Triptorelin, sold under the brand name Decapeptyl among others, is a

medication Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to medical diagnosis, diagnose, cure, treat, or preventive medicine, prevent disease. Drug therapy (pharmaco ...

that acts as an agonist analog of

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 rele ...

, repressing expression of

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 (G ...

(LH) 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, puberty, pubertal maturat ...

(FSH). It is a

decapeptide Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Dalton (unit), Da or more are called proteins. Chains of fewer t ...

(pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH₂) and a

gonadotropin-releasing hormone 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 tre ...

(GnRH agonist) used as the

acetate An acetate is a salt formed by the combination of acetic acid with a base (e.g. alkaline, earthy, metallic, nonmetallic, or radical base). "Acetate" also describes the conjugate base or ion (specifically, the negatively charged ion called ...

pamoate Pamoic acid, also called embonic acid, is a 2-Naphthoic acid derivative. Salts and esters of pamoic acid are known as pamoates or embonates. It can be prepared by the reaction of 3-hydroxy-2-naphthoic acid with formaldehyde. In pharmacology ...

salt In common usage, salt is a mineral composed primarily of sodium chloride (NaCl). When used in food, especially in granulated form, it is more formally called table salt. In the form of a natural crystalline mineral, salt is also known as r ...

s. Primary indications include

endometriosis Endometriosis is a disease in which Tissue (biology), tissue similar to the endometrium, the lining of the uterus, grows in other places in the body, outside the uterus. It occurs in women and a limited number of other female mammals. Endomet ...

, for the reduction of

uterine fibroids Uterine fibroids, also known as uterine leiomyomas, fibromyoma or fibroids, are leiomyoma, benign smooth muscle tumors of the uterus, part of the female reproductive system. Most people with fibroids have no symptoms while others may have dysm ...

, to treat

prostate cancer Prostate cancer is the neoplasm, uncontrolled growth of cells in the prostate, a gland in the male reproductive system below the bladder. Abnormal growth of the prostate tissue is usually detected through Screening (medicine), screening tests, ...

, and to treat male

hypersexuality Hypersexuality is a proposed medical condition said to cause unwanted or excessive sexual arousal, causing people to engage in or think about sexual activity to a point of distress or impairment., according to the website of ''Psychology Toda ...

with severe sexual deviation. The drug has also been used off label to delay puberty in patients with gender dysphoria. It was patented in 1975 and approved for medical use in 1986. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health s ...

Medical uses

Triptorelin is used to treat

as part of androgen deprivation therapy. Another common use in the United Kingdom is for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people (in conjunction with

estradiol valerate Estradiol valerate (EV), sold for use oral administration, by mouth under the brand name Progynova and for use by injection (medicine), injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen (medication), es ...

for trans women or testosterone for trans men).

Spironolactone Spironolactone, sold under the brand name Aldactone among others, is classed as a diuretic medication. It can be used to treat edema, fluid build-up due to hepatic cirrhosis, liver disease or kidney disease. It is also used to reduce risk o ...

and

cyproterone acetate Cyproterone acetate (CPA), sold alone under the brand name Androcur or Ethinylestradiol/cyproterone acetate, with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the tre ...

are other drugs used by trans people to suppress sex hormones, but these drugs have a completely different mechanism of action. It can also be used as a

puberty blocker Puberty blockers (also called puberty inhibitors or hormone blockers) are medicines used to postpone puberty in children. The most commonly used puberty blockers are gonadotropin-releasing hormone (GnRH) agonists, which suppress the natura ...

in the case of

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. There is early developm ...

. Triptorelin has been used as a

chemical castration Chemical castration is castration via anaphrodisiac drugs, whether to reduce libido and sexual activity, management of cancer, to treat cancer, or otherwise. Unlike orchiectomy, surgical castration, where the gonads are removed through an incision ...

agent for reducing sexual urges in

sex offender A sex offender (sexual offender, sex abuser, or sexual abuser) is a person who has committed a Sex and the law, sex crime. What constitutes a sex crime differs by culture and legal jurisdiction. The majority of convicted sex offenders have convi ...

Drug action

Triptorelin is a gonadorelin analogue, also known as luteinizing hormone releasing analogue (GnRH analogue, LHRH analogue). The drug binds to receptors in the pituitary gland and stimulates secretion of

gonadotropin Gonadotropins are glycoprotein hormones secreted by gonadotropic cells of the anterior pituitary of vertebrates. They are central to the complex endocrine system that regulates normal growth, sexual development, and reproductive function. T ...

s (namely

LH and

FSH). This causes an initial phase of LH and FSH stimulation, prior to

down-regulation In biochemistry, in the biological context of organisms' regulation of gene expression and production of gene products, downregulation is the process by which a cell decreases the production and quantities of its cellular components, such as RN ...

of the gonadotrophin-releasing hormone receptors, thereby reducing the release of gonadotropins in the long term, which in turn leads to the inhibition of

androgen An androgen (from Greek ''andr-'', the stem of the word meaning ) is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This includes ...

and

estrogen Estrogen (also spelled oestrogen in British English; see spelling differences) is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three ...

production.

Side-effects

General side effects can include: * Anaphylaxis * Arthralgia * Asthenia * Asthma * Breast tenderness (males and females) * Changes in blood pressure * Changes in breast size * Depression * Ovarian cysts * Mood changes * Skin rashes * Hot flashes * Weight changes

Society and culture

Brand names

Triptorelin is marketed under the brand names Decapeptyl (

Ipsen Ipsen is a French biopharmaceutical company headquartered in Paris, France, with a focus on drug development and commercialization in three therapeutic areas: oncology, rare diseases and neuroscience. Ipsen is one of the world's top 15 biopha ...

) for treating prostate cancer, endometriosis, uterine myomas, and precocious puberty, and Diphereline and Gonapeptyl (

Ferring Pharmaceuticals Ferring Pharmaceuticals is a Swiss multinational biopharmaceutical company specialising in areas such as reproductive health, maternal health, gastroenterology and urology. Ferring has been developing treatments for mothers and babies for over 50 ...

). In the United States, it is sold by Watson Pharmaceuticals as Trelstar and by Arbor Pharmaceuticals as Triptodur (an extended-release 6-month depot injection). In Iran, triptorelin is marketed under the brand name Variopeptyl. In the UK and Germany, it is sold as Salvacyl for the treatment of sexual deviations.

History

Triptorelin was developed in Andrew V. Schally's lab at

Tulane University The Tulane University of Louisiana (commonly referred to as Tulane University) is a private research university in New Orleans, Louisiana, United States. Founded as the Medical College of Louisiana in 1834 by a cohort of medical doctors, it b ...

Debiopharm Debiopharm is a Privately held company, privately-held Switzerland, Swiss biopharmaceutical company mainly active in drug development, development and Clinical trial, clinical testing of Drug discovery, drug candidates. It was founded in 1979 by ...

licensed the drug from Tulane in 1982.

Research

Triptorelin and other antiandrogens may be effective in the treatment of

obsessive–compulsive disorder Obsessive–compulsive disorder (OCD) is a mental disorder in which an individual has intrusive thoughts (an ''obsession'') and feels the need to perform certain routines (''Compulsive behavior, compulsions'') repeatedly to relieve the dis ...

Dosage in IVF treatment

Minimal daily dose of triptorelin acetate needed to suppress a premature LH surge during IVF treatment has been determined to be 15 microgram daily, and that 50 microg is equivalent to 100 microg in terms of IVF results.

GnRHa doses used in IVF are derived from treatment schedules used in disseminated prostate cancer, which aim at complete gonadal suppression under all circumstances. Some comparative studies indicate that the daily dose of agonist used in IVF may be decreased without compromising the results

The interval between initiation of study medication and start of FSH stimulation was defined as the desensitization phase. For both parameters, adjacent comparisons showed a statistically significant difference between the effect of placebo and 15 μgtriptorelin, but not between 15 and 50 μg, or between 50 and100 μg (Table II). moreover, it appeared that a daily dose of 50 μg triptorelincreates a state of pituitary desensitization comparable with the "standard" dose of 100 μg, and this endocrine finding was confirmed in the current study.

In prostate cancer

Modern assay technologies reveal that bilateral orchiectomy results in a serum T level of approximately 15 ng/dL as compared to the historical definition of castration of T < 50 ng/dL

Pharmacokinetics

Gonapeptyl Depot 3.75 mg

The systemic bioavailability of the active component triptorelin from the intramuscular depot is 38.3% in the first 13 days (2.9% per day). Further release is linear at 0.92% of the dose per day on average (34μg). Bioavailability after S.C. application is 69% of I.M. availability. Plasma triptorelin values decreased to approx. 100 pg/ml before the next application after I.M. or S.C. application (median values).

References

External links

* {{Portal bar , Medicine GnRH agonists Decapeptides Puberty blockers Drugs developed by AbbVie World Health Organization essential medicines