Histrelin is a synthetic GnRH agonist nonapeptide analog (MW ~1323.5 g/mol) with a D-His(benzyl) substitution at position 6. It is FDA-approved as a subdermal implant for advanced prostate cancer (Vantas, 50 mg implant releasing ~50 mcg/day for 12 months) and central precocious puberty (Supprelin LA, 50 mg implant releasing ~65 mcg/day for 12 months). The hydrogel implant technology provides consistent drug delivery for a full year, offering the longest interval between doses of any GnRH agonist formulation.
Category: Reproductive / Hormonal. Evidence rating: A (strong human clinical data).
Clinical status: FDA-approved (Vantas for advanced prostate cancer; Supprelin LA for central precocious puberty)
Histrelin is a GnRH agonist approximately 100 times more potent than native GnRH due to the D-His(N-benzyl) substitution at position 6, which confers enhanced receptor binding affinity and resistance to enzymatic degradation. Like all GnRH agonists, it operates through the "flare then suppression"…
Safety considerations: Implant site reactions: pain, bruising, soreness, erythema at insertion site (reported in up to 6%); Hot flashes (66% in prostate cancer patients); Fatigue and headache.
Reviewed by the PeptideAtlas Editorial Team. Last reviewed: 2026-08-12.
Related peptides: Kisspeptin, Gonadorelin, Oxytocin.
Compare: Histrelin vs Kisspeptin, Histrelin vs Gonadorelin, Histrelin vs Oxytocin.
The implant is placed subdermally in the inner aspect of the upper arm under local anesthesia through a small incision. After 12 months, it is removed through a small incision and a new implant can be placed at the same time. The procedure takes approximately 15-30 minutes in an outpatient setting.
The 12-month histrelin implant provides the longest dosing interval of any GnRH agonist, reducing clinic visits to once yearly. It also provides very consistent drug delivery without the peaks and troughs associated with injectable depot formulations, potentially resulting in more reliable testosterone suppression.
Both contain 50 mg of histrelin acetate in a hydrogel implant, but they are designed for different release rates and indications. Vantas releases approximately 50 mcg/day and is indicated for prostate cancer. Supprelin LA releases approximately 65 mcg/day and is indicated for central precocious puberty. They are not interchangeable.