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What Is Leuprolide?

Leuprolide acetate is a prescription gonadotropin-releasing hormone agonist. This page focuses on the current short-acting leuprolide acetate injection containing 1 mg per 0.2 mL. It is indicated for palliative treatment of advanced prostate cancer and is distinct from long-acting depot leuprolide products with different indications and schedules.

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What Is Leuprolide?

Leuprolide acetate is a prescription gonadotropin-releasing hormone agonist. This page focuses on the current short-acting leuprolide acetate injection containing 1 mg per 0.2 mL. It is indicated for palliative treatment of advanced prostate cancer and is distinct from long-acting depot leuprolide products with different indications and schedules.

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How Does Leuprolide Suppress Testosterone?

Leuprolide initially stimulates pituitary gonadotropin release, which temporarily raises testosterone. With continuous administration, pituitary gonadotropin secretion becomes suppressed and testosterone concentrations fall to castrate levels, commonly within two to four weeks.

Who Is Treated With Leuprolide Injection?

Current short-acting leuprolide acetate injection is used for palliative treatment of advanced prostate cancer. Patients with metastatic vertebral lesions or urinary tract obstruction are observed closely during the first weeks due to the risk of worsening symptoms.

How Is Leuprolide Injection Dosed?

The recommended dose is 1 mg, equal to 0.2 mL, by subcutaneous injection once daily. Injection sites are varied periodically. Testosterone and prostate-specific antigen concentrations are monitored during treatment.

What Serious Risks Are Linked to Leuprolide?

Leuprolide can cause an initial tumor flare with increased bone pain and can contribute to ureteral obstruction or spinal cord compression. Other serious concerns include severe cutaneous adverse reactions, hyperglycemia, diabetes, myocardial infarction, sudden cardiac death, stroke, QT prolongation, hypersensitivity, and fetal harm.

Frequently Asked Questions About Leuprolide

What does the current short-acting leuprolide injection treat?

It is indicated for palliative treatment of advanced prostate cancer.

What is the daily dose?

The recommended dose is 1 mg by subcutaneous injection once daily.

Why can symptoms worsen when treatment begins?

Leuprolide initially raises testosterone before sustained treatment suppresses hormone production, which can temporarily worsen prostate cancer symptoms.

Is short-acting leuprolide the same as depot leuprolide?

No. Long-acting depot products have different dosing schedules and can have different labeled indications.

References

DailyMed - LEUPROLIDE ACETATE injection. https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=d6bd26bd-b8d8-4c5a-bc5c-7b8a1efaa584. Date Accessed October 12, 2026.

Leuprolide. LiverTox. https://www.ncbi.nlm.nih.gov/books/NBK548676/. Date Accessed October 12, 2026.

Leuprolide Acetate. National Cancer Institute. https://www.cancer.gov/about-cancer/treatment/drugs/leuprolideacetate. Date Accessed October 12, 2026.

Leuprolide Acetate. PubChem. https://pubchem.ncbi.nlm.nih.gov/compound/Leuprolide-Acetate. Date Accessed October 12, 2026.

Leuprolide Injection. MedlinePlus. https://www.medlineplus.gov/druginfo/meds/a685040.html. Date Accessed October 12, 2026.