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Triptorelin, sold under the brand name Decapeptyl among others, is a that acts as an agonist analog of gonadotropin-releasing hormone, repressing expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

(2025). 9780857111739, Pharmaceutical Press.
It was patented in 1975 and approved for medical use in 1986.
(2025). 9783527607495, John Wiley & Sons. .
Triptorelin is a therapeutic alternative on the World Health Organization's List of Essential Medicines.

It is a (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2) and a gonadotropin-releasing hormone agonist (GnRH agonist) used as the or salts.

Primary indications include , for the reduction of , to treat , and to treat male with severe sexual deviation. The drug has also been used off label to delay puberty in patients with gender dysphoria.

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 for trans women or testosterone for trans men). and cyproterone acetate 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 in the case of precocious puberty.

Triptorelin has been used as a chemical castration agent for reducing sexual urges in .

Drug action
Triptorelin is a , also known as luteinizing hormone releasing analogue (GnRH analogue, LHRH analogue). The drug binds to receptors in the pituitary gland and stimulates secretion of (namely luteinizing hormone LH and follicle-stimulating hormone FSH). This causes an initial phase of LH and FSH stimulation, prior to of the gonadotrophin-releasing hormone receptors, thereby reducing the release of gonadotropins in the long term, which in turn leads to the inhibition of and production.

Side-effects
General side effects can include:
  • 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 () for treating prostate cancer, endometriosis, uterine myomas, and precocious puberty, and Diphereline and Gonapeptyl (Ferring Pharmaceuticals). In the United States, it is sold by 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. licensed the drug from Tulane in 1982.

Research
Triptorelin and other antiandrogens may be effective in the treatment of obsessive–compulsive disorder.

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).

Further reading
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