Cabergoline

Ergot Derivative — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Cabergoline is an ofp drug in the Ergot Derivative class catalogued in DrugCentral. It was first approved by the FDA in 1996. DrugCentral lists 17 molecular targets, including DRD2, DRD3 and HTR2B. Recorded indications include Hyperprolactinemia and Prevention of ovarian hyperstimulation syndrome.

• Approval status: ofp (first approved 1996 by the FDA).
• Drug class: Ergot Derivative.
• Molecular targets: DRD2, DRD3, HTR2B and HTR2A (17 listed in DrugCentral).
• Indications: Hyperprolactinemia and Prevention of ovarian hyperstimulation syndrome.
• ATC code: G02CB03 (Prolactine inhibitors).
• Molecular formula: C26H37N5O2; molecular weight 451.62 g/mol.

Indications & contraindications

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

Indications (2)

• Hyperprolactinemia
• Prevention of ovarian hyperstimulation syndrome

Contraindications (9)

• Breastfeeding (mother)
• Disease of liver
• Fibrosis of lung
• Fibrosis of pericardium
• Heart valve disorder
• Hypertensive urgency
• Occlusive Vascular Disease
• Retroperitoneal fibrosis
• Severe pre-eclampsia

Mechanism & targets

• Established pharmacologic class: Ergot Derivative

Molecular targets (17)

Target	Gene	Action	Activity
D(2) dopamine receptor	DRD2	agonist	Ki 9.20
D(3) dopamine receptor	DRD3	agonist	Ki 9.10
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 8.85
5-hydroxytryptamine receptor 2A	HTR2A	agonist	Ki 8.20
5-hydroxytryptamine receptor 1D	HTR1D	agonist	Ki 8.10
Alpha-2A adrenergic receptor	ADRA2A	antagonist	Ki 7.90
Alpha-2C adrenergic receptor	ADRA2C	antagonist	Ki 7.70
5-hydroxytryptamine receptor 1A	HTR1A	agonist	Ki 7.70
D(1B) dopamine receptor	DRD5	agonist	Ki 7.70
D(4) dopamine receptor	DRD4	agonist	Ki 7.30
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 7.22
Alpha-2B adrenergic receptor	ADRA2B	antagonist	Ki 7.10
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 6.78
D(1A) dopamine receptor	DRD1	agonist	Ki 6.70
Alpha-1A adrenergic receptor	ADRA1A	antagonist	Ki 6.50
5-hydroxytryptamine receptor 1B	HTR1B	agonist	Ki 6.30
5-hydroxytryptamine receptor 2C	HTR2C	agonist	Ki 6.20

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
1999-08-01	PMDA	—	PFIZER JAPAN INC.
1996-12-23	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
G02CB03	GENITO URINARY SYSTEM AND SEX HORMONES › OTHER GYNECOLOGICALS › OTHER GYNECOLOGICALS › Prolactine inhibitors
N04BC06	NERVOUS SYSTEM › ANTI-PARKINSON DRUGS › DOPAMINERGIC AGENTS › Dopamine agonists

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
Cerebrospinal fluid leakage	502.0
Insulin-like growth factor increased	373.8
Blood growth hormone increased	290.7
Pulmonary pain	289.9
Gambling disorder	240.8
Aortic valve incompetence	235.5
Cardiac valve disease	197.1
Amyloid arthropathy	191.1
Pneumocephalus	175.8
Mitral valve incompetence	162.1
Needle issue	155.2
Insulin-like growth factor decreased	148.4

Chemical structure

• Molecular formula: C₂₆H₃₇N₅O₂
• Molecular weight: 451.62 g/mol
• CAS number: —
• InChIKey: KORNTPPJEAJQIU-KJXAQDMKSA-N
• PubChem CID: 54746

CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(CC=C)C1

Frequently asked questions

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

What is Cabergoline used for?

DrugCentral lists the following indications for Cabergoline: Hyperprolactinemia and Prevention of ovarian hyperstimulation syndrome.

How does Cabergoline work?

Its molecular targets in DrugCentral include DRD2 (agonist), DRD3 (agonist), HTR2B and HTR2A (agonist).

When was Cabergoline first approved?

Cabergoline was first approved by the FDA in 1996.

What drug class does Cabergoline belong to?

Cabergoline is in the Ergot Derivative class.

What is the chemical formula of Cabergoline?

Cabergoline has the molecular formula C26H37N5O2 and a molecular weight of 451.62 g/mol.

Sources

• DrugCentral drug card 460 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201087 — compound record and bioactivity
• PubChem CID 54746 — chemical identifiers
• DrugBank DB00248 — drug record
• FDA UNII LL60K9J05T — substance identity
• DailyMed: FDA labels for Cabergoline — current prescribing information (label search)
• UniProt P14416 (DRD2) — target protein
• UniProt P35462 (DRD3) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P28221 (HTR1D) — target protein
• UniProt P08913 (ADRA2A) — 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.