Exemestane

Aromatase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Exemestane is an ofp drug in the Aromatase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1999. Its mechanism of action is classified as Aromatase Inhibitors. DrugCentral lists 3 molecular targets, including Cyp19a1, CYP19A1 and AR. Recorded indications include Advanced Breast Cancer Progression Post-Antiestrogen Therapy and Hormone receptor positive malignant neoplasm of breast.

• Approval status: ofp (first approved 1999 by the FDA).
• Drug class: Aromatase Inhibitor.
• Mechanism of action: Aromatase Inhibitors.
• Molecular targets: Cyp19a1, CYP19A1 and AR (3 listed in DrugCentral).
• Indications: Advanced Breast Cancer Progression Post-Antiestrogen Therapy and Hormone receptor positive malignant neoplasm of breast.
• ATC code: L02BG06 (Aromatase inhibitors).
• Molecular formula: C20H24O2; molecular weight 296.41 g/mol.

Indications & contraindications

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

Indications (2)

• Advanced Breast Cancer Progression Post-Antiestrogen Therapy
• Hormone receptor positive malignant neoplasm of breast

Off-label uses (1)

• Prevention of Breast Carcinoma

Contraindications (2)

• Osteopenia
• Pregnancy, function

Mechanism & targets

• Mechanism of action (MoA): Aromatase Inhibitors
• Established pharmacologic class: Aromatase Inhibitor

Molecular targets (3)

Target	Gene	Action	Activity
Aromatase	Cyp19a1	unknown	IC50 7.52
Aromatase	CYP19A1	inhibitor	IC50 5.69
Androgen receptor	AR	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1999-10-21	FDA	—	PHARMACIA AND UPJOHN	Yes

ATC classification

ATC code	Therapeutic hierarchy
L02BG06	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Aromatase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• FDA label: ESR1, ESR2, PGR · Testing Required
• HCSC 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	2105.7
Metastases to bone	1653.4
Metastases to liver	1357.9
Neoplasm progression	1091.5
Osteonecrosis of jaw	820.2
Breast cancer metastatic	629.9
Metastases to lung	558.9
Disease progression	503.9
Amaurosis fugax	490.5
Tumour marker increased	460.0
Metastases to lymph nodes	441.9
Ascites	417.5

Chemical structure

• Molecular formula: C₂₀H₂₄O₂
• Molecular weight: 296.41 g/mol
• CAS number: 107868-30-4
• InChIKey: BFYIZQONLCFLEV-DAELLWKTSA-N
• PubChem CID: 60198

C[C@]12CC[C@H]3[C@@H](CC(=C)C4=CC(=O)C=C[C@]34C)[C@@H]1CCC2=O

Frequently asked questions

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

What is Exemestane used for?

DrugCentral lists the following indications for Exemestane: Advanced Breast Cancer Progression Post-Antiestrogen Therapy and Hormone receptor positive malignant neoplasm of breast.

How does Exemestane work?

Exemestane is classified as Aromatase Inhibitors; its molecular targets in DrugCentral include Cyp19a1, CYP19A1 (inhibitor) and AR.

When was Exemestane first approved?

Exemestane was first approved by the FDA in 1999.

What drug class does Exemestane belong to?

Exemestane is in the Aromatase Inhibitor class.

What is the chemical formula of Exemestane?

Exemestane has the molecular formula C20H24O2 and a molecular weight of 296.41 g/mol.

Sources

• DrugCentral drug card 1122 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200374 — compound record and bioactivity
• PubChem CID 60198 — chemical identifiers
• DrugBank DB00990 — drug record
• FDA UNII NY22HMQ4BX — substance identity
• DailyMed: FDA labels for Exemestane — current prescribing information (label search)
• UniProt P11511 (CYP19A1) — target protein
• UniProt P10275 (AR) — 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.