classesGonadotropin Releasing Hormone Agonists

Gonadotropin Releasing Hormone Agonists: Uses, most common brand names, and safety information

Medically reviewed by Jamie Winn, PharmD

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Gonadotropin releasing hormone (GnRH) was discovered in 1971 and analogs of GnRH were introduced for medical use in the 1980s. The first GnRH agonist Lupron (leuprolide) was approved for use as androgen deprivation therapy for advanced prostate cancer in 1985. GnRH agonists are all given either as a subcutaneous or intramuscular injection. GnRH agonists, which are sometimes called luteinizing hormone-releasing hormone (LHRH) agonists are used to treat sex hormone-dependent conditions.

The list below includes gonadotropin releasing hormone agonists approved by the U.S. Food and Drug Administration (FDA) and their pricing:

List of Gonadotropin releasing hormone agonists

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Drug name

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Lupron Depot (leuprolide acetate)

Lupron Depot is indicated to treat advanced prostate cancer, endometriosis, and uterine fibroids.

Lupron Depot PED (leuprolide acetate)

Lupron Depot PED is indicated to treat advanced prostate cancer, endometriosis, and uterine fibroids.

Camcevi (leuprolide mesylate)

Camcevi is indicated to treat advanced prostate cancer, endometriosis, and uterine fibroids.

Fensolvi (leuprolide acetate)

Fensolvi is indicated to treat advanced prostate cancer, endometriosis, and uterine fibroids.

Eligard (leuprolide acetate)

Eligard is indicated to treat advanced prostate cancer, endometriosis, and uterine fibroids.

Zoladex (goserelin acetate)

Zoladex is indicated to treat prostate cancer, breast cancer, endometriosis, and endometrial thinning.

Zoladex LA (goserelin acetate)

Zoladex LA is indicated to treat prostate cancer, breast cancer, endometriosis, and endometrial thinning.

Supprelin LA (histrelin)

Supprelin LA is indicated for the palliative treatment of advanced prostate cancer.

Vantas (histrelin)

Vantas is indicated for the palliative treatment of advanced prostate cancer.

Trelstar (triptorelin)

Trelstar is indicated to treat advanced prostate cancer.

Trelstar LA (triptorelin)

Trelstar LA is indicated to treat advanced prostate cancer.

Trelstar Depot (triptorelin)

Trelstar Depot is indicated to treat advanced prostate cancer.

Synarel (nafarelin)

Synarel is indicated to treat endometriosis.

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What are gonadotropin releasing hormone agonists?

Gonadotropin releasing hormone (GnRH) can affect your sex hormone levels, libido, ovulation, and fertility. In children, high GnRH levels can bring on early puberty (precocious puberty), while low levels can delay puberty. GnRH agonists are structurally and functionally similar to GnRH your body naturally produces. They are used in both men and women to prevent the production and secretion of testosterone and estrogen. GnRH agonists are treatment options for conditions that are sex hormone-dependent, such as prostate cancer and endometriosis.

How do gonadotropin releasing hormone agonists work?

Gonadotropin releasing hormone is produced in your hypothalamus and stimulates your pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH). These hormones cause the production and release of testosterone by the testes in males and estrogen by the ovaries and placenta in females.

GnRH agonists are an analog of naturally occurring GnRH. It binds more effectively than the GnRH your body produces. When first starting GnRH agonist therapy, your levels of estrogen or testosterone may temporarily increase which can worsen the symptoms of your condition. With continuous use, GnRH agonists will reduce the amount of testosterone produced by the testes in males. This makes it effective in the treatment of prostate cancer. In females, GnRH agonists decrease ovarian production of estrogen and progesterone.

What conditions are gonadotropin releasing hormone agonists used to treat?

GnRH agonists are a class of medications used in the treatment of:

Endometriosis
Uterine fibroids
Central precocious puberty (early puberty) in pediatric patients
Prostate cancer
Breast cancer
Infertility
Heavy menstrual bleeding
Dysmenorrhea (painful menstruation)
Premenstrual dysphoric disorder (PMDD)
Gender dysphoria
Endometrial cancer

Are gonadotropin releasing hormone agonists safe?

The use of GnRH agonists is relatively safe and effective when taken as prescribed. Before beginning GnRH treatment, tell your doctor if you have any of the following medical conditions:

Heart disease
History of heart attack, stroke, or other cardiovascular risk factors
High cholesterol
Kidney disease
Diabetes
Asthma or lung disease
Osteoporosis or bone loss
History of brain tumors
Mental illness
Seizure disorder

What are the common side effects of gonadotropin releasing hormone agonists?

The adverse effects you experience from GnRH agonists will depend on several factors including the medication and dose. The most common adverse effects in clinical trials include:

Hot flashes
Vaginal dryness
Loss of sex drive
Headache
Erectile dysfunction
Weight gain
Gynecomastia (enlarged breasts in males)
Fluid retention
Injection site reactions
Cough
Acne
Nausea
Vomiting
Constipation

Sometimes, GnRH agonists can cause more serious side effects, including:

Decreased bone mineral density (osteoporosis)
High blood sugar (hyperglycemia)
Heart problems
Seizures
Anemia
Depression or mood disorders
Severe allergic reactions

This is not a complete list of side effects and we encourage you to consult with your healthcare provider or mental health professional for medical advice about any possible side effects.

What is the difference between a GnRH agonist and a GnRH antagonist?

GnRH agonists work the same as naturally made GnRH. When they are first given, it stimulates the pituitary to produce more FSH and LH. After constant stimulation over some time, the pituitary doesn’t respond to GnRH agonists, which decreases the production of FSH and LH. GnRH antagonists take a more direct approach. They directly block the pituitary from binding and responding to naturally made GnRH.

How effective is GnRH therapy in the treatment of prostate cancer?

According to a clinical study, androgen deprivation therapy with medications such as GnRH agonists is effective in the treatment of prostate cancer. It is the first-line treatment for patients with metastatic prostate cancer, with an almost 85% response rate. In males treated for prostate cancer, testosterone concentrations were reduced to below castration levels within 2 to 4 weeks after initiation of treatment.

How much do gonadotropin releasing hormone agonists cost?

Gonadotropin releasing hormone agonists are very expensive with an average cost of around $10,000 per year.

You can purchase Gonadotropin releasing hormone agonists for $49 per month from NiceRx if eligible for assistance. Prices at the pharmacy vary by location, strength, and quantity, as well as your insurance status.

Related resources for Gonadotropin releasing hormone agonists

The content on this website is intended for information purposes only. It does not constitute medical advice. The information on this website should not be relied upon and is not a substitute for professional medical advice. You should always speak to your doctor regarding the risks and benefits of any treatment.