers
• DrugBank DB00751 — drug record
• FDA UNII Q13WX941EF — substance identity
• DailyMed: FDA labels for Epinastine — current prescribing information (label search)
• UniProt P35367 (HRH1) — target protein
• UniProt Q96FL8 (SLC47A1) — target protein
• UniProt O15244 (SLC22A2) — target protein
• UniProt Q86VL8 (SLC47A2) — target protein
• UniProt Q12809 (KCNH2) — target protein
• UniProt P25021 (HRH2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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