Leuprolide
Also known as: Lupron, Lupron Depot, Eligard, Fensolvi, Camcevi, Leuprorelin, TAP-144
Key Facts: Leuprolide
- Category
- Hormonal
- FDA Status
- FDA Approved
- Clinical Status
- FDA Approved - Multiple indications (first approved 1985). 3-month Lupron Depot-PED (11.25 mg and 30 mg) for central precocious puberty has been approved since 2011; Fensolvi (6-month) since 2020. WADA: prohibited at all times in male athletes (S2, GnRH agonist analogues).
- Banned in Sport (WADA)
- Prohibited at all times under WADA S2 (testosterone-stimulating peptides in males: leuprorelin is named). Males only; not prohibited for females.
- Administration
- Intramuscular or subcutaneous depot injection
- Typical Dose
- Variable - depends on formulation
- Frequency
- Daily, monthly, or every 3-6 months
- Duration
- Months to years depending on indication
How does Leuprolide work?
Leuprolide is a superagonist at the pituitary GnRH receptor. When you first give it, it strongly stimulates the receptor and causes a transient surge in LH, FSH, and sex hormones, the so-called flare. With continuous exposure, the pituitary internalizes and downregulates its GnRH receptors and becomes desensitized, so within roughly two to four weeks LH and FSH plummet and gonadal testosterone or estrogen falls to near-castrate levels. In prostate cancer, removing testosterone starves androgen-dependent tumor cells; in endometriosis and fibroids, dropping estrogen shrinks hormone-driven tissue and eases pain. That early flare is clinically important because it can briefly worsen symptoms in prostate cancer or endometriosis, which is why doctors sometimes co-administer other drugs to blunt it.
What does the research show?
Leuprolide has decades of clinical trial and real-world evidence behind it. It was first FDA-approved in 1985 as a daily injection, with the long-acting Lupron Depot following, and newer forms like Eligard, Fensolvi (6-month pediatric, 2020) and Camcevi (2021) came later, so unlike most peptides in this space its efficacy is not in question. GnRH agonists like leuprolide largely replaced surgical castration in prostate cancer management because they achieve the same hormonal suppression reversibly. In endometriosis and fibroids, trials show it reduces lesion size, pelvic pain, and bleeding, and it is a standard tool for central precocious puberty in children. The trade-off is the low-estrogen or low-testosterone state it induces, which brings hot flashes, bone density loss with longer use, and other menopausal or andropausal effects, so courses are often limited or paired with add-back hormone therapy. Labels also warn about high blood sugar and heart risk in men on long-term treatment, and psychiatric symptoms, seizures and pseudotumor cerebri in children. This is a mainstream oncology and gynecology drug; the honest framing is that it is highly effective for its approved uses and that its 'side effects' are the direct, expected consequence of shutting down sex hormones.
What doses have been studied?
Typical Dosingⓘ
Community experience
Variable - depends on formulation
1 mg daily to 45 mg every 6 months
Daily, monthly, or every 3-6 months
A GnRH agonist used in prostate cancer, endometriosis and precocious puberty. Multiple formulations exist.
Research Dosingⓘ
Scientific studies
FDA-approved dosing
Doses from Studies
7.5mg monthly depot
22.5mg 3-month depot
45mg 6-month depot
Duration
Months to years depending on indication
Administration
Intramuscular or subcutaneous depot injection
When and how is Leuprolide taken?
Best Time to Take
Morning or as directed
Follow recommended protocol
Food Recommendation
With or without food
Why This Timing?
Timing may vary based on individual response and goals. Consistency is generally more important than specific timing.
What are the side effects of Leuprolide?
Not everyone experiences these effects. Individual responses vary based on dosage, duration, and personal factors.
- ●Hot flashes (very common)
- ●Injection site reactions
- ●Headache
- ●Fatigue
- ●Depression and mood changes
- ●Bone thinning (long-term)
- ●Tumor flare reaction
- ●High blood sugar / diabetes risk
- ●Cardiovascular risks
- ●Seizures (rare)
- ●Pseudotumor cerebri (children, rare)
References
- https://www.ncbi.nlm.nih.gov/books/NBK551662/
- https://go.drugbank.com/drugs/DB00007
- https://pmc.ncbi.nlm.nih.gov/articles/PMC10201295/
- https://pubmed.ncbi.nlm.nih.gov/17970643/
- https://www.drugpatentwatch.com/p/NDA/019010
- https://www.healio.com/news/endocrinology/20120325/fda-approves-two-strengths-of-a-new-leuprolide-acetate-formulation
- https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/019732s050,020517s047lbl.pdf
- https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211488Orig1s000Approv.pdf
- https://www.wada-ama.org/en/prohibited-list
Research This Peptide Further
Frequently Asked Questions
What does Leuprolide do?
Leuprolide (brand name Lupron) is a synthetic GnRH agonist, a modified peptide far more potent than natural GnRH, and it is FDA-approved for advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. The clever part is counterintuitive: it works by overstimulating the GnRH system so hard that the pituitary shuts down sex hormone production. It is a real, long-established prescription drug (first US approval 1985), not a research peptide, and it carries meaningful side effects from the low-hormone state it creates.
How does Leuprolide work?
Leuprolide is a superagonist at the pituitary GnRH receptor. When you first give it, it strongly stimulates the receptor and causes a transient surge in LH, FSH, and sex hormones, the so-called flare. With continuous exposure, the pituitary internalizes and downregulates its GnRH receptors and becomes desensitized, so within roughly two to four weeks LH and FSH plummet and gonadal testosterone or estrogen falls to near-castrate levels. In prostate cancer, removing testosterone starves androgen-dependent tumor cells; in endometriosis and fibroids, dropping estrogen shrinks hormone-driven tissue and eases pain. That early flare is clinically important because it can briefly worsen symptoms in prostate cancer or endometriosis, which is why doctors sometimes co-administer other drugs to blunt it.
Is Leuprolide FDA approved?
Yes, Leuprolide is FDA approved. FDA Approved - Multiple indications (first approved 1985). 3-month Lupron Depot-PED (11.25 mg and 30 mg) for central precocious puberty has been approved since 2011; Fensolvi (6-month) since 2020. WADA: prohibited at all times in male athletes (S2, GnRH agonist analogues).
Is Leuprolide banned in sport?
Prohibited at all times under WADA S2 (testosterone-stimulating peptides in males: leuprorelin is named). Males only; not prohibited for females.
What are the side effects of Leuprolide?
Reported side effects include: Hot flashes (very common), Injection site reactions, Headache, Fatigue, Depression and mood changes. Individual responses vary based on dosage, duration, and personal health factors.
What is the typical dose of Leuprolide?
Community-reported common dose: Variable - depends on formulation (Daily, monthly, or every 3-6 months). Range: 1 mg daily to 45 mg every 6 months. Administration: Intramuscular or subcutaneous depot injection. Prescription drug. Dose set by prescriber per label. Not medical advice.
Related Peptides
Peptides commonly compared with Leuprolide or used in similar applications.
Octreotide
FDAOctreotide is a synthetic eight-amino-acid mimic of the natural hormone somatostatin, the body's main 'off switch' for hormone secretion. It shuts down excess growth hormone, so it is a frontline FDA-approved drug for acromegaly, and it also tames the flushing and diarrhea of hormone-secreting carcinoid and other neuroendocrine tumors. This is real, approved medicine with decades of clinical data behind it, sold as Sandostatin (injectable, since 1988), Sandostatin LAR (monthly depot), and Mycapssa (oral capsule, approved 2020).
HormonalLanreotide
FDALanreotide (development code BIM-23014) is an eight-amino-acid somatostatin analog, a close cousin of octreotide, given as a long-acting deep-injection gel (Somatuline Depot/Autogel) usually once a month. The FDA approved it for acromegaly in 2007, for gastroenteropancreatic neuroendocrine tumors in 2014, and for carcinoid syndrome in 2017. Generic versions now exist alongside Ipsen's Somatuline Depot. It is established prescription medicine, not an experimental compound.
HormonalPegvisomant
FDAPegvisomant (brand name Somavert) flips the usual acromegaly strategy on its head: instead of telling the tumor to make less growth hormone, it blocks growth hormone's receptor on target tissues directly. It is a PEGylated, genetically modified version of human growth hormone that acts as a receptor antagonist, FDA-approved in 2003 for acromegaly patients who do not respond well to surgery or other drugs. It is the single most effective option for normalizing IGF-1, which is why it is a key second-line therapy.
HormonalMacimorelin
FDAMacimorelin (brand name Macrilen) is an orally active ghrelin receptor agonist used as a diagnostic test, not a treatment. You drink a single dose, then doctors measure how much growth hormone the pituitary releases to diagnose adult growth hormone deficiency. It was FDA approved in December 2017 as the first oral diagnostic agent for that condition.
HormonalHMG
FDAHMG (human menopausal gonadotropin, sold as menotropins under the brand Menopur) is a purified hormone mix extracted from the urine of postmenopausal women. Each standard vial carries 75 IU of FSH activity and 75 IU of LH activity, with most of the LH activity coming from hCG. It is an FDA-approved fertility drug used to stimulate egg development in IVF, and it is also used, mostly off-label in the US, together with hCG to kick-start sperm production in men whose pituitary does not make enough FSH and LH. This one has decades of real clinical use behind it.
HormonalTriptorelin
FDATriptorelin is a synthetic analog of gonadotropin-releasing hormone (GnRH) with a D-tryptophan swapped in at position 6, which makes it far more potent and longer-lasting than the natural hormone. As a long-acting depot it is FDA-approved to shut down testosterone in advanced prostate cancer (Trelstar) and to pause early puberty in children (Triptodur), and in Europe it is sold as Decapeptyl, including a short-acting 0.1 mg form used in IVF. In men's health circles it is known for something else: a single small dose used to 'restart' testosterone after steroid use. That idea rests on very little published evidence.
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