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| Trade names | Cetrotide, others |
| AHFS/Drugs.com | Monograph |
| Routes of administration | Subcutaneous injection |
| Drug class | GnRH analogue;GnRH antagonist;Antigonadotropin |
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| Pharmacokinetic data | |
| Bioavailability | 85% |
| Protein binding | 86% |
| Eliminationhalf-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) |
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| ECHA InfoCard | 100.212.148 |
| Chemical and physical data | |
| Formula | C70H92ClN17O14 |
| Molar mass | 1431.06 g·mol−1 |
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Cetrorelix (INNTooltip International Nonproprietary Name,BANTooltip British Approved Name), orcetrorelix acetate (USANTooltip United States Adopted Name,JANTooltip Japanese Accepted Name), sold under the brand nameCetrotide, is an injectablegonadotropin-releasing hormone (GnRH)antagonist. Asyntheticdecapeptide, 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 ofluteinizing hormone (LH) andfollicle-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; ifhuman 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 ageneric medication.[3][4]
Cetrorelix is marketed byMerck Serono for use inin-vitro fertilization in all countries except Japan, where it is marketed byShionogi andNippon Kayaku.[5] 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 thehCG administration by the treating physician. As an alternative to the GnRH antagonist, also aGnRH agonist could be given, but agonist have to be started earlier to overcome the agonistic effect. Cetrorelix can be mixed withfollitropin alpha without compromising their reported safety and efficacy.[6]
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.[citation needed]
Cetrorelix was under development for the treatment ofbenign prostatic hyperplasia,premenopausalbreast cancer,endometriosis,ovarian cancer,prostate cancer, anduterine fibroids, but development for these indications was discontinued.[7]
Cetrorelix was shown to prevent development of reproductive defects induced by injection ofanti-Müllerian hormone in a mouse model ofpolycystic ovary syndrome (PCOS), suggesting its potential as PCOS therapeutic.[8]
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 inhigh density lipoproteins (HDLs) were seen. HDLs are responsible for removing cholesterol from the blood and higher amounts are correlated with increased cardiovascular health.[9]
