FDA Approved Sexual & Reproductive Health

Histrelin

also known as: Supprelin LA, Vantas

Endo Pharmaceuticals' Supprelin LA (pediatric) and Vantas (adult prostate cancer) — a 12-month subcutaneous hydrogel implant delivering histrelin for continuous GnRH-receptor suppression over a full year, minimizing dosing burden for pediatric CPP patients and adult prostate cancer patients alike.

A synthetic GnRH agonist with D-His(benzyl) at position 6 and ethylamide at position 10, formulated into a 50 mg Hydron-polymer subcutaneous implant that releases approximately 50–65 mcg/day of histrelin over 12 months. Marketed in the US as Supprelin LA (pediatric central precocious puberty, approved 2007) and Vantas (adult advanced prostate cancer, approved 2004; US relaunch 2023 after a supply interruption). The 12-month depot is the longest-duration GnRH agonist formulation available in US practice.

Mechanism of action

GnRHR agonism with continuous drug release from a subcutaneous polymer implant producing sustained receptor desensitization, abolition of pulsatile LH, and chemical castration. Flare phase is brief.

Primary uses

  • Central precocious puberty, pediatric (Supprelin LA)
  • Advanced prostate cancer (Vantas, palliative ADT)

Typical dosing

50 mg implant every 12 months (subcutaneous implant (inner aspect of upper arm))

Implant inserted under local anesthetic via small skin incision; removed and optionally replaced after 12 months. Pediatric use should be reassessed annually based on bone-age progression and clinical pubertal staging.

Regulatory status

FDA-approved as Vantas (histrelin acetate 50 mg implant, Endo Pharmaceuticals, approved 2004) for palliative treatment of advanced prostate cancer — US supply paused 2020, relaunched late 2023; and as Supprelin LA (histrelin acetate 50 mg implant, approved 2007) for central precocious puberty in children aged 2 years and older. Both use the same active ingredient and implant platform; Supprelin LA is specifically indicated and dosed for pediatric CPP.

References

  1. [fda-pi] Supprelin LA (histrelin acetate) Prescribing Information. Endo Pharmaceuticals.
  2. [fda-pi] Vantas (histrelin acetate) Prescribing Information. Endo Pharmaceuticals.
  3. [pubmed] Eugster EA, et al. "Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial." J Clin Endocrinol Metab, 2007;92:1697-1704.

Related peptides

Leuprolide

The prototypical long-acting GnRH agonist, FDA-approved across multiple formulations (Lupron Depot, Eligard, Fensolvi, Camcevi) for advanced prostate cancer, endometriosis, central precocious puberty, uterine fibroids, and IVF protocols.

Triptorelin

A widely used long-acting GnRH agonist — FDA-approved as Trelstar for advanced prostate cancer and as Triptodur for pediatric central precocious puberty; approved internationally (Decapeptyl, Gonapeptyl) for endometriosis, uterine fibroids, and female infertility protocols.

Goserelin

AstraZeneca's Zoladex — a long-acting GnRH agonist delivered as a subcutaneous biodegradable implant. FDA-approved for advanced prostate cancer, advanced breast cancer in premenopausal women, endometriosis, and endometrial thinning prior to ablation.

Nafarelin

Pfizer's Synarel — the only FDA-approved intranasal GnRH agonist. Approved for endometriosis and central precocious puberty; offers a depot-free alternative to injectable leuprolide for patients who prefer nasal dosing.

Gonadorelin

The native GnRH decapeptide — the hypothalamic signal that drives LH/FSH release and downstream testosterone/estradiol production. Historically FDA-approved (Factrel, Lutrepulse), now widely used in TRT-adjacent fertility protocols as a testicular-preservation alternative to HCG.
Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.