Research Reference
Leuprolide
FDA-approved GnRH agonist for prostate cancer and endometriosis
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Leuprolide (Lupron) is an FDA-approved GnRH agonist used for prostate cancer, endometriosis, and other hormone-sensitive conditions.
Dosing Reference
Reconstitution
Add 1 mL bacteriostatic water to the 3.75 mg vial. Resulting concentration: 3.75 mg/mL.
| Dose | Syringe Units | mL Volume | Schedule |
|---|---|---|---|
| 1 mg | 26.67 units | 0.27 mL | SubQ, dailyLupron daily (FDA) |
| 3.75 mg | 100 units | 1 mL | SubQ, monthlyMonthly depot (FDA) |
| 11.25 mg | 300 units | 3 mL | SubQ, every 3 months3-month depot (FDA) |
| 30 mg | 800 units | 8 mL | SubQ, every 4 months4-month depot (FDA) |
Math assumes U-100 insulin syringes (1 mL = 100 units). Verify your syringe matches before use. Round half-units to the nearest visible mark.
Reconstitution
Leuprolide (Lupron) is FDA-approved for prostate cancer, endometriosis, uterine fibroids, and central precocious puberty, supplied as a daily subcutaneous injection or a depot (1-, 3-, 4-, or 6-month) intramuscular/subcutaneous suspension. It is not user-reconstituted from lyophilized powder except per the specific depot kit instructions. Compounded research-peptide forms are not FDA-approved.
For compounded forms, concentration depends on vial size and diluent volume; no standard compounded protocol exists. Compounded forms are not FDA-approved.
Cycling Protocol
FDA-approved leuprolide is used as chronic therapy (daily or depot every 1–6 months) for the indicated condition; no fixed cycle end. Dosing frequency depends on the specific depot formulation prescribed.
Routes of Administration
Subcutaneous injection (daily Lupron): Once daily into the abdomen.
Intramuscular or subcutaneous depot (Lupron Depot, Eligard): Every 1, 3, 4, or 6 months depending on the formulation.
No oral route is established (peptide). Compounded forms are not FDA-approved.
Stacking Protocols
| Stack | Components | Purpose | | --- | --- | --- | | Androgen deprivation | Leuprolide + antiandrogen | Standard prostate cancer protocol (FDA, under oncology supervision) | | Add-back therapy | Leuprolide + low-dose estrogen | Endometriosis protocol (FDA, under supervision) |
Leuprolide combinations are managed under specialist oncology/gynecology supervision. Compounded forms are not FDA-approved.
Side Effects & Safety
- Hot flashes — very common
- Decreased libido, erectile dysfunction — common
- Bone density loss — risk with long-term use
- Injection-site reactions — common
- Mood changes, depression — common
- Tumor flare — transient testosterone increase at initiation (managed with antiandrogen)
- Cardiovascular events — risk, especially in prostate cancer use
Leuprolide (Lupron) is FDA-approved for prostate cancer, endometriosis, fibroids, and central precocious puberty. Compounded research-peptide forms are not FDA-approved.
Research Basis
Leuprolide is a synthetic GnRH (gonadotropin-releasing hormone) agonist, FDA-approved (Lupron).
Mechanism: Initially stimulates then suppresses gonadotropin (LH/FSH) release via pituitary GnRH receptor downregulation, leading to suppressed testosterone (men) or estrogen (women) — chemical castration.
Clinical evidence: FDA-approved for prostate cancer (androgen deprivation), endometriosis, uterine fibroids, and central precocious puberty. Extensive clinical experience.
FDA-approved for the indications above. Compounded research-peptide forms are not FDA-approved.