Fulvestrant

Estrogen Receptor Antagonist — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Fulvestrant is an ofp drug in the Estrogen Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2002. Its mechanism of action is classified as Estrogen Receptor Antagonists and Selective Estrogen Receptor Modulators. DrugCentral lists 11 molecular targets, including PGR, ESR1 and ESR2. Recorded indications include Metastatic Breast Cancer Progression Post-Antiestrogen Therapy.

• Approval status: ofp (first approved 2002 by the FDA).
• Drug class: Estrogen Receptor Antagonist.
• Mechanism of action: Estrogen Receptor Antagonists; Selective Estrogen Receptor Modulators.
• Molecular targets: PGR, ESR1, ESR2 and ESRRA (11 listed in DrugCentral).
• Indications: Metastatic Breast Cancer Progression Post-Antiestrogen Therapy.
• ATC code: L02BA03 (Anti-estrogens).
• Molecular formula: C32H47F5O3S; molecular weight 606.78 g/mol.

Indications & contraindications

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

Indications (1)

• Metastatic Breast Cancer Progression Post-Antiestrogen Therapy

Contraindications (5)

• Blood coagulation disorder
• Breastfeeding (mother)
• Disease of liver
• Pregnancy, function
• Thrombocytopenic disorder

Mechanism & targets

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

Molecular targets (11)

Target	Gene	Action	Activity
Progesterone receptor	PGR	unknown	IC50 9.68
Estrogen receptor	ESR1	antagonist	Ki 9.62
Estrogen receptor beta	ESR2	antagonist	Ki 8.74
Steroid hormone receptor ERR1	ESRRA	unknown	IC50 8.70
Estrogen receptor	Esr1	unknown	IC50 8.23
Bifunctional epoxide hydrolase 2	EPHX2	unknown	Ki 7.59
G-protein coupled estrogen receptor 1	GPER1	unknown	EC50 7.00
Bile acid receptor	NR1H4	unknown	IC50 6.10
Nuclear receptor subfamily 1 group I member 2	NR1I2	unknown	EC50 5.71
NAD-dependent protein deacylase sirtuin-5, mitochondrial	SIRT5	unknown	IC50 5.58
Beta-lactamase TEM	bla; blaT-3; blaT-4;	unknown	IC50 4.25

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2004-03-10	EMA	—	—
2002-04-25	FDA	—	ASTRAZENECA

ATC classification

ATC code	Therapeutic hierarchy
L02BA03	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: ERBB2, ESR1, ESR2, PGR · Testing Required
• FDA label: ERBB2, ESR1, ESR2, PGR · Testing Required
• HCSC label: ERBB2, ESR1, ESR2 · Testing Required
• PMDA label: ESR1, ESR2 · Testing Required

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
Malignant neoplasm progression	6015.8
Metastases to bone	4175.3
Metastases to liver	3345.5
Neoplasm progression	2991.6
Neutropenia	2132.5
Breast cancer metastatic	1266.2
Tumour marker increased	1193.5
White blood cell count decreased	1135.8
Metastases to lung	1113.5
Osteonecrosis of jaw	899.3
Metastases to lymph nodes	762.6
Carbohydrate antigen 15-3 increased	711.6

Chemical structure

• Molecular formula: C₃₂H₄₇F₅O₃S
• Molecular weight: 606.78 g/mol
• CAS number: —
• InChIKey: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• PubChem CID: 104741

C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC1=CC(O)=CC=C31

Frequently asked questions

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

What is Fulvestrant used for?

DrugCentral lists the following indications for Fulvestrant: Metastatic Breast Cancer Progression Post-Antiestrogen Therapy.

How does Fulvestrant work?

Fulvestrant is classified as Estrogen Receptor Antagonists and Selective Estrogen Receptor Modulators; its molecular targets in DrugCentral include PGR, ESR1 (antagonist), ESR2 (antagonist) and ESRRA.

When was Fulvestrant first approved?

Fulvestrant was first approved by the FDA in 2002.

What drug class does Fulvestrant belong to?

Fulvestrant is in the Estrogen Receptor Antagonist class.

What is the chemical formula of Fulvestrant?

Fulvestrant has the molecular formula C32H47F5O3S and a molecular weight of 606.78 g/mol.

Sources

• DrugCentral drug card 1255 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1358 — compound record and bioactivity
• PubChem CID 104741 — chemical identifiers
• DrugBank DB00947 — drug record
• FDA UNII 22X328QOC4 — substance identity
• DailyMed: FDA labels for Fulvestrant — current prescribing information (label search)
• UniProt P06401 (PGR) — target protein
• UniProt P03372 (ESR1) — target protein
• UniProt Q92731 (ESR2) — target protein
• UniProt P11474 (ESRRA) — target protein
• UniProt P34913 (EPHX2) — target protein
• UniProt Q99527 (GPER1) — 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.