Accession NumberDB00050  (BTD00115, APRD00686, BIOD00115)
TypeSmall Molecule
GroupsApproved, Investigational

Cetrorelix is a man-made hormone that blocks the effects of Gonadotropin Releasing Hormone (GnRH). GnRH controls another hormone that is called luteinizing hormone (LH), which is the hormone that starts ovulation during the menstrual cycle. When undergoing hormone treatment sometimes premature ovulation can occur, leading to eggs that are not ready for fertilization to be released. Cetrorelix does not allow the premature release of these eggs to occur.

External IDs SB 75
Product Ingredients
IngredientUNIICASInChI KeyDetails
Cetrorelix AcetateXPQ226310Q 145672-81-7KFEFLCOCAHJBEA-ANRVCLKPSA-NDetails
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CetrotidePowder, for solution0.25 mgSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2004-03-03Not applicableCanada
CetrotideInjection, powder, for solution0.25 mgSubcutaneousMerck Serono Europe Limited1999-04-13Not applicableEu
CetrotidePowder, for solution3 mgSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2004-02-252014-10-20Canada
CetrotideKitSubcutaneousEmd Serono2000-08-11Not applicableUs
CetrotideInjection, powder, for solution0.25 mgSubcutaneousMerck Serono Europe Limited1999-04-13Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
CAS number120287-85-6
WeightAverage: 1431.038
Monoisotopic: 1429.669818444
Chemical FormulaC70H92ClN17O14
CC(C)C[[email protected]](NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[[email protected]](CC1=CC=C(O)C=C1)NC(=O)[[email protected]](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=CC=CC=C2C=C1)NC(C)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[[email protected]]1C(=O)N[[email protected]](C)C(N)=O

For the inhibition of premature LH surges in women undergoing controlled ovarian stimulation

Structured Indications Not Available

Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.

Mechanism of action

Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.

TargetKindPharmacological actionActionsOrganismUniProt ID
Lutropin-choriogonadotropic hormone receptorProteinunknownNot AvailableHumanP22888 details
Gonadotropin-releasing hormone receptorProteinyes
HumanP30968 details
Related Articles

Rapidly absorbed following subcutaneous injection. The mean absolute bioavailability following subcutaneous administration to healthy female subjects is 85%.

Volume of distribution
  • 1.16 L/kg
Protein binding



In in vitro studies, cetrorelix was stable against phase I- and phase II-metabolism. Cetrorelix was transformed by peptidases, and the (1-4) peptide was the predominant metabolite.

Route of elimination

Following subcutaneous administration of 10 mg cetrorelix to males and females, only unchanged cetrorelix was detected in urine.

Half life

~62.8 hours

  • 1.28 ml/min·kg [adult healthy female with 3 mg single SC administration]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Drug Interactions No interactions found.
Food InteractionsNot Available
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesH01CC02 — Cetrorelix
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (221 KB)
MSDSDownload (35.2 KB)
Clinical Trials
Clinical Trials
0Active Not RecruitingBasic ScienceAging / Menopause1
1, 2WithdrawnNot AvailableAdministration of Increased Dose of GnRH Antagonist for Coasting for Decreasing the Risk for Ovarian Hyperstimulation Syndrome( OHSS)1
2CompletedTreatmentAssisted Reproduction1
2CompletedTreatmentRheumatoid Arthritis1
2TerminatedTreatmentInfertilities / Ovulation induction therapy1
2, 3Active Not RecruitingTreatmentInfertilities1
3CompletedTreatmentBenign Prostatic Hypertrophy (BPH)1
3CompletedTreatmentEffects of Gonadotropin / Oocyte Maturation / Ovarian Hyperstimulation Syndrome1
3CompletedTreatmentInfertilities / OHSS / Polycystic Ovarian Syndrome1
3CompletedTreatmentOther Complications Associated With Artificial Fertilization1
3CompletedTreatmentPolycystic Ovarian Syndrome1
3RecruitingTreatmentInfertilities / Polycystic Ovaries Syndrome1
3TerminatedTreatmentBenign Prostatic Hypertrophy (BPH)1
3Unknown StatusScreeningEmbryo's Genetic and Chromosomal Quality1
4CompletedNot AvailableEffect of Two Protocols of Ovarian Stimulation on Oocyte Quality1
4CompletedNot AvailableLeiomyomas1
4CompletedTreatmentInfertile Women Undergoing Assisted Reproductive Technology (ART)1
4Not Yet RecruitingTreatmentInVitro Fertilization1
4Not Yet RecruitingTreatmentInfertilities1
4RecruitingSupportive CareAssisted Reproductive Technology therapy / Infertilities1
4TerminatedTreatmentAssisted Reproductive Technology therapy / Intracytoplasmic Sperm Injection1
4Unknown StatusTreatmentAneuploidy / Blastocyst Disintegration / Chemical Pregnancy / Complication of Implant / Embryo/Fetus Death1
4Unknown StatusTreatmentPoor Responders Undergoing IVF1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableInfertilities2
Not AvailableCompletedTreatmentFertility1
Not AvailableCompletedTreatmentInfertilities3
Not AvailableCompletedTreatmentPremenopause1
Not AvailableNot Yet RecruitingTreatmentOvarian Hyperstimulation Syndrome1
Not AvailableUnknown StatusTreatmentComplications Associated With Artificial Fertilization / Female Infertility Due to Nonimplantation of Ovum1
Not AvailableUnknown StatusTreatmentInfertilities1
  • Emd serono inc
Dosage forms
Injection, powder, for solutionSubcutaneous0.25 mg
Powder, for solutionSubcutaneous0.25 mg
Powder, for solutionSubcutaneous3 mg
Unit descriptionCostUnit
Cetrotide 3 mg kit689.92USD kit
Cetrotide 0.25 mg kit137.99USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2115943 No2003-08-052014-02-18Canada
US5198533 No1993-10-242010-10-24Us
US6319192 No1999-04-232019-04-23Us
Experimental PropertiesNot Available
Predicted Properties
Water Solubility0.00694 mg/mLALOGPS
pKa (Strongest Acidic)9.49ChemAxon
pKa (Strongest Basic)11.11ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count18ChemAxon
Hydrogen Donor Count17ChemAxon
Polar Surface Area495.67 Å2ChemAxon
Rotatable Bond Count38ChemAxon
Refractivity384.16 m3·mol-1ChemAxon
Polarizability148.09 Å3ChemAxon
Number of Rings6ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Human Intestinal Absorption+0.913
Blood Brain Barrier-0.9647
Caco-2 permeable-0.748
P-glycoprotein substrateSubstrate0.8796
P-glycoprotein inhibitor INon-inhibitor0.8235
P-glycoprotein inhibitor IIInhibitor0.6194
Renal organic cation transporterNon-inhibitor0.6856
CYP450 2C9 substrateNon-substrate0.7609
CYP450 2D6 substrateNon-substrate0.7938
CYP450 3A4 substrateSubstrate0.6358
CYP450 1A2 substrateNon-inhibitor0.7491
CYP450 2C9 inhibitorNon-inhibitor0.6987
CYP450 2D6 inhibitorNon-inhibitor0.8339
CYP450 2C19 inhibitorNon-inhibitor0.7056
CYP450 3A4 inhibitorInhibitor0.6531
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9001
Ames testNon AMES toxic0.6327
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7014 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7601
hERG inhibition (predictor II)Inhibitor0.649
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Mass Spec (NIST)Not Available
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
DescriptionThis compound belongs to the class of chemical entities known as polypeptides. These are peptides containing ten or more amino acid residues.
KingdomChemical entities
Super ClassOrganic compounds
ClassOrganic Polymers
Sub ClassPolypeptides
Direct ParentPolypeptides
Alternative ParentsPeptides / Tyrosine and derivatives / Phenylalanine and derivatives / Leucine and derivatives / N-acyl-alpha amino acids and derivatives / Proline and derivatives / Serine and derivatives / Alpha amino acid amides / Alanine and derivatives / Naphthalenes
SubstituentsPolypeptide / Alpha peptide / Tyrosine or derivatives / Phenylalanine or derivatives / Leucine or derivatives / Proline or derivatives / N-acyl-alpha amino acid or derivatives / Alpha-amino acid amide / Serine or derivatives / Alanine or derivatives
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptorsoligopeptide (CHEBI:59224 )


Pharmacological action
General Function:
Luteinizing hormone receptor activity
Specific Function:
Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
Gene Name:
Uniprot ID:
Molecular Weight:
78642.01 Da
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Ascoli M, Fanelli F, Segaloff DL: The lutropin/choriogonadotropin receptor, a 2002 perspective. Endocr Rev. 2002 Apr;23(2):141-74. [PubMed:11943741 ]
Pharmacological action
General Function:
Peptide binding
Specific Function:
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
Gene Name:
Uniprot ID:
Molecular Weight:
37730.355 Da
  1. Volker P, Grundker C, Schmidt O, Schulz KD, Emons G: Expression of receptors for luteinizing hormone-releasing hormone in human ovarian and endometrial cancers: frequency, autoregulation, and correlation with direct antiproliferative activity of luteinizing hormone-releasing hormone analogues. Am J Obstet Gynecol. 2002 Feb;186(2):171-9. [PubMed:11854630 ]
  2. Zapatero-Caballero H, Sanchez-Franco F, Guerra-Perez N, Fernandez-Mendez C, Fernandez-Vazquez G: Gonadotropin-releasing hormone receptor gene expression during pubertal development of male rats. Biol Reprod. 2003 May;68(5):1764-70. Epub 2002 Dec 11. [PubMed:12606421 ]
  3. Zapatero-Caballero H, Sanchez-Franco F, Fernandez-Mendez C, Garcia-San Frutos M, Botella-Cubells LM, Fernandez-Vazquez G: Gonadotropin-releasing hormone receptor gene expression during pubertal development of female rats. Biol Reprod. 2004 Feb;70(2):348-55. Epub 2003 Oct 15. [PubMed:14561652 ]
  4. Roth C, Hegemann F, Hildebrandt J, Balzer I, Witt A, Wuttke W, Jarry H: Pituitary and gonadal effects of GnRH (gonadotropin releasing hormone) analogues in two peripubertal female rat models. Pediatr Res. 2004 Jan;55(1):126-33. Epub 2003 Nov 6. [PubMed:14605254 ]
  5. Castellon E, Clementi M, Hitschfeld C, Sanchez C, Benitez D, Saenz L, Contreras H, Huidobro C: Effect of leuprolide and cetrorelix on cell growth, apoptosis, and GnRH receptor expression in primary cell cultures from human prostate carcinoma. Cancer Invest. 2006 Apr-May;24(3):261-8. [PubMed:16809153 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Drug created on June 13, 2005 07:24 / Updated on July 23, 2017 12:16