Reproductive

Leuprolide

Also known as Lupron, Eligard, Leuprorelin

One-dose burn-down
Half-life
3.0 h
Tmax
1.0 h
Bioavailability
94%
Typical dose
1 mg

GnRH receptor agonist used in prostate cancer, endometriosis, central precocious puberty and fertility protocols. Daily SC (immediate-release) or depot.

Mechanism of action

Continuous GnRH-receptor stimulation desensitizes the pituitary, ultimately suppressing LH/FSH and sex-hormone output (after an initial flare).

Approved drug. PK here is immediate-release SC (~3 h); depot formulations release over 1–6 months and are not modeled here. Expect an initial testosterone/estrogen flare.

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FDA Prescribing Information (DailyMed)

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