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 syntheticdecapeptide, it is used in assisted reproduction to inhibit premature luteinizing hormone surges[1] 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[citation needed] and breast (in pre-/perimenopausal women)[citation needed] and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning).[citation needed] 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.
Cetrorelix is marketed by Merck Serono for use in in-vitro fertilization in all countries except Japan, where it is marketed by Shionogi and Nippon Kayaku.[4] Aeterna Zentaris receives royalties on these sales and retains rights to develop cetrorelix for other indications. In IVF use it is injected daily after follicle stimulation has been initiated and evidence of follicle maturation is approaching; given daily it prevents an endogenous LH surge that would trigger an untimely ovulation prior to the hCG administration by the treating physician. As an alternative to the GnRH antagonist, also a GnRH agonist could be given, but agonist have to be started earlier to overcome the agonistic effect. Cetrorelix can be mixed with follitropin alpha without compromising their reported safety and efficacy.[5]
Contraindicationsedit
The use of cetrorelix is contraindicated in severe renal impairment. It is not intended for women aged 65 years or older. Use in women with severe allergic conditions is not recommended. Use with caution in women with active allergies or history of allergies.
A study published in Nature Medicine found a link between hormonal imbalance in the womb and Polycystic ovary syndrome (PCOS), specifically prenatal exposure to anti-Müllerian hormone. [7] For the study, the researchers injected pregnant mice with AMH so that they had a higher than normal concentration of the hormone. Indeed, they gave birth to daughters who later developed PCOS-like tendencies. These included problems with fertility, delayed puberty, and erratic ovulation. To reverse it, the researchers dosed the polycystic mice with cetrorelix, which made the symptoms to go away. These experiments should be confirmed in humans, but it could be the first step in understanding the relationship between the polycystic ovary and the anti-Müllerian hormone.
In another study, over a period of 3 weeks, daily injections of cetrorelix were administered to 12 men in order to suppress testosterone levels. Testosterone levels were significantly suppressed as compared to a control group. During this time of suppression, increases in high density lipoproteins(HDLs) were seen. HDLs are responsible for removing cholesterol from the blood and higher amounts are correlated with increased cardiovascular health.[8]
Referencesedit
^(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. 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. from the original on 29 June 2023. Retrieved 29 June 2023.
^Tata B, Mimouni NE, Barbotin AL, Malone SA, Loyens A, Pigny P, et al. (June 2018). "Elevated prenatal anti-Müllerian hormone reprograms the fetus and induces polycystic ovary syndrome in adulthood". Nature Medicine. 24 (6): 834–846. doi:10.1038/s41591-018-0035-5. PMC6098696. PMID 29760445.
^von Eckardstein A (1997). "Suppression of Endogenous Testosterone in Young Men Increases Serum Levels of High Density Lipoprotein Subclass Lipoprotein A-I and Lipoprotein(a)". Journal of Clinical Endocrinology. 82 (10): 3367.
External linksedit
"Cetrorelix". Drug Information Portal. U.S. National Library of Medicine.
"Cetrorelix acetate". Drug Information Portal. U.S. National Library of Medicine.
cetrorelix, inntooltip, international, nonproprietary, name, bantooltip, british, approved, name, cetrorelix, acetate, usantooltip, united, states, adopted, name, jantooltip, japanese, accepted, name, sold, under, brand, name, cetrotide, injectable, gonadotrop. 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 1 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 citation needed and breast in pre perimenopausal women citation needed and some benign gynaecological disorders endometriosis uterine fibroids and endometrial thinning citation needed 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 CetrorelixClinical dataTrade namesCetrotide othersAHFS Drugs comMonographRoutes ofadministrationSubcutaneous injectionDrug classGnRH analogue GnRH antagonist AntigonadotropinATC codeH01CC02 WHO Legal statusLegal statusUS only EU Rx onlyPharmacokinetic dataBioavailability85 Protein binding86 Elimination half life62 8 hours 3 mg single dose 5 hours 0 25 mg single dose 20 6 hours 0 25 mg multiple dosesExcretionfeces 5 to 10 as unchanged drug and metabolites urine 2 to 4 as unchanged drug IdentifiersIUPAC 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 amideCAS Number120287 85 6 YPubChem CID16130924IUPHAR BPS1190DrugBankDB00050 YChemSpider10482082 YUNIIOON1HFZ4BAKEGGD07665 YChEBICHEBI 59224 YChEMBLChEMBL1200490 NCompTox Dashboard EPA DTXSID7040996ECHA InfoCard100 212 148Chemical and physical dataFormulaC 70H 92Cl N 17O 14Molar mass1431 06 g mol 13D model JSmol Interactive imageSMILES 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 OInChI 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 YKey SBNPWPIBESPSIF MHWMIDJBSA N Y N Y what is this verify It is available as a generic medication 2 3 Contents 1 Medical uses 2 Contraindications 3 Research 4 References 5 External linksMedical uses editCetrorelix is marketed by Merck Serono for use in in vitro fertilization in all countries except Japan where it is marketed by Shionogi and Nippon Kayaku 4 Aeterna Zentaris receives royalties on these sales and retains rights to develop cetrorelix for other indications In IVF use it is injected daily after follicle stimulation has been initiated and evidence of follicle maturation is approaching given daily it prevents an endogenous LH surge that would trigger an untimely ovulation prior to the hCG administration by the treating physician As an alternative to the GnRH antagonist also a GnRH agonist could be given but agonist have to be started earlier to overcome the agonistic effect Cetrorelix can be mixed with follitropin alpha without compromising their reported safety and efficacy 5 Contraindications editThe use of cetrorelix is contraindicated in severe renal impairment It is not intended for women aged 65 years or older Use in women with severe allergic conditions is not recommended Use with caution in women with active allergies or history of allergies Research editCetrorelix was under development for the treatment of benign prostatic hyperplasia premenopausal breast cancer endometriosis ovarian cancer prostate cancer and uterine fibroids but development for these indications was discontinued 6 A study published in Nature Medicine found a link between hormonal imbalance in the womb and Polycystic ovary syndrome PCOS specifically prenatal exposure to anti Mullerian hormone 7 For the study the researchers injected pregnant mice with AMH so that they had a higher than normal concentration of the hormone Indeed they gave birth to daughters who later developed PCOS like tendencies These included problems with fertility delayed puberty and erratic ovulation To reverse it the researchers dosed the polycystic mice with cetrorelix which made the symptoms to go away These experiments should be confirmed in humans but it could be the first step in understanding the relationship between the polycystic ovary and the anti Mullerian hormone In another study over a period of 3 weeks daily injections of cetrorelix were administered to 12 men in order to suppress testosterone levels Testosterone levels were significantly suppressed as compared to a control group During this time of suppression increases in high density lipoproteins HDLs were seen HDLs are responsible for removing cholesterol from the blood and higher amounts are correlated with increased cardiovascular health 8 References edit 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 Aeternia Zentaris product page Lin YH Wen YR Chang Y Seow KM Hsieh BC Hwang JL Tzeng CR June 2010 Safety and efficacy of mixing cetrorelix with follitropin alfa a randomized study Fertility and Sterility 94 1 179 83 doi 10 1016 j fertnstert 2009 02 062 PMID 19339001 Cetrorelix AdisInsight Tata B Mimouni NE Barbotin AL Malone SA Loyens A Pigny P et al June 2018 Elevated prenatal anti Mullerian hormone reprograms the fetus and induces polycystic ovary syndrome in adulthood Nature Medicine 24 6 834 846 doi 10 1038 s41591 018 0035 5 PMC 6098696 PMID 29760445 von Eckardstein A 1997 Suppression of Endogenous Testosterone in Young Men Increases Serum Levels of High Density Lipoprotein Subclass Lipoprotein A I and Lipoprotein a Journal of Clinical Endocrinology 82 10 3367 External links edit Cetrorelix Drug Information Portal U S National Library of Medicine Cetrorelix acetate Drug Information Portal U S National Library of Medicine Portal nbsp Medicine Retrieved from https en wikipedia org w index php title Cetrorelix amp oldid 1190948122, wikipedia, wiki, book, books, library,
