Evidence Grade A — Regulatory approved. 95 published studies. 4 registered clinical trials.
Medically reviewed by a licensed medical professional
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Histrelin (sold as Supprelin LA) is a hormone-suppressing implant the size of a small matchstick, placed under the skin of the upper arm in a minor procedure. Providing a full year of continuous treatment from a single insertion, it is primarily used to treat central precocious puberty — a condition where children begin puberty abnormally early. It has also seen significant off-label use as a puberty blocker in gender-affirming care.
Histrelin is also known by these brand and alternate names:
95 published studies: 62 human, 12 animal, 2 in-vitro, 18 reviews
Histrelin is available as Supprelin LA for central precocious puberty (approved 2007). The Vantas implant for prostate cancer was approved in 2004 but discontinued in 2021. The implant requires a minor surgical procedure for insertion and removal/replacement each year.
Supprelin LA's main clinical advantage is its 12-month duration — the longest of any GnRH agonist — which is particularly valuable in paediatric patients where treatment compliance over years is important. Clinical studies demonstrated effective suppression of puberty markers in over 97% of patients. The implant has also seen significant off-label use in gender-affirming care as a puberty blocker, where its annual dosing schedule offers practical benefits for adolescent patients and their families.
Histrelin works through the same mechanism as leuprolide and goserelin — it mimics the brain's natural GnRH hormone but delivers a constant rather than pulsed signal, ultimately shutting down sex hormone production. What makes histrelin unique is its delivery system: a tiny hydrogel implant inserted in the upper arm that slowly releases medication over 12 months, eliminating the need for monthly or quarterly injections entirely.
Clinical studies showed Supprelin LA effectively suppressed puberty markers in over 97% of patients, with the 12-month duration offering the longest dosing interval of any GnRH agonist. For families managing a child's treatment over multiple years, annual rather than monthly or quarterly visits is a meaningful practical advantage. Post-marketing data suggests some implants may retain efficacy beyond the labelled 12 months. The main drawback is that insertion and removal require a minor surgical procedure under local anaesthesia, which can be daunting for paediatric patients. A separate prostate cancer formulation (Vantas) was previously available but was discontinued commercially in 2021. No major new research programmes are active for histrelin itself.
PeptideTrace tracks 4 registered clinical trials for Histrelin sourced from ClinicalTrials.gov.
Prospective Multicentre Non-interventional Study of VANTAS® for the Treatment of Patients With Advanced Prostate Cancer
Vantas Implant Retrieval Study
Histrelin Subcutaneous Implant in Children With Central Precocious Puberty
Study to Evaluate Efficacy and Safety of Histrelin Subdermal Implant in Men With Advanced Prostate Cancer
Health Canada Market Authorisation
FDA ORIG 1
FDA SUPPL 1
FDA SUPPL 3
FDA SUPPL 6
FDA SUPPL 9
FDA SUPPL 11
FDA SUPPL 8
FDA SUPPL 12
FDA SUPPL 14
FDA SUPPL 15
FDA SUPPL 16
FDA SUPPL 17
FDA SUPPL 20
Histrelin is a synthetic nonapeptide (9 amino acids) GnRH agonist delivered via a unique non-biodegradable hydrogel subcutaneous implant providing continuous drug release over 12 months. The 50 mg implant releases approximately 65 mcg/day.
Histrelin shares the GnRH agonist mechanism: continuous receptor stimulation → initial flare → downregulation → sustained HPG axis suppression. The hydrogel implant embedded in the inner arm provides the most extended-duration delivery of any GnRH agonist formulation, eliminating the need for monthly or quarterly injections.
Histrelin is available as Vantas (prostate cancer, approved October 12, 2004—now discontinued) and Supprelin LA (central precocious puberty, approved May 3, 2007). The implant is placed subcutaneously in the inner upper arm and requires minor surgical insertion and removal/replacement annually. Supprelin LA remains the preferred GnRH agonist for CPP due to its 12-month duration and reliable suppression.
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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This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
