Leuprolide

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Leuprolide

Clinical data
Pregnancy category	X
Routes of administration	Implant / Injection
ATC code	L02AE02 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life	3 hours
Excretion	Renal
Identifiers
IUPAC name N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(diaminomethylideneamino)-1- [2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxo-pentan-2- yl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl- butyl]carbamoyl]-2-(4-hydroxyphenyl)ethyl] carbamoyl]-2-hydroxy-ethyl]carbamoyl]-2-(1H-indol-3- yl)ethyl]carbamoyl]-2-(3H-imidazol-4-yl)ethyl]-5-oxo- pyrrolidine-2-carboxamide
CAS Number	53714-56-0
PubChem CID	441410
DrugBank	BTD00009
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C59H84N16O12
Molar mass	1209.4 g/mol

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Leuprorelin (INN) or leuprolide acetate (USAN) is a gonadotropin-releasing hormone agonist (GnRH agonist).

Mode of action

By causing constant stimulation of the pituitary GnRH receptors, it initially causes stimulation (flare), but thereafter decreases pituitary secretion (downregulation) of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Clinical usage

Like other GnRH agonists, leuprolide may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat precocious puberty, and to control ovarian stimulation in In Vitro Fertilization (IVF). It is considered a possible treatment for paraphilias.

A 2005 paper suggested it as a treatment for autism, the hypothetical method of action being the controversial theory that autism is caused by mercury, with the additional assumption that mercury binds irreversibly to testosterone and therefore leuprolide can help cure autism by lowering the testosterone level and thereby the mercury level. However, used on children or adolescents it could cause disastrous and irreversible damage to sexual functioning, and there is no scientifically valid or reliable research to show its effectiveness in treating autism. Mark Geier, the proponent of the hypothesis, has frequently been barred from testifying in vaccine-autism related cases on the grounds of not being sufficiently expert in that particular issue.

Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease.

Approvals

• Lupron® Injection (5 mg/mL for daily subcutaneous injection) was first approved by the FDA for treatment of advanced prostate cancer on April 9, 1985.
• Lupron® Depot (7.5 mg/vial for monthly intramuscular depot injection) was first approved by the FDA for palliative treatment of advanced prostate cancer on January 26, 1989, and subsequently in 22.5 mg/vial and 30 mg/vial for intramuscular depot injection every 3 and 4 months, respectively. 3.75 mg/vial and 11.25 mg/vial dosage forms were subsequently approved for subcutaneous depot injection every month and every 3 months, respectively for treatment of endometriosis or fibroids. 7.5 mg/vial, 11.25 mg/vial, and 15 mg/vial dosage forms were subsequently approved for subcutaneous depot injection for treatment of children with central precocious puberty.
• Viadur® (72 mg yearly subcutaneous implant) was first approved by the FDA for palliative treatment of advanced prostate cancer on March 6, 2000.
• Eligard® (7.5 mg for monthly subcutaneous depot injection) was first approved by the FDA for palliative treatment of advanced prostate cancer on January 24, 2002, and subsequently in 22.5 mg, 30 mg, and 45 mg doses for subcutaneous depot injection every 3, 4, and 6 months, respectively.

Leuprolide acetate is marketed by Bayer AG under the brand name Viadur®, by Sanofi-Aventis under the brand name Eligard®, and by TAP Pharmaceuticals under the brand name Lupron®. It is available as a slow-release implant or subcutaneous/intramuscular injection.

In the UK, leuprorelin is marketed by Wyeth as Prostap SR®(one month injection) and Prostap 3® (three month injection).

External links

• Lupron Depot (manufacturer's website)
• Lupron® Injection (package insert from abbott)
• Eligard™ (professional information about the drug)
• Reforming (purportedly) Non-Punitive Responses to Sexual Offending (journal article discussing use of Lupron as a form of reforming sex offender law)