Cetrorelix

Summary

Cetrorelix (CHEMBL1200490) is an approved protein GnRH antagonist (ATC H01CC02) targeting GNRHR; indicated across 5 conditions including benign prostatic hyperplasia and infertility disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: H01CC02
• Targets: 1 (GNRHR)
• Indications: 5 conditions
• Clinical trials: 39
• Chemistry: 1431 Da · C70H92ClN17O14

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1200490
Name	Cetrorelix
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	25074887
ChEBI	CHEBI:59224
ATC	H01CC02
Molecular formula	C70H92ClN17O14
Molecular weight	1431
InChIKey	SBNPWPIBESPSIF-MHWMIDJBSA-N

SMILES: C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCNC(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC3=CN=CC=C3)NC(=O)[C@@H](CC4=CC=C(C=C4)Cl)NC(=O)[C@@H](CC5=CC6=CC=CC=C6C=C5)NC(=O)C

IUPAC name: (2S)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(carbamoylamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-N-[(2R)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide

ChEBI definition: A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N5-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.

Pharmacological roles (ChEBI): GnRH antagonist, antineoplastic agent.

Also known as: Cetrorelix, Cetrotide, CETRORELIX, Cetrorelix (Acetate), cetrorelix

Parent form; salt/anhydrous children: CHEMBL2103735

Patent coverage: 3,818 distinct patent families (16,775 SureChEMBL compound mentions), from 7 matched compound structure(s). One matched structure accounts for 16,725 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GNRHR	GnRH1 receptor	Antagonist	8.7	0.1%	P30968

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Gonadotropin-releasing hormone receptor, D(1A) dopamine receptor, Mu-type opioid receptor, Mas-related G-protein coupled receptor member X2.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GNRHR	9.87	Kd	0.14	nM	CHEMBL_ACT_22430574
GNRHR	8.9	Kd	1.26	nM	CHEMBL_ACT_1290257
GNRHR	8.38	IC50	4.2	nM	CHEMBL_ACT_1290256
MRGPRX2	6.21	EC50	616.6	nM	CHEMBL_ACT_26241694
MRGPRX2	6.09	EC50	812.8	nM	CHEMBL_ACT_26241810

Target pathways

Aggregated over 1 target gene(s): GNRHR.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Hormone ligand-binding receptors	1	GNRHR
G alpha (q) signalling events	1	GNRHR

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
gonadotropin secretion	1
cellular response to hormone stimulus	1
signal transduction	1
cellular response to gonadotropin-releasing hormone	1

Indications & clinical

Indications

5 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
benign prostatic hyperplasia	3	MONDO:0010811	EFO:0000284
infertility disorder	3	MONDO:0005047	EFO:0000545
ovarian hyperstimulation syndrome	3	MONDO:0011972	MONDO:0011972
rheumatoid arthritis	2	MONDO:0008383	EFO:0000685
endometriosis	2	MONDO:0005133	EFO:0001065

Clinical trials

Total trials: 39.

Phase distribution

Phase	Trials
Not specified	13
PHASE4	12
PHASE3	5
PHASE2	4
PHASE2/PHASE3	2
PHASE1/PHASE2	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00439829	PHASE4	COMPLETED	Synchronization of Follicle Wave Emergence and Ovarian Stimulation
NCT00505817	PHASE4	COMPLETED	GnRH Agonist and Antagonists in an Oocyte Donation Program
NCT01005784	PHASE4	COMPLETED	Fixed Versus Flexible Gonadotropin-releasing Hormone (GnRH) Antagonist Initiation
NCT01225835	PHASE4	COMPLETED	Progesterone Serum Levels in Subfertile Female Patients Undergoing in Vitro Fertilisation (IVF)
NCT03118830	PHASE4	COMPLETED	Long Protocol and Freeze All Embryos vs Antagonist Protocol With Fresh Embryo Transfer in PCOS Patients Undergoing ICSI
NCT04094467	PHASE4	UNKNOWN	Comparison Between Two Different Protocols in Polycystic Ovary Symdrome Women Undergoing Intra-cytoplasmic Injection
NCT04671966	PHASE4	UNKNOWN	Sex Differences in Myocardial Steatosis Induced Left Ventricular Dysfunction
NCT04724343	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on IVF/ICSI Outcomes.
NCT04724486	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on Oocyte Morphology During IVF/ICSI
NCT04727671	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on IVF/ICSI Outcomes in Polycystic Ovary Syndrome Patients.
NCT04727684	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on Oocyte Morphology in Polycystic Ovary Syndrome Patients During IVF/ICSI
NCT04993924	PHASE4	UNKNOWN	GnRH Antagonist Pre-treatment in the Early Follicular Phase for Resolution of a Baseline Functional Ovarian Cyst
NCT00663858	PHASE3	COMPLETED	Cetrorelix Pamoate in Patients With Symptomatic Benign Prostatic Hypertrophy (BPH)
NCT00670306	PHASE3	COMPLETED	Cetrorelix Pamoate IM Regimens in Patients With Symptomatic Benign Prostatic Hyperplasia (BPH)
NCT01709942	PHASE3	COMPLETED	Use of Degarelix in Controlled Ovarian Hyperstimulation (COH) Protocol for Women With PoliCystic Ovarian Syndrome (PCOS)
NCT02333253	PHASE3	COMPLETED	Delayed Start Versus Conventional Antagonist Protocol in Poor Responders Pretreated by Estradiol in Luteal Phase
NCT02823080	PHASE2/PHASE3	UNKNOWN	Outcome of Cetrotide Therapy for Management of Women at High-risk of Ovarian Hyperstimulation Syndrome
NCT05951400	PHASE2/PHASE3	COMPLETED	Progesterone Primed Protocol Versus GnRH Antagonist in With PCO Undergoing ICSI
NCT06868576	PHASE3	COMPLETED	PPOS Protocol Versus GnRH Anatagonist for Expected Normal Responder Patients Undergoing ART : a Randomized Clinical Trial
NCT00244452	PHASE2	COMPLETED	A Multinational, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Investigate the Efficacy, Safety and Duration of Effect of a Single Administration of Various Doses of Cetrorelix SR in Subjects With Histologically Confirmed Endometriosis
NCT00667758	PHASE2	COMPLETED	Gonadotropin-Releasing Hormone (GnRH)-Antagonist Therapy in Rheumatoid Arthritis
NCT01109888	PHASE1/PHASE2	WITHDRAWN	Administration of Increased Dose of GnRH Antagonist for Coasting for Decreasing the Risk for Ovarian Hyperstimulation Syndrome( OHSS)
NCT02784457	PHASE2	COMPLETED	Gonadotropin Releasing Hormone Antagonist in Treatment of Early-onset Severe Ovarian Hyperstimulation Syndrome
NCT05738382	PHASE2	UNKNOWN	Efficacy and Safety of BG2109 During Controlled Ovarian Hyperstimulation in Female Subjects Undergoing ART Procedures
NCT06608186	PHASE1/PHASE2	COMPLETED	Can Drospirenone be Used to Prevent LH Surge in Controlled Ovarian Stimulation in PCOS?!
NCT02042196	EARLY_PHASE1	COMPLETED	Sex Hormones and Atherosclerosis Prevention in Perimenopausal Women
NCT06378268	Not specified	ACTIVE_NOT_RECRUITING	PPOS vs GnRH Antagonist in Ovarian Stimulation (ProGanOS Study)
NCT00628121	Not specified	COMPLETED	Clinical Pharmacological Study of GnRH Antagonist, Cetrorelix for Healthy Female Volunteer
NCT01109654	Not specified	COMPLETED	An Observational Study of Cetrotide® Gonadotropin-releasing Hormone Antagonist (GnRH Antagonist) With GONAL-f® in Assisted Reproductive Technologies (ART)
NCT01457703	Not specified	COMPLETED	Reproductive Hormonal Alterations in Obesity
NCT01468441	Not specified	COMPLETED	Ovarian Stimulation Using Recombinant Follicle-stimulating Hormone (FSH) and Gonadotrophin Releasing Hormone (GnRH) Agonist in Alternate Days
NCT01595334	Not specified	UNKNOWN	Study on Influence of Leutinizing Hormone (LH) on Oocyte Maturity
NCT02392520	Not specified	UNKNOWN	Luteal Antagonist Versus Conventional Treatment in Women With Severe Early Ovarian Hyperstimulation Syndrome (OHSS)
NCT02478775	Not specified	COMPLETED	Dysregulation of FSH in Obesity: Functional and Statistical Analysis
NCT03680053	Not specified	TERMINATED	Comparison of the Live Birth Rate Between the PPOS and the GnRH Antagonist Protocol in Patients Undergoing IVF
NCT04308343	Not specified	UNKNOWN	The Aromatase Inhibitor and Gnrh Antagonist Versus Methotrexate for Management of Undisturbed Ectopic Pregnancy
NCT04418908	Not specified	COMPLETED	Estrogen, Diabetes, and Endothelial Function
NCT05112692	Not specified	UNKNOWN	Progestin-primed Ovarian Stimulation Protocol Versus GnRH Antagonist Protocol in Polycystic Ovary Syndrome Patients Undergoing IVF/ICSI Cycles
NCT05751681	Not specified	UNKNOWN	Dydrogesterone-Primed Ovarian Stimulation Protocol Versus Gonadotropin Releasing Hormone Antagonist Protocol in ICSI

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
DEGARELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ELAGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
GANIRELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
RELUGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ABARELIX	ChEMBL	Phase 4 (approved)	GNRHR
GONADORELIN	ChEMBL	Phase 4 (approved)	GNRHR
LEUPROLIDE	ChEMBL	Phase 4 (approved)	GNRHR
LINZAGOLIX	ChEMBL	Phase 4 (approved)	GNRHR
ACYLINE	ChEMBL	Phase 2	GNRHR
SUFUGOLIX	ChEMBL	Phase 2	GNRHR
Belzutifan	PubChem	Approved	GNRHR
Deslorelin	PubChem	Approved	GNRHR
Triptorelin	PubChem	Approved	GNRHR