Degarelix

Gonadotropin Releasing Hormone Receptor Antagonist — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Degarelix is a drug in the Gonadotropin Releasing Hormone Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2008. Its mechanism of action is classified as Gonadotropin Releasing Hormone Receptor Antagonists. DrugCentral lists 1 molecular target, including GNRHR. Recorded indications include Advanced hormone-dependent prostate cancer and Advanced Prostatic Carcinoma.

• Drug class: Gonadotropin Releasing Hormone Receptor Antagonist.
• Mechanism of action: Gonadotropin Releasing Hormone Receptor Antagonists.
• Molecular targets: GNRHR (1 listed in DrugCentral).
• Indications: Advanced hormone-dependent prostate cancer and Advanced Prostatic Carcinoma.
• ATC code: L02BX02 (Other hormone antagonists and related agents).
• Molecular formula: C82H103ClN18O16; molecular weight 1632.29 g/mol.

Indications & contraindications

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

Indications (2)

• Advanced hormone-dependent prostate cancer
• Advanced Prostatic Carcinoma

Contraindications (10)

• Chronic heart failure
• Congenital long QT syndrome
• Disease of liver
• Hypokalemia
• Hypomagnesemia
• Liver function tests abnormal
• Osteopenia
• Pregnancy, function
• Prolonged QT interval
• Torsades de pointes

Mechanism & targets

• Mechanism of action (MoA): Gonadotropin Releasing Hormone Receptor Antagonists
• Established pharmacologic class: Gonadotropin Releasing Hormone Receptor Antagonist

Molecular targets (1)

Target	Gene	Action	Activity
Gonadotropin-releasing hormone receptor	GNRHR	antagonist	Ki 8.77

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2023-09-29	EMA	—	ACCORD HEALTHCARE S.L.U.
2012-06-26	PMDA	—	Astellas Pharma Inc.
2008-12-24	FDA	—	FERRING

ATC classification

ATC code	Therapeutic hierarchy
L02BX02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Other hormone antagonists and related agents

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
Product storage error	580.0
Prostatic specific antigen increased	420.4
Injection site erythema	353.9
Injection site pain	326.3
Hot flush	240.0
Injection site induration	234.6
Injection site swelling	230.5
Interstitial lung disease	183.4
Injection site cellulitis	147.0
Osteonecrosis of jaw	143.8
Injection site mass	130.5
Injection site nodule	103.6

Chemical structure

• Molecular formula: C₈₂H₁₀₃ClN₁₈O₁₆
• Molecular weight: 1632.29 g/mol
• CAS number: 214766-78-6
• InChIKey: MEUCPCLKGZSHTA-XYAYPHGZSA-N
• PubChem CID: 16136245

CC(C)C[C@H](NC(=O)[C@@H](CC1=CC=C(NC(N)=O)C=C1)NC(=O)[C@H](CC1=CC=C(NC(=O)[C@@H]2CC(=O)NC(=O)N2)C=C1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC1=CN=CC=C1)NC(=O)[C@@H](CC1=CC=C(Cl)C=C1)NC(=O)[C@@H](CC1=CC2=C(C=CC=C2)C=C1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O

Frequently asked questions

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

What is Degarelix used for?

DrugCentral lists the following indications for Degarelix: Advanced hormone-dependent prostate cancer and Advanced Prostatic Carcinoma.

How does Degarelix work?

Degarelix is classified as Gonadotropin Releasing Hormone Receptor Antagonists; its molecular targets in DrugCentral include GNRHR (antagonist).

When was Degarelix first approved?

Degarelix was first approved by the FDA in 2008.

What drug class does Degarelix belong to?

Degarelix is in the Gonadotropin Releasing Hormone Receptor Antagonist class.

What is the chemical formula of Degarelix?

Degarelix has the molecular formula C82H103ClN18O16 and a molecular weight of 1632.29 g/mol.

Sources

• DrugCentral drug card 4379 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2028987 — compound record and bioactivity
• PubChem CID 16136245 — chemical identifiers
• DrugBank DB06699 — drug record
• FDA UNII SX0XJI3A11 — substance identity
• DailyMed: FDA labels for Degarelix — current prescribing information (label search)
• UniProt P30968 (GNRHR) — 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.