Overview
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In plain language
Leuprolide (brand name Lupron, and others) is an FDA-approved medicine that copies GnRH, the brain hormone that controls sex hormones. It is 9 amino acids long.
Oddly, it lowers sex hormones by overstimulating the system: after a short rise at first, the body stops responding. It is used for prostate cancer, endometriosis, uterine fibroids and early puberty in children. It is given as a long-lasting injection every one to six months.
For students
Leuprolide (leuprorelin) is a GnRH agonist nonapeptide, about 1,209 Da. Compared with GnRH, it has D-Leu at position 6 and a C-terminal ethylamide in place of Gly10. These changes resist enzyme breakdown and increase receptor affinity.
Continuous receptor stimulation causes an initial flare in LH, FSH and testosterone or estrogen, then receptor desensitization and suppression to castrate or postmenopausal levels within two to four weeks. Depot formulations use polymer microspheres or gels.
For researchers and instructors
Clinical use. Advanced prostate cancer, endometriosis, fibroid-associated anemia, central precocious puberty, and as part of some fertility protocols.
Safety. The early flare can worsen symptoms in metastatic prostate cancer, so antiandrogens are often given at the start. Long-term effects include hot flashes, bone loss and metabolic changes.
Status. FDA-approved since 1985, with many formulations.
Molecular identity
- Amino acids
- 9
- Molecular weight
- ~1,209.4 Da
- Formula
- C₅₉H₈₄N₁₆O₁₂
- Sequence
- pGlu–His–Trp–Ser–Tyr–D-Leu–Leu–Arg–Pro–NHEt
Origin and history
Leuprolide was made in the 1970s by Masahiko Fujino’s team at Takeda in Japan, as a stronger version of GnRH. The surprise was that a “super” GnRH, given continuously, shuts down the reproductive hormone system instead of stimulating it.
This made it a treatment for advanced prostate cancer, approved as Lupron in 1985, and later endometriosis and early puberty. In 2001 the U.S. marketer TAP Pharmaceutical Products paid $875 million in one of the largest health-care fraud settlements of its time over Lupron sales practices.
Key people
- Masahiko FujinoTakeda Chemical Industries
- Andrew SchallyShowed GnRH analogues can treat prostate cancer
Timeline
- 1974
Leuprolide described
- 1985
Lupron approved for prostate cancer
- 1989
Monthly depot approved
- 2001
$875 million TAP settlement
See every peptide on one history timeline.
Human evidence
Approved for prostate cancer, endometriosis, uterine fibroids and central precocious puberty.
Registration and enrollment are not proof of benefit; check study results directly.
Explore original publications and distinguish preclinical findings from controlled human evidence.
Safety and regulatory status
See every compound on the regulatory tracker.
FDA-approved.
This profile is educational and does not provide treatment, dosing or sourcing guidance.
Sources
- PubMed literature search: Leuprolide
- PubChem compound search: Leuprolide
- DailyMed (FDA label search): Leuprolide
- PubMed: Fujino leuprolide
- ClinicalTrials.gov search: Leuprolide
Hernandez Gener, E. (2026, November 7). Leuprolide: molecular data, research history and evidence. VALREXA Biosciences. https://valrexa.com/peptides/leuprolide.html
APA style · Last reviewed November 7, 2026 · Our editorial standardsLast reviewed November 7, 2026. Trial and regulatory status can change; confirm in the linked registries. This profile is educational and is not medical advice, a treatment recommendation, or dosing or sourcing guidance. Report an error · Corrections policy