deslorelin

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      Deslorelin, sold under the brand name Suprelorin among others, is an injectable gonadotropin releasing hormone superagonist (GnRH agonist) which is used in veterinary medicine for various indications.


      Uses




      = Veterinary

      =
      Deslorelin is used in veterinary medicine. One commercial form of deslorelin acetate is marketed by Peptech with the brand name Ovuplant. Another form is available in the United States, Sucromate Equine, which was FDA-approved for use in horses in November 2010. This is manufactured by Thorne BioScience LLC and was introduced to the United States market following the withdrawal of Ovuplant. The deslorelin products are currently approved for use in veterinary medicine and to promote ovulation in mares as part of the artificial insemination process. It is also used to stabilize high-risk pregnancies, mainly of livestock. Unlike other GnRH agonists, which are mainly used to inhibit luteinizing hormone and follicle-stimulating hormone by their ultimate downregulation of the pituitary gland, Deslorelin is primarily used for the initial flare effect upon the pituitary, and its associated surge of LH secretion. Suprelorin is a slowly releasing deslorelin implant used for chemical castration of dogs and ferrets. It is marketed by Virbac. Deslorelin is also used to treat benign prostate hyperplasia in dogs. It is also used to treat pet parrots suffering from chronic egg laying behavior.


      Pharmacology




      = Pharmacokinetics

      =

      Bioavailability is almost complete.


      Chemistry



      Deslorelin is a synthetic analogue of naturally occurring gonadotropin-releasing hormone (GnRH).


      History


      Deslorelin was successfully trialed in the U.S. and was approved for veterinary use under certain circumstances. In Europe, it was approved for use in equine assisted reproduction.
      Ovuplant was withdrawn from the U.S. market following issues with mares which did not become pregnant failing to return to estrus in a timely manner. Techniques were developed where the implant was removed 48 hours after implantation in the mare, however compounded biorelease Deslorelin products were at the time available as well as more commonly used ovulation promoters such as hCG, which did not produce the same failure effect. Upon "Sucromate Equine" receiving FDA-approval, the compounded products were no longer legally available within the U.S., however they remain available in Australia and New Zealand where an approved version is marketed.
      It is also being trialed in humans to study its efficacy in treatment of breast cancer in women, and in treating precocious puberty and congenital adrenal hyperplasia in male and female children.
      As of August 2011 this drug was not approved for general use outside the FDA-licensed functions in the U.S., other than within approved clinical trials. Orphan drug status has been designated in the U.S., though approval had not been issued as of 2011.


      Research


      Deslorelin was under development for the treatment of endometriosis, polycystic ovary syndrome, precocious puberty, prostate cancer, and uterine fibroids in humans and reached phase III clinical trials for prostate cancer but development was discontinued for all of these indications by 2001.


      References

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    deslorelin

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    Deslorelin - Wikipedia

    Deslorelin, sold under the brand name Suprelorin among others, is an injectable gonadotropin releasing hormone superagonist (GnRH agonist) which is used in veterinary medicine for …

    Deslorelin | VCA Animal Hospitals

    What is deslorelin? Deslorelin (brand name Suprelorin-F®) is a synthetic hormonal agent used to manage adrenocortical disease in ferrets. Deslorelin has also been used as a temporary …

    Use of Deslorelin to Control Reproduction in Cats

    Deslorelin is a long acting synthetic agonist of gonadotropin-releasing hormone (GnRH) marketed for veterinary use in most western countries as a 2.1 mg, 4.7 mg and 9.4 mg implant; the 2.1 …

    Deslorelin | EquiMed - Horse Health Matters

    Jun 17, 2014 · Deslorelin is a synthetic hormone that stimulates the release of the pituitary hormones in the mare that cause ovulation from mature ovarian follicles. It's use permits the …

    Deslorelin (Suprelorin) for Chickens and Ducks - PoultryDVM

    Deslorelin (brand name Suprelorin®), also commonly referred to as a 'hormone implant', is a subcutaneous implant used 'off label' in birds. The implant contains deslorelin, a …

    Clinical Use of Deslorelin (GnRH agonist) in Companion Animals: …

    Oct 3, 2014 · Deslorelin implants can be used as an alternative to dopamine agonists to induce fertile oestrus in bitches. However, in some bitches, anovulatory cycles have been reported, …

    Deslorelin: Uses, Interactions, Mechanism of Action - DrugBank …

    Feb 26, 2016 · Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist also known as an LHRH agonist. It stops the production of sex hormones. Be among the first …

    Deslorelin | C64H83N17O12 | CID 25077495 - PubChem

    Deslorelin is a synthetic nonapeptide analogue of the natural gonadotrophin releasing hormone (GnRH) with potential antineoplastic activity. Deslorelin binds to and activates pituitary …

    Deslorelin - an overview | ScienceDirect Topics

    Deslorelin is a small peptide that is administered subcutaneously in the form of an implant (Ovuplant) containing 2.1 mg of the active ingredient.

    Deslorelin: What's That? - Exotic Vet Care

    In birds, deslorelin is utilized to address hormonal behaviors such as self-mutilation, egg-laying, aggression, and reproductively associated feather-damaging behavior/plucking. Because it is …