FDA Approved Sexual & Reproductive Health

Leuprolide

also known as: Lupron, Lupron Depot, Eligard, Fensolvi, Camcevi, leuprorelin

The prototypical long-acting GnRH agonist, FDA-approved across multiple formulations (Lupron Depot, Eligard, Fensolvi, Camcevi) for advanced prostate cancer, endometriosis, central precocious puberty, uterine fibroids, and IVF protocols.

A synthetic decapeptide GnRH agonist with a D-Leu substitution at position 6 and ethylamide at position 10, giving it prolonged receptor occupancy relative to endogenous GnRH. Continuous exposure produces pituitary GnRH-receptor downregulation and chemical castration within 2–4 weeks after an initial testosterone/estradiol flare. Marketed as Lupron (daily SC), Lupron Depot (monthly or every-3/4/6-month IM), Eligard (1/3/4/6-month SC depot), Fensolvi (6-month pediatric SC depot), and Camcevi (6-month SC depot) for prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and as an adjunct in IVF controlled ovarian stimulation.

Mechanism of action

Binds pituitary GnRH receptor (GnRHR). Initial stimulation causes a transient LH/FSH surge with testosterone/estradiol flare (day 3–10). Continuous exposure then desensitizes and downregulates GnRHR expression, abolishing pulsatile LH release. Testosterone falls to castrate levels (<50 ng/dL) within 2–4 weeks in men; estradiol falls to menopausal levels in premenopausal women. In pediatric central precocious puberty, this halts premature pubertal progression.

Primary uses

  • Advanced prostate cancer (androgen-deprivation therapy)
  • Endometriosis symptom management
  • Uterine leiomyomata (fibroids) preoperative
  • Central precocious puberty (pediatric)
  • Adjunct in IVF controlled ovarian stimulation (long-protocol downregulation)
  • Gender-affirming care (puberty suppression, off-label)

Typical dosing

varies by formulation daily SC to 6-month depot (subcutaneous or intramuscular)

Lupron Depot prostate cancer: 7.5 mg IM monthly, 22.5 mg IM every 3 months, 30 mg IM every 4 months, or 45 mg IM every 6 months. Endometriosis: 3.75 mg IM monthly or 11.25 mg IM every 3 months (max 6 months or 12 months with add-back). Fensolvi pediatric CPP: 45 mg SC every 6 months. Flare prevention with a first-generation anti-androgen (bicalutamide) is standard in metastatic prostate cancer.

Regulatory status

FDA-approved across numerous formulations: Lupron / Lupron Depot (TAP/AbbVie, first approved 1985) for advanced prostate cancer, endometriosis, uterine leiomyomata, and central precocious puberty; Eligard (Tolmar) for advanced prostate cancer; Fensolvi (Tolmar, 2020) for pediatric central precocious puberty; Camcevi (Accord BioPharma, 2021) ready-to-administer 6-month prostate cancer depot.

References

  1. [fda-pi] Lupron Depot (leuprolide acetate) Prescribing Information. AbbVie.
  2. [fda-pi] Eligard (leuprolide acetate) Prescribing Information. Tolmar Pharmaceuticals.
  3. [fda-pi] Fensolvi (leuprolide acetate) Prescribing Information. Tolmar Pharmaceuticals.
  4. [review] Conn PM, Crowley WF Jr. "Gonadotropin-releasing hormone and its analogues." N Engl J Med, 1991;324:93-103 (foundational pharmacology).

Related peptides

Triptorelin

A widely used long-acting GnRH agonist — FDA-approved as Trelstar for advanced prostate cancer and as Triptodur for pediatric central precocious puberty; approved internationally (Decapeptyl, Gonapeptyl) for endometriosis, uterine fibroids, and female infertility protocols.

Goserelin

AstraZeneca's Zoladex — a long-acting GnRH agonist delivered as a subcutaneous biodegradable implant. FDA-approved for advanced prostate cancer, advanced breast cancer in premenopausal women, endometriosis, and endometrial thinning prior to ablation.

Histrelin

Endo Pharmaceuticals' Supprelin LA (pediatric) and Vantas (adult prostate cancer) — a 12-month subcutaneous hydrogel implant delivering histrelin for continuous GnRH-receptor suppression over a full year, minimizing dosing burden for pediatric CPP patients and adult prostate cancer patients alike.

Degarelix

Ferring's Firmagon — a GnRH antagonist for advanced prostate cancer that achieves castrate testosterone within 3 days, eliminating the clinical flare risk of GnRH-agonist therapy in patients with symptomatic bone metastases or impending spinal cord compression.

Gonadorelin

The native GnRH decapeptide — the hypothalamic signal that drives LH/FSH release and downstream testosterone/estradiol production. Historically FDA-approved (Factrel, Lutrepulse), now widely used in TRT-adjacent fertility protocols as a testicular-preservation alternative to HCG.
Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.