Deslorelin, sold under the brand names Ovuplant, SucroMate, and Suprelorin among others, is an

injectable An injection (often and usually referred to as a "shot" in US English, a "jab" in UK English, or a "jag" in Scottish English and Scots) is the act of administering a liquid, especially a drug, into a person's body using a needle (usually a hypod ...

gonadotropin releasing hormone Gonadotropin-releasing hormone (GnRH) is a releasing hormone responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is a tropic peptide hormone synthesized and released ...

superagonist In the field of pharmacology, a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for the target receptor, and thus has an efficacy of more than 100%. For example, goserelin is ...

(

GnRH agonist A gonadotropin-releasing hormone agonist (GnRH agonist) is a type of medication which affects gonadotropins and sex hormones. They are used for a variety of indications including in fertility medicine and to lower sex hormone levels in the treat ...

) which is used in

veterinary medicine Veterinary medicine is the branch of medicine that deals with the prevention, management, diagnosis, and treatment of disease, disorder, and injury in animals. Along with this, it deals with animal rearing, husbandry, breeding, research on nutri ...

for various indications.

Uses

Veterinary

Deslorelin is used in

. 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 Ovulation is the release of eggs from the ovaries. In women, this event occurs when the ovarian follicles rupture and release the secondary oocyte ovarian cells. After ovulation, during the luteal phase, the egg will be available to be fertilize ...

in mares as part of the

artificial insemination Artificial insemination is the deliberate introduction of sperm into a female's cervix or uterine cavity for the purpose of achieving a pregnancy through in vivo fertilization by means other than sexual intercourse. It is a fertility treatment ...

process. It is also used to stabilize high-risk pregnancies, mainly of

livestock Livestock are the domesticated animals raised in an agricultural setting to provide labor and produce diversified products for consumption such as meat, eggs, milk, fur, leather, and wool. The term is sometimes used to refer solely to anima ...

. Unlike other GnRH agonists, which are mainly used to inhibit

luteinizing hormone Luteinizing hormone (LH, also known as luteinising hormone, lutropin and sometimes lutrophin) is a hormone produced by gonadotropic cells in the anterior pituitary gland. The production of LH is regulated by gonadotropin-releasing hormone (Gn ...

and

follicle-stimulating hormone Follicle-stimulating hormone (FSH) is a gonadotropin, a glycoprotein polypeptide hormone. FSH is synthesized and secreted by the gonadotropic cells of the anterior pituitary gland and regulates the development, growth, pubertal maturation, ...

by their ultimate

downregulation In the biological context of organisms' production of gene products, downregulation is the process by which a cell decreases the quantity of a cellular component, such as RNA or protein, in response to an external stimulus. The complementary ...

of the

pituitary gland In vertebrate anatomy, the pituitary gland, or hypophysis, is an endocrine gland, about the size of a chickpea and weighing, on average, in humans. It is a protrusion off the bottom of the hypothalamus at the base of the brain. The hypop ...

, 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 Chronic egg laying is a maladaptive, behavioural disorder commonly seen in pet birds which repeatedly lay clutches of infertile eggs in the absence of a mate. It is particularly common in cockatiels, budgerigars, lovebirds, macaws and amazon parrot ...

behavior.

Pharmacology

Pharmacokinetics

Bioavailability In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. ...

is almost complete.

Chemistry

Deslorelin is a

synthetic Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to: Science * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic o ...

analogue of

naturally occurring A natural product is a natural compound or substance produced by a living organism—that is, found in nature. In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by chemical syn ...

gonadotropin-releasing hormone Gonadotropin-releasing hormone (GnRH) is a releasing hormone responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is a tropic peptide hormone synthesized and released ...

(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 Equinae is a subfamily of the family Equidae, which have lived worldwide (except Indonesia and Australia) from the Hemingfordian stage of the Early Miocene (16 million years ago) onwards. They are thought to be a monophyletic grouping.B. J. Mac ...

assisted reproduction Assisted reproductive technology (ART) includes medical procedures used primarily to address infertility. This subject involves procedures such as in vitro fertilization (IVF), intracytoplasmic sperm injection (ICSI), cryopreservation of gametes o ...

. 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 Breast cancer is cancer that develops from breast tissue. Signs of breast cancer may include a lump in the breast, a change in breast shape, dimpling of the skin, milk rejection, fluid coming from the nipple, a newly inverted nipple, or ...

in women, and in treating

precocious puberty In medicine, precocious puberty is puberty occurring at an unusually early age. In most cases, the process is normal in every aspect except the unusually early age and simply represents a variation of normal development. In a minority of childre ...

and

congenital adrenal hyperplasia Congenital adrenal hyperplasia (CAH) is a group of autosomal recessive disorders characterized by impaired cortisol synthesis. It results from the deficiency of one of the five enzymes required for the synthesis of cortisol in the adrenal cortex. ...

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 An orphan drug is a pharmaceutical agent developed to treat medical conditions which, because they are so rare, would not be profitable to produce without government assistance. The conditions are referred to as orphan diseases. The assignment of ...

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 Endometriosis is a disease of the female reproductive system in which cells similar to those in the endometrium, the layer of tissue that normally covers the inside of the uterus, grow outside the uterus. Most often this is on the ovaries, ...

polycystic ovary syndrome Polycystic ovary syndrome, or PCOS, is the most common endocrine disorder in women of reproductive age. The syndrome is named after the characteristic cysts which may form on the ovaries, though it is important to note that this is a sign and n ...

prostate cancer Prostate cancer is cancer of the prostate. Prostate cancer is the second most common cancerous tumor worldwide and is the fifth leading cause of cancer-related mortality among men. The prostate is a gland in the male reproductive system that su ...

, and

uterine fibroids Uterine fibroids, also known as uterine leiomyomas or fibroids, are benign smooth muscle tumors of the uterus. Most women with fibroids have no symptoms while others may have painful or heavy periods. If large enough, they may push on the bl ...

in humans and reached phase III

clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

s for prostate cancer but development was discontinued for all of these indications by 2001.

References

{{GnRH and gonadotropin receptor modulators GnRH agonists Peptides Veterinary drugs