Deslorelin

Deslorelin
Deslorelin
Systematic (IUPAC) name
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Clinical data
Trade names Ovuplant
AHFS/Drugs.com International Drug Names
Pregnancy cat. X (USA)
Legal status  ?
Routes implant / Inhalation
Pharmacokinetic data
Excretion renal
Identifiers
ATCvet code QH01CA93
PubChem CID 7979044
UNII TKG3I66TVE N
Chemical data
Formula C64H83N17O12 
Mol. mass 1282.45 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. It stops the production of sex hormones (testosterone and oestrogen).

Deslorelin Acetate is marketed by Peptech with the brand name Ovuplant.[1] It is currently approved for use in veterinary medicine and is used to induce 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.

Pharmacokinetics

Deslorelin is a synthetic analogue of a naturally occurring luteinising-hormone releasing hormone (LHRH). Bioavailability is almost complete.

Clinical trials

Deslorelin was successfully trialed in the US and was approved for veterinary use under certain circumstances. In Europe, it was approved for use in equine assisted reproduction.[2]

It is also being trialed in humans to study its efficacy in treatment of breast cancer in women,[3] and in treating precocious puberty and congenital adrenal hyperplasia in male and female children.[4]

As of August 2011 this drug was not approved for general use in the US, other than within approved clinical trials. Orphan drug status has been designated in the US, though approval had not been issued as of 2011.[5]

References

  1. ^ Peptech official Ovuplant site
  2. ^ Deslorelin Acetate - European Agency for the Evaluation of Medicinal Products
  3. ^ Deslorelin Combined With Low-Dose Add-Back Estradiol and Testosterone in Preventing Breast Cancer in Premenopausal Women Who Are at High Risk for This Disease - National Cancer Institute
  4. ^ Three Drug Combination Therapy Versus Conventional Treatment of Children With Congenital Adrenal Hyperplasia - National Institutes of Health Clinical Center
  5. ^ "Results for Orphan Drug Product Designations Search". FDA. http://www.accessdata.fda.gov/scripts/opdlisting/oopd/OOPD_Results_2.cfm?Index_Number=016086. Retrieved 3 September 2011. 
v · d · eGonadotropins and GnRH (G03G)
Gonadotropin
preparations
Agonist
Antigonadotropin
GnRH
Buserelin • Goserelin • Histrelin • Leuprorelin • Nafarelin • Triptorelin • Deslorelin
#WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III


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