Evidence Grade A — Regulatory approved. 994 published studies. 257 registered clinical trials.
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Triptorelin (sold as Trelstar) is a hormone-suppressing injectable for advanced prostate cancer, available in one-month, three-month, and six-month depot formulations. It is one of the most commonly used GnRH agonists worldwide and has also been widely used internationally as a puberty blocker in gender-affirming care and central precocious puberty.
Triptorelin is also known by these brand and alternate names:
994 published studies: 746 human, 79 animal, 133 in-vitro, 76 reviews
Triptorelin is marketed as Trelstar (approved 2000) for advanced prostate cancer, available as intramuscular depot injections in monthly (3.75 mg), three-monthly (11.25 mg), and six-monthly (22.5 mg) formulations. It is also widely used internationally for gender-affirming care and central precocious puberty.
Triptorelin is one of the most commonly used GnRH agonists globally, though it faces the same competitive pressure as other agents in this class from newer oral GnRH antagonists like relugolix, which avoid the initial hormone flare and offer potential cardiovascular advantages. Clinical data demonstrate reliable testosterone suppression comparable to other GnRH agonists in this class.
Triptorelin works through the standard GnRH agonist mechanism: continuous stimulation of the pituitary gland causes an initial brief hormone surge followed by sustained shutdown of sex hormone production. It achieves castrate-level testosterone suppression in over 90% of patients within the first month. The depot injection forms a slow-release reservoir at the injection site, maintaining therapeutic drug levels for one to six months depending on the formulation.
Triptorelin's evidence base is well established, with reliable testosterone suppression comparable to other GnRH agonists in the class. The six-month formulation offers the longest dosing interval among injectable GnRH agonists, reducing clinic visits to just twice yearly. Like all GnRH agonists, triptorelin causes an initial testosterone surge before suppression takes effect, and long-term hormone suppression carries risks of bone density loss, cardiovascular effects, and metabolic changes. The oral GnRH antagonist relugolix (Orgovyx) has emerged as a competitor that avoids the initial hormone surge and offers potential cardiovascular advantages. Triptorelin's use in gender-affirming care for adolescents has been a focus of both clinical research and regulatory discussion across multiple countries.
PeptideTrace tracks 257 registered clinical trials for Triptorelin sourced from ClinicalTrials.gov.
Analysis of Genetic and Environmental Parameters Influencing Growth Rate of Precocious Puberty Children
FET in Adenomyosis
Successive Doses of GnRH Agonist Versus Single Dose of GnRH Agonist to Trigger Ovulation in Hyper-responders
Triggering Ovulation in Normo-responders Using a Modified Dual Trigger Protocol or HCG Trigger
Triggering Oocyte Maturation in POSEIDON Group 3 and 4 Poor Responders Using Double Trigger or HCG Trigger
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Triptorelin is a synthetic decapeptide (10 amino acids) GnRH agonist with a D-Trp6 substitution, conferring approximately 100-fold greater potency than native GnRH. It is available in multiple intramuscular depot formulations.
Triptorelin shares the GnRH agonist mechanism: continuous stimulation → initial flare → receptor downregulation → sustained sex steroid suppression. Castrate testosterone levels are achieved by day 29 in 91–98% of patients across formulations. The D-Trp6 modification provides high receptor affinity and metabolic stability.
Triptorelin is marketed as Trelstar (approved June 15, 2000). Available as IM depot formulations: 3.75 mg monthly, 11.25 mg 3-monthly, and 22.5 mg 6-monthly. The primary indication is advanced prostate cancer. Triptorelin is also widely used internationally for gender-affirming care as a puberty blocker.
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Carbetocin has not been approved by the FDA. It is registered in over 80 countries for prevention of uterine atony and excessive bleeding after caesarean delivery. A heat-stable formulation was added to the WHO Essential Medicines List in 2019. The CHAMPION trial (WHO, 2018; over 29,000 women) compared a heat-stable carbetocin formulation to oxytocin for preventing postpartum haemorrhage after vaginal delivery, and found it to be non-inferior. The heat-stable formulation addresses a significant limitation of oxytocin, which degrades in warm climates without refrigeration — a major concern in low-resource settings where postpartum haemorrhage causes the most deaths. Its regulatory status varies by jurisdiction.
Kisspeptin-54 has no marketing authorisation. Phase II trials conducted primarily at Imperial College London have investigated its use as an IVF oocyte maturation trigger. One trial (60 patients) reported 95% oocyte maturation with zero cases of ovarian hyperstimulation syndrome. Kisspeptin-54 has a more advanced clinical evidence base than kisspeptin-10, with multiple Phase II studies in reproductive medicine. Its potential advantage over conventional IVF triggers relates to a lower risk of the serious complication of ovarian hyperstimulation. Clinical development is ongoing in academic settings. No Phase III trials have been completed.
Goserelin is marketed as Zoladex by AstraZeneca, available as 3.6 mg monthly and 10.8 mg three-monthly subcutaneous implants. First approved in 1989, it is used in advanced prostate cancer, premenopausal breast cancer, endometriosis, and for thinning the uterine lining before surgical procedures. Goserelin achieves castrate-level testosterone suppression (below 50 ng/dL) within two to four weeks. Its unique implant delivery system means there is no liquid injection, reconstitution, or refrigeration required — a practical advantage in some clinical settings. Like all GnRH agonists, it causes an initial hormone flare before suppression takes effect. Goserelin holds an important niche in breast cancer treatment, where it is used to suppress ovarian function in premenopausal women with hormone-receptor-positive disease, often in combination with aromatase inhibitors.
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