Supprelin LA, Vantas
Evidence Grade A — Regulatory approved. 95 published studies. 4 registered clinical trials.
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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.
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.
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
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.
Nafarelin is marketed as Synarel (approved 1990) for endometriosis and central precocious puberty. It requires administration as one spray in each nostril twice daily — a higher frequency than injectable alternatives but avoids needles entirely, which can be a significant advantage for some patients, particularly children. Clinical trials showed symptom improvement in 75–92% of endometriosis patients. However, absorption can be affected by nasal congestion or concurrent use of nasal decongestants, which can be a practical limitation. As with all GnRH agonists, prolonged use leads to bone density loss, and treatment for endometriosis is typically limited to six months. Nafarelin occupies a niche for patients who prefer non-injectable hormone suppression, though it has become less commonly prescribed as longer-acting depot injections and oral alternatives have become available.
Elagolix is marketed as Orilissa for endometriosis pain (approved July 2018) and as a component of Oriahnn for heavy menstrual bleeding from uterine fibroids (approved May 2020). Oriahnn combines elagolix with low-dose hormone add-back therapy to mitigate bone density loss. Clinical trials showed that the higher dose reduced menstrual pain in approximately 76% of patients and non-menstrual pelvic pain in about 55% at six months. The main limitation is bone density loss with prolonged use, which the add-back therapy in Oriahnn helps address. As an oral tablet taken daily, it offers a fundamentally different experience from injectable or implanted hormone treatments, though it requires consistent daily dosing. It is important to note that elagolix is not a peptide — it is included in this database because it targets the same GnRH pathway as peptide-based treatments.
