Leuprorelin 53714-56-0

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Leuprorelin

Leuprorelin or leuprolide acetate is a gonadotropin-releasing hormone analog . Proper Sequence: p-Pro-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt

Mode of action

Leuprolide acts at pituitary GnRH receptors. It down regulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) leading to a dramatic reduction in estradiol levels.

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 A 2005 paper suggested it as a treatment for autism, the hypothetical method of action being the now defunct 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 has been tested as a treatment for reducing sexual urges in pedophiles and other cases of paraphilia. Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease. Leuprolide (Lupron) is also used to treat chronic adrenal disease in ferrets. it also used for treatment of steroid abuse

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 (1985-2008) and Abbott Laboratories (2008-current) under the brand name Lupron. It is available as a slow-release implant or subcutaneous/intramuscular injection. In the UK and Ireland , leuprorelin is marketed by Takeda UKProstap SR(one month injection) and Prostap 3 (three month injection).

    Warnings

    {{Cleanup

     

     

    date=October 2009

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    Systematic (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
    Leuprorelin CAS number: 53714-56-0
    ATC code: L02AE02
    PubChem: 441410
    DrugBank: DB00007
    Formula: C59H84N16O12
    Molecular mass: 1209.4 [[Gram g/mol
    Leuprorelin Assay/Purity: Typically NLT 98%
    Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.