Cetrorelix

Cetrorelix
Clinical data
Trade names	Cetrotide, others
AHFS/Drugs.com	Monograph
Routes of; administration	Subcutaneous injection
Drug class	GnRH analogue; GnRH antagonist; Antigonadotropin
ATC code	H01CC02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	85%
Protein binding	86%
Elimination half-life	62.8 hours / 3 mg single dose; 5 hours / 0.25 mg single dose; 20.6 hours / 0.25 mg multiple doses
Excretion	feces (5% to 10% as unchanged drug and metabolites); urine (2% to 4% as unchanged drug)
Identifiers
	IUPAC name Acetyl-D-3-(2′-naphtyl)-alanine-D-4-chlorophenylalanine-D-3-(3′-pyridyl)- alanine-L-serine-L-tyrosine-D-citrulline-L-leucine-L-arginine-L-proline-D-alanine-amide;
CAS Number	120287-85-6 ;
PubChem CID	16130924;
IUPHAR/BPS	1190;
DrugBank	DB00050 ;
ChemSpider	10482082 ;
UNII	OON1HFZ4BA;
KEGG	D07665 ;
ChEBI	CHEBI:59224 ;
ChEMBL	ChEMBL1200490 ;
CompTox Dashboard (EPA)	DTXSID7040996 ;
ECHA InfoCard	100.212.148
Chemical and physical data
Formula	C70H92ClN17O14
Molar mass	1431.06 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O;
	InChI InChI=1S/C70H92ClN17O14/c1-39(2)31-52(61(94)82-51(15-9-28-77-69(73)74)68(101)88-30-10-16-58(88)67(100)79-40(3)59(72)92)83-60(93)50(14-8-29-78-70(75)102)81-63(96)54(34-43-20-25-49(91)26-21-43)86-66(99)57(38-89)87-65(98)56(36-45-11-7-27-76-37-45)85-64(97)55(33-42-18-23-48(71)24-19-42)84-62(95)53(80-41(4)90)35-44-17-22-46-12-5-6-13-47(46)32-44/h5-7,11-13,17-27,32,37,39-40,50-58,89,91H,8-10,14-16,28-31,33-36,38H2,1-4H3,(H2,72,92)(H,79,100)(H,80,90)(H,81,96)(H,82,94)(H,83,93)(H,84,95)(H,85,97)(H,86,99)(H,87,98)(H4,73,74,77)(H3,75,78,102)/t40-,50-,51+,52+,53-,54+,55-,56-,57+,58+/m1/s1 ; Key:SBNPWPIBESPSIF-MHWMIDJBSA-N ;
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Cetrorelix (INNTooltip International Nonproprietary Name, BANTooltip British Approved Name), or cetrorelix acetate (USANTooltip United States Adopted Name, JANTooltip Japanese Accepted Name), sold under the brand name Cetrotide, is an injectable gonadotropin-releasing hormone (GnRH) antagonist. A synthetic decapeptide, it is used in assisted reproduction to inhibit premature luteinizing hormone surges^[2] The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In addition, cetrorelix can be used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection. The duration of the 3 mg single dose is four days; if human chorionic gonadotropin (hCG) is not administered within four days, a daily 0.25 mg dose is started and continued until hCG is administered.

It is available as a generic medication.^[3]^[4]

^ "Cetrorelix RBX (Sun Pharma ANZ Pty Ltd)". Therapeutic Goods Administration (TGA). 13 March 2025. Retrieved 24 March 2025.
^ "Cetrotide 0.25 mg" (PDF). emdserono.com. Archived from the original (PDF) on 5 April 2016. Retrieved 30 January 2016.
^ "2022 First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Archived from the original on 30 June 2023. Retrieved 30 June 2023.
^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.

[1] "Cetrorelix RBX (Sun Pharma ANZ Pty Ltd)". Therapeutic Goods Administration (TGA). 13 March 2025. Retrieved 24 March 2025.

[2] "Cetrotide 0.25 mg" (PDF). emdserono.com. Archived from the original (PDF) on 5 April 2016. Retrieved 30 January 2016.

[3] "2022 First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Archived from the original on 30 June 2023. Retrieved 30 June 2023.

[4] "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.

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