Toremifene

Estrogen Agonist/Antagonist — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Toremifene is an ofp drug in the Estrogen Agonist/Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1997. Its mechanism of action is classified as Selective Estrogen Receptor Modulators. DrugCentral lists 4 molecular targets, including HTR6, GP and ESR1. Recorded indications include Metastatic Breast Carcinoma.

• Approval status: ofp (first approved 1997 by the FDA).
• Drug class: Estrogen Agonist/Antagonist.
• Mechanism of action: Selective Estrogen Receptor Modulators.
• Molecular targets: HTR6, GP, ESR1 and ESRRG (4 listed in DrugCentral).
• Indications: Metastatic Breast Carcinoma.
• ATC code: L02BA02 (Anti-estrogens).
• Molecular formula: C26H28ClNO; molecular weight 405.97 g/mol.

Indications & contraindications

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

Indications (1)

• Metastatic Breast Carcinoma

Contraindications (12)

• Breastfeeding (mother)
• Congenital long QT syndrome
• Endometrial hyperplasia
• Hypercalcemia
• Hypokalemia
• Hypomagnesemia
• Leukopenia
• Pregnancy, function
• Prolonged QT interval
• Thrombocytopenic disorder
• Thromboembolic disorder
• Torsades de pointes

Mechanism & targets

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

Molecular targets (4)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 5.38
Envelope glycoprotein	GP	unknown	Kd 4.80
Estrogen receptor	ESR1	modulator	—
Estrogen-related receptor gamma	ESRRG	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1997-05-29	FDA	—	PROSTRAKAN INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
L02BA02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Anti-estrogens

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ESR1, ESR2
• FDA label: ESR1, ESR2
• HCSC label

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
Osteonecrosis of jaw	75.8
Endometrial thickening	50.6
Pseudocirrhosis	47.2
Osteomyelitis	44.8
Endometrial hyperplasia	40.4

Chemical structure

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

• Molecular formula: C₂₆H₂₈ClNO
• Molecular weight: 405.97 g/mol
• CAS number: —
• InChIKey: XFCLJVABOIYOMF-QPLCGJKRSA-N
• PubChem CID: 3005573

CN(C)CCOC1=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 Toremifene used for?

DrugCentral lists the following indications for Toremifene: Metastatic Breast Carcinoma.

How does Toremifene work?

Toremifene is classified as Selective Estrogen Receptor Modulators; its molecular targets in DrugCentral include HTR6, GP, ESR1 (modulator) and ESRRG.

When was Toremifene first approved?

Toremifene was first approved by the FDA in 1997.

What drug class does Toremifene belong to?

Toremifene is in the Estrogen Agonist/Antagonist class.

What is the chemical formula of Toremifene?

Toremifene has the molecular formula C26H28ClNO and a molecular weight of 405.97 g/mol.

Sources

• DrugCentral drug card 2709 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200675 — compound record and bioactivity
• PubChem CID 3005573 — chemical identifiers
• DrugBank DB00539 — drug record
• FDA UNII 7NFE54O27T — substance identity
• DailyMed: FDA labels for Toremifene — current prescribing information (label search)
• UniProt P50406 (HTR6) — target protein
• UniProt P03372 (ESR1) — target protein
• UniProt P62508 (ESRRG) — 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.