Leuprolide
LUPRON
What it isGnRH receptor agonist causing downregulation; prostate cancer, endometriosis, fibroids and precocious puberty.
Why this oneIts broad depot range supports sustained suppression across oncology, gynecology, and precocious puberty.
What limits itAn initial testosterone flare requires antiandrogen cover in prostate cancer. Hot flushes and bone loss.
FDA-approved for
- prostate cancer/endometriosis (1985)
FDA label
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| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Advanced prostate cancer (palliative) | Adults | 1 mg SC QD | 1 mg SC QD | 1 mg SC QD |
Renal Undefined
Hepatic Undefined
Instructions
- Single daily subcutaneous injection; vary injection site periodically.
- Inspect solution for discoloration/particulates before each use.
Contraindications
- Known hypersensitivity to GnRH, GnRH agonist analogs, or excipients (anaphylaxis reported)
Cautions
- Transient testosterone surge in first weeks → tumor flare (bone pain, urinary obstruction, worsening vertebral metastases/neurologic symptoms)
- Decreased bone density with long-term use
- Pituitary apoplexy (rare), some within hours of first dose
Adverse reactions
- Hot flashes
- Peripheral edema, ECG changes/ischemia
- Decreased testicular size, gynecomastia, impotence, general pain, asthenia
Pregnancy May cause fetal harm based on animal data (malformations); no human data. Safety/efficacy not established in females.
Lactation No information; safety/efficacy not established in females.
NO BOXED WARNINGS
Principal riskTestosterone flare needing antiandrogen cover; bone loss
Cost, est. cash$10–$1,000/month
Generic entry1998
Classes and tags
Clinical profile
Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent
Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.
Mechanism of action: Leuprolide ballicule
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Memory aids: mascots and interaction avatars
QT prolongation
