Browse Medications by Drug Class: Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists

Written by Amar Lunagaria
Pharm.D • NiHowdy Founder

Reviewed by James Wong
Pharm.D • NiHowdy Founder
Published Jan 15, 2025

What are Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists?
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List of drugs in Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists
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Brief history about Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists?
How do Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists work?
What are Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists used to treat?
Prostate Cancer
GnRH receptor antagonists like degarelix and relugolix are used to treat advanced prostate cancer by rapidly reducing testosterone levels. Testosterone fuels the growth of prostate cancer cells, and these medications help slow disease progression, alleviate symptoms, and improve overall outcomes.
Endometriosis
In individuals with endometriosis, GnRH receptor antagonists like elagolix reduce estrogen levels, alleviating symptoms such as pelvic pain, painful menstruation, and discomfort during intercourse. These medications provide effective symptom control while avoiding the initial symptom flare associated with agonists.
Fertility Treatment
GnRH receptor antagonists are used in assisted reproductive technologies (ART) to prevent premature ovulation during ovarian stimulation. By inhibiting GnRH action, these medications allow for better timing of egg retrieval, improving the success rate of in vitro fertilization (IVF) procedures.
Who should consider Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists medications?
Adults
Adults with hormone-sensitive conditions like prostate cancer, endometriosis, or uterine fibroids benefit significantly from GnRH receptor antagonists. These medications provide rapid symptom relief and are tailored to individual treatment goals, offering a safer and more convenient alternative to traditional therapies.
Children
GnRH receptor antagonists are rarely used in pediatric populations but may be considered for conditions like central precocious puberty, where early hormone suppression is necessary to delay puberty. Treatment is carefully monitored to ensure safety and effectiveness.
Seniors
Seniors with advanced prostate cancer or other hormone-sensitive conditions rely on GnRH receptor antagonists for effective hormone suppression and symptom management. Age-related changes in metabolism and comorbidities require careful monitoring to balance the benefits and risks of therapy.
Are Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists safe?
Can I take Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists during pregnancy?
Are Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists safe to take while lactating?
Are Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists controlled substances?
Side effects of Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonists?
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