Source: FDA label
| Molecular formula | C59H84N16O12 |
|---|---|
| Molecular weight | 1209.4 g/mol |
| Registered trials | 538 |
| PubChem CID | 657181 |
| Brand names | Vabrinty |
Mechanism of Action
12.1 Mechanism of Action Leuprolide acetate, a gonadotropin releasing hormone (GnRH) agonist, acts as an inhibitor of gonadotropin secretion when given continuously in therapeutic doses. Animal and human studies indicate that after an initial stimulation, chronic administration of leuprolide acetate results in suppression of testicular and ovarian steroidogenesis. This effect is reversible upon discontinuation of drug therapy.
Key takeaways
- Leuprolide is a GnRH agonist sold under the brand name Vabrinty for advanced prostate cancer.
- It works by suppressing testicular steroidogenesis after an initial phase of hormone stimulation.
- More than 538 clinical trials have studied this compound, spanning multiple prostate cancer treatment strategies.
- FAERS reports are dominated by hot flushes, fatigue, and injection or device related issues.
- No boxed warning is listed on the current label.
What Leuprolide Is
Leuprolide acetate is a gonadotropin releasing hormone (GnRH) agonist. It is a synthetic peptide that mimics the body's natural GnRH signal. When given continuously, it eventually shuts down the pituitary signals that drive testicular and ovarian hormone production. Animal and human data show this suppression is reversible once treatment stops.
What Leuprolide Is Approved For
Leuprolide, marketed as Vabrinty, is approved for the treatment of advanced prostate cancer. As a GnRH agonist, it lowers testosterone production, which can slow the growth of hormone sensitive prostate tumors. The current label does not carry a boxed warning.
What the Evidence Shows
Leuprolide has been studied in 538 registered clinical trials, reflecting decades of use in prostate cancer research. A Phase 2 trial (NCT05593497) is currently recruiting to test leuprolide alongside abiraterone acetate and an AKT inhibitor in high-risk localized prostate cancer with PTEN loss. A Phase 3 trial (NCT03678025) is recruiting participants to compare standard systemic therapy with and without additional definitive treatment in metastatic prostate cancer.
Reported Side Effects
FAERS data reflect reported cases, not confirmed incidence or proven causation. The most frequently reported reactions are hormonal, led by hot flush (9,557 reports) and fatigue (5,129), alongside injection site pain (4,869). A large share of reports also describe product handling problems, including preparation errors (9,058), syringe issues (7,884), device leakage (6,123), and incorrect usage technique (5,336). Death was also reported (8,367 cases), though FAERS entries cannot establish that leuprolide caused these outcomes.
FAQ
What is leuprolide used for?
Leuprolide, sold as Vabrinty, is approved to treat advanced prostate cancer. It works as a GnRH agonist that lowers testosterone production over time, which can slow hormone sensitive tumor growth.
How does leuprolide work in the body?
Leuprolide mimics a natural hormone signal called GnRH. With continuous use, it eventually suppresses the body's production of testicular and ovarian steroid hormones. This effect reverses once the drug is stopped.
Does leuprolide have a boxed warning?
No. The current label for leuprolide does not include a boxed warning.
What side effects are most commonly reported with leuprolide?
The most frequently reported reactions in FAERS data are hot flushes, fatigue, and injection site pain. A notable number of reports also describe issues with product preparation, syringes, or injection devices. These are counts of submitted reports, not confirmed rates of occurrence or proof that leuprolide caused the event.
Is leuprolide still being studied in clinical trials?
Yes. More than 538 trials have registered leuprolide, including active Phase 2 and Phase 3 studies in prostate cancer. Current trials are exploring it in combination with other therapies and alongside definitive local treatment.
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Content is editorial information, not medical advice. Talk to your doctor before any treatment decision.
Sources: DailyMed label (Vabrinty) FDA FAERS ClinicalTrials.gov PubChem CID 657181
Updated 2026-08-03