Hormonal & Sexual Health

Leuprolide

Leuprolide works by overwhelming the system rather than blocking it: constant stimulation of the pituitary GnRH receptor exhausts it, and sex hormone production shuts down within weeks. That single off-switch serves four unrelated problems, advanced prostate cancer, endometriosis, uterine fibroids and central precocious puberty, which is why one molecule appears under names as different as Lupron Depot, Eligard and Camcevi. It has been on the US market since 1990, and the randomised evidence goes back further, to a 1984 trial against diethylstilbestrol and a 1989 double-blind trial in 603 men with metastatic prostate cancer. Used off-label as an IVF trigger it produced fewer live births than hCG, with less ovarian hyperstimulation.

Last updated 12 August 2026

Studied forAndrogen suppression therapy · Endometriosis management research · Precocious puberty treatment

Evidence on fileFDA-approved · 2 randomised human trials

Strongest sourceA Controlled Trial of Leuprolide with and without Flutamide in Prostatic Carcinoma (New England Journal of Me… (randomised human trial)

Mechanism

Continuous receptor stimulation downregulates pituitary GnRH receptors, cutting LH and FSH and suppressing testosterone or oestradiol.

Regulatory status

Approved by the FDA. Marketed as LUPRON DEPOT, ELIGARD, VABRINTY, CAMCEVI, LEUPROLIDE ACETATE. Earliest approval 1990-10-22. Application NDA020011, NDA020517, NDA021343, NDA021731, NDA211488, ANDA075471, ANDA212963, ANDA215826, ANDA217437.

An approval grades as rung 1 on this site, because 21 CFR 314.126 requires adequate and well-controlled human investigations and one cannot be granted without them. It covers specific indications and doses, though, and does not transfer to other uses of the same molecule.

Reported effects

What sources associate with this compound. Reported categories, not outcomes we have graded — each would need its own citation and rung.

Androgen suppression therapy
Endometriosis management research
Precocious puberty treatment

Dosing on file unverified

SC: 7.5 mg monthly, 22.5 mg q3mo, 30 mg q4mo, 45 mg q6mo; IM: 3.75 mg monthly, 11.25 mg q3mo; Implant: 65 mg × 12 months

Carried from a source that labels it unverified, and reproduced with that label attached. A record of what is reported, not a recommendation. No citation on this page establishes it.

Half-life, storage & sport

Elimination half-life: 3 hours (human, IV) — study. LUPRON DEPOT FDA prescribing information, section 12.3.

The half-life on file is 3 h, measured intravenously. No dosing schedule could be read from this record, so the curve below is one dose drawn from the moment it is given. Nothing here says how often it is repeated.

One dose. 15 h of decay, normalised to its own peak.

The half-life was measured by a route this is not given by. That makes it a lower bound rather than an estimate: absorption from an injection site goes on supplying the blood after an intravenous bolus would have cleared, so the real curve is flatter and lasts longer than the one drawn here. It is never shorter.

The rise is not modelled and the axis is not a blood level. No absorption rate constant and no volume of distribution are on file, so each dose appears at full height the instant it is given, and the axis is percent of this compound's own peak.

Literature on file 3

human RCT
A Controlled Trial of Leuprolide with and without Flutamide in Prostatic Carcinoma (New England Journal of Medicine 1989, cited 1185x) graded on: names a randomised controlled trial — the indexed publication type — “Randomized Controlled”
human RCT
Leuprolide versus Diethylstilbestrol for Metastatic Prostate Cancer (New England Journal of Medicine 1984, cited 571x) graded on: names a randomised controlled trial — the indexed publication type — “Randomized Controlled”
human RCT
FDA approval NDA020011, NDA020517, NDA021343, NDA021731, NDA211488, ANDA075471, ANDA212963, ANDA215826, ANDA217437 graded on: an FDA approval (NDA020011, NDA020517, NDA021343, NDA021731, NDA211488, ANDA075471, ANDA212963, ANDA215826, ANDA217437), which requires adequate and well-controlled human investigations — “NDA020011, NDA020517, NDA021343, NDA021731, NDA211488, ANDA075471, ANDA212963, ANDA215826, ANDA217437”

Identity

Space-filling 3D model of Leuprolide, carbon grey, nitrogen blue, oxygen red — Built from the SMILES on this record — the atoms and bonds are exact. The shape is **one computed low-energy pose**, not a measured structure: a flexible peptide in solution has no single conformation, and where the SMILES leaves a stereocentre undefined the pose commits to one arbitrarily. The skeletal formula below claims connectivity and nothing more, which is what we actually know.

2D chemical structure of Leuprolide — Built from the SMILES on this record — the atoms and bonds are exact. The shape is **one computed low-energy pose**, not a measured structure: a flexible peptide in solution has no single conformation, and where the SMILES leaves a stereocentre undefined the pose commits to one arbitrarily. The skeletal formula below claims connectivity and nothing more, which is what we actually know.

Molecular weight: 1209.4
Molecular formula: C59H84N16O12
CAS number: 53714-56-0
PubChem CID: 657181
InChI key: GFIJNRVAKGFPGQ-LIJARHBVSA-N
Sequence: XHWSYLLRP
SMILES: CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H]6CCC(=O)N6
InChI: InChI=1S/C59H84N16O12/c1-6-63-57(86)48-14-10-22-75(48)58(87)41(13-9-21-64-59(60)61)68-51(80)42(23-32(2)3)69-52(81)43(24-33(4)5)70-53(82)44(25-34-15-17-37(77)18-16-34)71-56(85)47(30-76)74-54(83)45(26-35-28-65-39-12-8-7-11-38(35)39)72-55(84)46(27-36-29-62-31-66-36)73-50(79)40-19-20-49(78)67-40/h7-8,11-12,15-18,28-29,31-33,40-48,65,76-77H,6,9-10,13-14,19-27,30H2,1-5H3,(H,62,66)(H,63,86)(H,67,78)(H,68,80)(H,69,81)(H,70,82)(H,71,85)(H,72,84)(H,73,79)(H,74,83)(H4,60,61,64)/t40-,41-,42-,43+,44-,45-,46-,47-,48-/m0/s1

Notes unverified prose

FDA-approved (Lupron, Eligard, Camcevi, Viadur); Drugs.com; FDA-approved (Lupron, Eligard)

Not on file 0

All 8 tracked fields hold a value on this record: molecular weight and formula, CAS number, PubChem CID, amino-acid sequence, SMILES, InChI and InChI key.

Counted from the record itself, not from what a source said it was missing. 163 of 188 records still have at least one empty.

Listed prices 3

What 1 shop we track listed for Leuprolide, read from their own public catalogues on 2026-09-14. We take no commission on these and they are not ranked by any payment — how vendors are scored.

Compare prices3 listings from 1 shop

Listed in USD
Vendor	Size	Price	Per mg
Mountainside Medical	14 mg	$115.00 USD ~~$189.95 USD~~	$8.21/mg
Mountainside Medical	size not listed	$3500.00 USD ~~$3800.00 USD~~	—
Mountainside Medical	size not listed	$22500.00 USD	—

Prices are the vendor's own listing, reproduced with the date we read it — never converted between currencies, and compared per milligram only where the vendor states the vial size.

At a glance

Strongest rung: human RCT
Citations: 3
Regulatory: FDA approved
Route: Subcutaneous / Intramuscular / Implant
Declared gaps: 0

Citations by rung

human RCT3

Strongest wins, never an average.