Cetrorelix

Gonadotropin Releasing Hormone Receptor Antagonist — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS

Key facts

Cetrorelix is a drug in the Gonadotropin Releasing Hormone Receptor Antagonist class catalogued in DrugCentral. It was first approved by the EMA in 1999. Its mechanism of action is classified as Gonadotropin Releasing Hormone Receptor Antagonists. DrugCentral lists 2 molecular targets, including GNRHR and LHCGR. Recorded indications include Premature Luteinizing Hormone Surges, Prevention of premature ovulation and Prevention of premature ovulation during controlled ovarian stimulation.

• Drug class: Gonadotropin Releasing Hormone Receptor Antagonist.
• Mechanism of action: Gonadotropin Releasing Hormone Receptor Antagonists.
• Molecular targets: GNRHR and LHCGR (2 listed in DrugCentral).
• Indications: Premature Luteinizing Hormone Surges, Prevention of premature ovulation and Prevention of premature ovulation during controlled ovarian stimulation.
• ATC code: H01CC02 (Anti-gonadotropin-releasing hormones).
• Molecular formula: C70H92ClN17O14; molecular weight 1431.06 g/mol.

Indications & contraindications

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

Indications (3)

• Premature Luteinizing Hormone Surges
• Prevention of premature ovulation
• Prevention of premature ovulation during controlled ovarian stimulation

Contraindications (3)

• Acute nephropathy
• Breastfeeding (mother)
• Pregnancy, function

Mechanism & targets

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

Molecular targets (2)

Target	Gene	Action	Activity
Gonadotropin-releasing hormone receptor	GNRHR	antagonist	Ki 8.80
Lutropin-choriogonadotropic hormone receptor	LHCGR	unknown	—

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2006-04-20	PMDA	—	NIPPON KAYAKU CO., LTD.
2000-08-11	FDA	—	EMD SERONO INC
1999-04-12	EMA	—	MERCK EUROPE B.V.

ATC classification

ATC code	Therapeutic hierarchy
H01CC02	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Anti-gonadotropin-releasing hormones

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
Ovarian hyperstimulation syndrome	969.8
Premature ovulation	246.7
Blood luteinising hormone increased	131.2
Abortion spontaneous	98.2
Ascites	83.3
Blood oestrogen increased	82.2
Drug level decreased	65.8

Chemical structure

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

• Molecular formula: C₇₀H₉₂ClN₁₇O₁₄
• Molecular weight: 1431.06 g/mol
• CAS number: 120287-85-6
• InChIKey: SBNPWPIBESPSIF-MHWMIDJBSA-N
• PubChem CID: 25074887

CC(C)C[C@H](NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](CC1=CC=C(O)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=CC=C2C=CC=CC2=C1)NC(C)=O)C(=O)N[C@@H](CCCNC(N)=N)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 Cetrorelix used for?

DrugCentral lists the following indications for Cetrorelix: Premature Luteinizing Hormone Surges, Prevention of premature ovulation and Prevention of premature ovulation during controlled ovarian stimulation.

How does Cetrorelix work?

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

When was Cetrorelix first approved?

Cetrorelix was first approved by the EMA in 1999.

What drug class does Cetrorelix belong to?

Cetrorelix is in the Gonadotropin Releasing Hormone Receptor Antagonist class.

What is the chemical formula of Cetrorelix?

Cetrorelix has the molecular formula C70H92ClN17O14 and a molecular weight of 1431.06 g/mol.

Sources

• DrugCentral drug card 583 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200490 — compound record and bioactivity
• PubChem CID 25074887 — chemical identifiers
• DrugBank DB00050 — drug record
• FDA UNII OON1HFZ4BA — substance identity
• DailyMed: FDA labels for Cetrorelix — current prescribing information (label search)
• UniProt P30968 (GNRHR) — target protein
• UniProt P22888 (LHCGR) — 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.