Ospemifene

Estrogen Agonist/Antagonist — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Ospemifene is an ofp drug in the Estrogen Agonist/Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2013. Its mechanism of action is classified as Selective Estrogen Receptor Modulators. DrugCentral lists 2 molecular targets, including ESR2 and ESR1. Recorded indications include Atrophic vulva and Dyspareunia.

• Approval status: ofp (first approved 2013 by the FDA).
• Drug class: Estrogen Agonist/Antagonist.
• Mechanism of action: Selective Estrogen Receptor Modulators.
• Molecular targets: ESR2 and ESR1 (2 listed in DrugCentral).
• Indications: Atrophic vulva and Dyspareunia.
• ATC code: G03XC05 (Selective estrogen receptor modulators).
• Molecular formula: C24H23ClO2; molecular weight 378.90 g/mol.

Indications & contraindications

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

Indications (2)

• Atrophic vulva
• Dyspareunia

Mechanism & targets

• Mechanism of action (MoA): Selective Estrogen Receptor Modulators
• Established pharmacologic class: Estrogen Agonist/Antagonist

Molecular targets (2)

Target	Gene	Action	Activity
Estrogen receptor beta	ESR2	antagonist	Ki 6.39
Estrogen receptor	ESR1	modulator	IC50 6.08

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2014-11-20	EMA	—	Shionogi Limited
2013-02-26	FDA	—	SHIONOGI INC

ATC classification

ATC code	Therapeutic hierarchy
G03XC05	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › Selective estrogen receptor modulators

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2B6, CYP2C9
• FDA label: CYP2B6, CYP2C9
• HCSC label: CYP2B6, CYP2C9

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
Hot flush	329.8
Labelled drug-drug interaction medication error	206.9
Vaginal discharge	186.2
Vaginal haemorrhage	148.7
No adverse event	121.7
Therapeutic response unexpected	121.4
Muscle spasms	104.3
Vulvovaginal burning sensation	80.4
Vulvovaginal discomfort	72.8
Inability to afford medication	56.6
Vulvovaginal pruritus	55.9
Hyperhidrosis	48.0

Chemical structure

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

• Molecular formula: C₂₄H₂₃ClO₂
• Molecular weight: 378.90 g/mol
• CAS number: 128607-22-7
• InChIKey: LUMKNAVTFCDUIE-VHXPQNKSSA-N
• PubChem CID: 3036505

OCCOC1=CC=C(C=C1)C(=C(\CCCl)C1=CC=CC=C1)\C1=CC=CC=C1

Frequently asked questions

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

What is Ospemifene used for?

DrugCentral lists the following indications for Ospemifene: Atrophic vulva and Dyspareunia.

How does Ospemifene work?

Ospemifene is classified as Selective Estrogen Receptor Modulators; its molecular targets in DrugCentral include ESR2 (antagonist) and ESR1 (modulator).

When was Ospemifene first approved?

Ospemifene was first approved by the FDA in 2013.

What drug class does Ospemifene belong to?

Ospemifene is in the Estrogen Agonist/Antagonist class.

What is the chemical formula of Ospemifene?

Ospemifene has the molecular formula C24H23ClO2 and a molecular weight of 378.90 g/mol.

Sources

• DrugCentral drug card 4749 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2105395 — compound record and bioactivity
• PubChem CID 3036505 — chemical identifiers
• DrugBank DB04938 — drug record
• FDA UNII B0P231ILBK — substance identity
• DailyMed: FDA labels for Ospemifene — current prescribing information (label search)
• UniProt Q92731 (ESR2) — target protein
• UniProt P03372 (ESR1) — 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.