Histrelin
Supprelin LA, Vantas (discontinued), histrelin acetate, RWJ 17070, ORF 17070
1What it is
Histrelin is a potent GnRH superagonist first described in the 1980s (Ortho/Johnson & Johnson) and originally given as a daily injection to children with central precocious puberty — puberty starting abnormally early because the hypothalamic–pituitary axis switches on too soon. Its modern form is a small (about 3.5 cm) soft hydrogel cylinder inserted under the skin of the upper arm through a 2–3 mm incision. It releases a steady trickle of drug for a year, after which it is removed and, if needed, replaced. This gives children one minor procedure a year instead of monthly or 3-monthly injections.
The prostate-cancer version (Vantas) was approved in 2004 but was discontinued in 2021 after manufacturing-quality problems and is not expected to return. Supprelin LA remains available in the US through specialty pharmacies; it is not widely approved elsewhere. Community use is essentially non-existent.
2How it's thought to work
As with other , continuous exposure converts stimulation into suppression (see Buserelin, #211). In children with CPP this returns LH, FSH and sex steroids to pre-pubertal levels, halting breast or testicular development, slowing the accelerated bone-age advance, and preserving adult height potential. Because release is continuous rather than pulsatile, the implant avoids the trough-related "escape" from suppression that can occur late in a depot injection cycle.
3What the research shows
Central precocious puberty
Implant duration beyond 12 months
Prostate cancer (Vantas)
Gender-affirming puberty suppression
4Reported side effects and interactions
Literature-reported
implant-site reactions (bruising, pain, swelling, occasionally infection or keloid) in a sizeable minority; implant breakage on removal and difficulty locating the implant (ultrasound sometimes needed) are specific to this product; a transient rise in sex steroids and, in girls, vaginal bleeding in the first weeks (flare); headache, emotional lability, weight gain, hot flushes in adults. In men, class-level androgen-deprivation effects (bone loss, metabolic change, QT prolongation). Rare reports of pseudotumour cerebri (idiopathic intracranial hypertension) with GnRH in children led to a class label update in 2022 †.Community-reported
essentially none documented.Theoretical. the hydrogel is non-biodegradable, so an unretrieved implant means prolonged drug exposure.
Interactions. no formal interaction studies; the same QT and glucose-lowering cautions as other agonists in adults.
Markers researchers commonly monitor
Based on paediatric endocrinology and oncology practice:
| Marker | Why it's watched |
|---|---|
| Stimulated or random LH (ultrasensitive assay), oestradiol or testosterone | confirms suppression in CPP at 1 month and then every 6 months or yearly. |
| Growth velocity, bone age (hand X-ray), Tanner staging | the clinical outcomes the drug is given for. |
| Testosterone and PSA (men, historical Vantas use) | confirms castrate suppression and tumour response. |
| Bone mineral density | for prolonged suppression in adolescents or adults. |
| Implant-site examination | for infection, migration or extrusion. |
Free for everyone. Safety information is never behind a paywall.
5Reconstitution and handling
Supplied as a sterile implant in a kit with insertion tool. Inserted and removed by a trained clinician under local anaesthetic. No or dose calculation is involved; the calculator is not applicable.
6Commonly studied alongside
Leuprolide depot and triptorelin (the main CPP comparators; see GnRH analogue profiles #102–#108), goserelin (#212), buserelin (#211). In CPP, growth hormone has occasionally been co-studied to improve height outcomes.
Informational cross-links. Not stack recommendations.
7Regulatory status by region
| Region | Status (checked —) |
|---|---|
| United States | Supprelin LA FDA-approved (2007) for central precocious puberty in children aged 2 years and older; specialty-pharmacy distribution. Vantas (prostate cancer) discontinued September 2021, no generic |
| European Union | Not centrally authorised; limited or no national marketing † |
| United Kingdom | Not licensed; occasional import on a named-patient basis † |
| Australia | Not registered on the ARTG † |
| South Africa | Not registered † |
| Sport (WADA) | Prohibited in males under S2 (LH-releasing factors); not named explicitly but falls within the class; not prohibited in females |
8Open questions
- Optimal age to stop treatment in CPP to maximise adult height without delaying puberty unduly.
- Long-term bone and psychosocial outcomes after multi-year suppression in adolescents, particularly in gender-affirming care, where evidence is contested.
- Whether supply of Supprelin LA will remain stable given its single-source manufacture.
9References
- 1Eugster EA et al. (2007). Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial. J Clin Endocrinol Metab. PubMed · DOI
- 2Silverman LA et al. (2015). Long-term continuous suppression with once-yearly histrelin subcutaneous implants for the treatment of central precocious puberty: a final report of a phase 3 multicenter trial. J Clin Endocrinol Metab. PubMed · DOI
- 3Schlegel PN et al. (2006). Efficacy and safety of histrelin subdermal implant in patients with advanced prostate cancer. J Urol. PubMed · DOI
- 4Carel JC et al. (2009). Consensus statement on the use of gonadotropin-releasing hormone analogs in children. Pediatrics. PubMed · DOI
- 5Supprelin LA (histrelin acetate) subcutaneous implant US prescribing information (current label). PubMed
References are being resolved to PubMed/DOI identifiers; links search PubMed for the citation until then.
† Being confirmed by our reviewers against current sources.
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Self-reported side effects Phase 2
11Page history
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