Triptorelin
Encyclopedia
Triptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist
Gonadotropin-releasing hormone agonist
A gonadotropin-releasing hormone agonist is a synthetic peptide modeled after the hypothalamic neurohormone GnRH that interacts with the gonadotropin-releasing hormone receptor to elicit its biologic response, the release of the pituitary hormones FSH and LH.GnRH agonists are pregnancy category...

 (GnRH agonist) used at the acetate
Acetate
An acetate is a derivative of acetic acid. This term includes salts and esters, as well as the anion found in solution. Most of the approximately 5 billion kilograms of acetic acid produced annually in industry are used in the production of acetates, which usually take the form of polymers. In...

 or pamoate salts. By causing constant stimulation of the pituitary
Pituitary gland
In vertebrate anatomy the pituitary gland, or hypophysis, is an endocrine gland about the size of a pea and weighing 0.5 g , in humans. It is a protrusion off the bottom of the hypothalamus at the base of the brain, and rests in a small, bony cavity covered by a dural fold...

, it decreases pituitary secretion of gonadotropins luteinizing hormone
Luteinizing hormone
Luteinizing hormone is a hormone produced by the anterior pituitary gland. In females, an acute rise of LH called the LH surge triggers ovulation and development of the corpus luteum. In males, where LH had also been called interstitial cell-stimulating hormone , it stimulates Leydig cell...

 (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer
Prostate cancer
Prostate cancer is a form of cancer that develops in the prostate, a gland in the male reproductive system. Most prostate cancers are slow growing; however, there are cases of aggressive prostate cancers. The cancer cells may metastasize from the prostate to other parts of the body, particularly...

 or breast cancer
Breast cancer
Breast cancer is cancer originating from breast tissue, most commonly from the inner lining of milk ducts or the lobules that supply the ducts with milk. Cancers originating from ducts are known as ductal carcinomas; those originating from lobules are known as lobular carcinomas...

, precocious puberty
Precocious puberty
As a medical term, precocious puberty describes puberty occurring at an unusually early age. In most of these children, the process is normal in every respect except the unusually early age, and simply represents a variation of normal development. In a minority of children, the early development is...

, estrogen
Estrogen
Estrogens , oestrogens , or œstrogens, are a group of compounds named for their importance in the estrous cycle of humans and other animals. They are the primary female sex hormones. Natural estrogens are steroid hormones, while some synthetic ones are non-steroidal...

-dependent conditions (such as endometriosis
Endometriosis
Endometriosis is a gynecological medical condition in which cells from the lining of the uterus appear and flourish outside the uterine cavity, most commonly on the ovaries. The uterine cavity is lined by endometrial cells, which are under the influence of female hormones...

 or uterine fibroids
Uterine fibroids
A uterine fibroid is a benign tumor that originates from the smooth muscle layer and the accompanying connective tissue of the uterus.Fibroids are the most common benign tumors in...

), and in assisted reproduction
Reproductive technology
Reproductive technology encompasses all current and anticipated uses of technology in human and animal reproduction, including assisted reproductive technology, contraception and others.-Assisted reproductive technology:...

. Triptorelin is marketed under the brand names Decapeptyl (Ipsen
Ipsen
Ipsen is a French pharmaceutical company headquartered in Paris, France. It primarily develops and markets medications used in oncology, endocrinology and the treatment of neuromuscular disorders. In 2005, Ipsen spent € 169 million—20.9% of consolidated sales—on research and development, according...

) and Diphereline and Gonapeptyl (Ferring Pharmaceuticals
Ferring Pharmaceuticals
Ferring Pharmaceuticals is a pharmaceutical company that specializes in the development and marketing of drugs for use in human medicine.It was founded by Frederik Paulsen Sr in Malmö, Sweden, in 1950, initially as the Nordiska Hormon Laboratoriet, renamed Ferring in 1954. A ferring in Frisian is a...

). In the United States, it is sold by Watson
Watson Pharmaceuticals
Watson Pharmaceuticals, Incorporated is the 5th largest pharmaceutical company in the United States based on number of prescriptions dispensed...

 as Trelstar.In Iran Triptorelin is marketed under the brand name Variopeptyl® 0.1

During the treatment of prostate cancer
Prostate cancer
Prostate cancer is a form of cancer that develops in the prostate, a gland in the male reproductive system. Most prostate cancers are slow growing; however, there are cases of aggressive prostate cancers. The cancer cells may metastasize from the prostate to other parts of the body, particularly...

 it does cause a surge of testosterone
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...

 (an initial uplevel of testosterone levels), known as a flare effect. In men a reduction of serum testosterone levels into the range normally seen after surgical castration occurs approximately two to four weeks after initiation of therapy. In contrast, gonadotropin-releasing hormone antagonist
Gonadotropin-releasing hormone antagonist
Gonadotrophin-releasing hormone antagonists are a class of compounds that are similar in structure to natural GnRH but that have an antagonistic effect. GnRH antagonists are peptide molecules that are made up multiple, often synthetically produced amino acids...

s do not cause a surge, but a sudden reduction of testosterone levels.

Systematic IUPAC Name: [d-Trp6]GnRH
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