GnRH Analogues
19 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- AbarelixAbarelix is a synthetic decapeptide that acts as a gonadotropin‑releasing hormone (GnRH) antagonist. It was investigated for rapid hormonal castration in advanced prostate cancer and, in women, for conditions such as endometriosis and hormone‑dependent breast cancer. Although it received FDA approval in 2004, development was later discontinued and the drug is now listed as withdrawn.
- AcylineAcyline is a synthetic peptide that acts as a gonadotropin‑releasing hormone (GnRH) antagonist. It is being investigated for its ability to suppress the pituitary release of luteinising hormone (LH) and follicle‑stimulating hormone (FSH), thereby lowering circulating sex steroids such as testosterone. Studies in dogs and healthy men have shown that a single subcutaneous dose can produce reversible hormonal suppression for several days, and an oral formulation using a GIPET enhancer has demonstrated short‑term suppression of testosterone in men.
- BuserelinBuserelin is a synthetic nonapeptide analogue of gonadotropin‑releasing hormone (GnRH) that functions as a GnRH agonist. It is an approved prescription drug administered by implant, subcutaneous injection, intranasal spray or intravenous infusion. By creating a reversible hypogonadal state, it is used in hormone‑dependent conditions such as prostate and premenopausal breast cancers, endometriosis, central precocious puberty, and as a pretreatment in assisted reproduction. Veterinary applications include induction of estrus in bitches.
- CetrorelixCetrorelix is a synthetic decapeptide GnRH antagonist approved for use in assisted reproductive technology. It is administered by subcutaneous injection to achieve rapid, dose‑dependent suppression of luteinising hormone (LH) and follicle‑stimulating hormone (FSH), thereby preventing the ovarian hormonal surge that can complicate controlled ovarian stimulation. Beyond IVF, cetrorelix is being investigated for hormone‑dependent conditions such as uterine fibroids and advanced prostate cancer.
- DegarelixDegarelix is a synthetic decapeptide GnRH antagonist approved for androgen deprivation therapy (ADT) in men with prostate cancer. Delivered by subcutaneous injection, it rapidly suppresses luteinising hormone and testosterone without the initial surge seen with GnRH agonists. It is used to achieve castration‑level testosterone as part of definitive or palliative treatment strategies.
- DeslorelinDeslorelin is a synthetic GnRH super‑agonist peptide approved for veterinary use. Delivered mainly as a subcutaneous slow‑release implant, it is employed to suppress fertility in dogs and cats, postpone puberty in pre‑pubertal animals, and to induce or synchronize estrus for breeding programs. Its high potency allows long‑acting hormonal control with a single administration.
- DetirelixDetirelix is a synthetic decapeptide that acts as a gonadotropin‑releasing hormone (GnRH) antagonist. In research settings it has been used to suppress pituitary secretion of luteinising hormone (LH) and follicle‑stimulating hormone (FSH), thereby reducing downstream sex steroids such as estradiol and testosterone. Studies in women, post‑menopausal volunteers, free‑ranging African elephants and sheep have demonstrated its ability to block gonadotropin release, inhibit follicular development and prevent ovulation, with effects that reverse after the drug is cleared.
- GanirelixGanirelix is a prescription GnRH‑antagonist peptide administered subcutaneously. It is approved for use in assisted reproductive technology to rapidly suppress the pituitary release of LH and FSH during controlled ovarian hyperstimulation, preventing an untimely LH surge. The drug’s quick onset and short protocol have also prompted investigation for hormone‑dependent cancers and other reproductive disorders.
- GonadorelinGonadorelin is a synthetic analogue of the natural gonadotropin‑releasing hormone (GnRH) peptide. It is approved for prescription use and is administered via intranasal, intravenous, or subcutaneous routes. The compound has been investigated as one of many hormonal approaches for premenstrual syndrome (PMS), but the systematic review cited does not provide specific efficacy or safety data for this indication.
- GoserelinGoserelin is a synthetic decapeptide analogue of gonadotropin‑releasing hormone (GnRH) used to suppress ovarian estrogen production in premenopausal women with hormone‑receptor‑positive breast cancer. By creating a medically induced menopause, it enables the use of aromatase inhibitors, fulvestrant, or CDK4/6 inhibitors that otherwise require low estrogen levels. Goserelin is administered as a subcutaneous depot injection and is approved for clinical use in several countries.
- HistrelinHistrelin is a synthetic non‑peptide analogue of gonadotropin‑releasing hormone (GnRH) formulated as a subcutaneous, diffusion‑controlled implant. It is approved for the treatment of advanced prostate cancer and for central precocious puberty (CPP) in children. The implant releases histrelin continuously, providing long‑term suppression of the hypothalamic‑pituitary‑gonadal axis, which lowers testosterone in men and halts pubertal development in youngsters.
- IturelixIturelix (also known as antide or D‑63153) is an investigational decapeptide GnRH antagonist studied for use in assisted reproduction. In early‑phase clinical trials it was given subcutaneously to women undergoing IVF/ICSI to suppress premature luteinising hormone (LH) surges and to optimise hormonal conditions for embryo implantation.
- LeuprolideLeuprolide is a synthetic GnRH agonist approved for injectable use. It is employed to relieve endometriosis‑related pelvic pain and as androgen‑deprivation therapy for prostate cancer by suppressing ovarian estrogen or testicular testosterone production. Formulations include intramuscular, subcutaneous depot injections and subcutaneous implants.
- NafarelinNafarelin is a synthetic decapeptide analogue of gonadotropin‑releasing hormone (GnRH) that acts as a potent GnRH agonist. It is administered as a nasal spray and is approved in several countries for conditions that benefit from profound suppression of sex steroids, such as endometriosis, advanced prostate cancer, and central precocious puberty. Clinicians also use it off‑label to facilitate assisted reproductive technology cycles, to shrink uterine fibroids (leiomyomas), and to manage hormone‑sensitive disorders where temporary hypo‑estrogenic states are desired.
- OzarelixOzarelix is an investigational decapeptide that acts as a gonadotropin‑releasing hormone (GnRH) antagonist. Developed for subcutaneous administration, it is being explored for its ability to block GnRH receptors and thereby suppress downstream reproductive hormone signaling. Current research focuses on its physicochemical properties, especially its strong binding to anionic polymers and propensity to form nanostructured aggregates that could be harnessed for drug‑delivery applications.
- RamorelixRamorelix is an investigational gonadotropin‑releasing hormone (GnRH) antagonist studied in rats for its ability to suppress ovarian hormone production and to affect hormone‑dependent mammary tumours. The compound is delivered in biodegradable slow‑release microparticles or implants and is being explored as a research tool for cancer prevention and treatment, not as an approved therapy.
- TeverelixTeverelix is an investigational gonadotropin‑releasing hormone (GnRH) antagonist being evaluated for androgen‑deprivation therapy in hormone‑sensitive advanced prostate cancer. Administered as an injectable peptide, it aims to rapidly suppress luteinizing hormone (LH), follicle‑stimulating hormone (FSH) and downstream testosterone production.
- TriptorelinTriptorelin is a synthetic decapeptide GnRH agonist approved for prescription use. By suppressing the pituitary release of luteinising hormone and follicle‑stimulating hormone, it creates a hypo‑gonadal state that lowers circulating estrogen or testosterone. It is employed as part of ovarian suppression in premenopausal breast‑cancer patients, to achieve medical castration in advanced prostate cancer, and to induce hypo‑estrogenism for endometriosis symptom control.
- Zoptarelin doxorubicinZoptarelin doxorubicin (AEZS‑108) is an investigational peptide‑drug conjugate that links the chemotherapy agent doxorubicin to a luteinizing hormone‑releasing hormone (LHRH) agonist. Designed to home in on tumor cells that express LHRH receptors, it is being evaluated for ovarian, endometrial, prostate and other solid cancers. Early‑phase clinical trials suggest modest antitumor activity with a toxicity profile that appears milder than free doxorubicin, but the compound remains experimental and is not approved for routine use.