Histrelin

Summary

Histrelin is a potent synthetic GnRH agonist delivered via a subcutaneous implant. It is FDA-approved for the palliative treatment of advanced prostate cancer (Vantas) and for the treatment of central precocious puberty (CPP) in children (Supprelin LA). The implant releases histrelin continuously over approximately 12 months, providing sustained hormonal suppression.

Mechanism of Action

Synthetic analogue of gonadotropin-releasing hormone (GnRH) that, upon continuous administration, causes desensitization and downregulation of pituitary GnRH receptors, leading to suppression of LH and FSH secretion, and subsequently reducing gonadal steroid production (testosterone in males, estrogen in females) to castrate levels.

Routes of Administration

Goals & Uses

• Palliative treatment of advanced prostate cancerOncologyHigh
• Testosterone suppression in transgender womenGender Affirming CareModerate
• Endometriosis managementGynecologyLow
• Treatment of central precocious puberty (CPP)Pediatric EndocrinologyHigh

Contraindications

• Hypersensitivity to histrelin, GnRH, or GnRH analoguesAllergyHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Women of childbearing potential not using effective contraceptionReproductiveHigh

Adverse Effects

• Implant site reactionsLocal/dermatologicCommon
• Testosterone flare (initial)EndocrineCommon
• Decreased bone mineral densityMusculoskeletalCommon
• Sexual dysfunction / decreased libidoEndocrine/sexualCommon
• QT prolongationCardiovascularUncommonExtended QT interval on ECG
• Hot flushes / hot flashesEndocrine/vasomotorCommon

Drug Interactions

• Anticoagulants (e.g., warfarin)Moderate
• Insulin / antidiabetic agentsModerate
• QT-prolonging agents (e.g., antiarrhythmics, antipsychotics, fluoroquinolones)High

Population Constraints

• Patients with osteoporosis or high fracture riskMusculoskeletalRelative
• Patients with cardiovascular diseaseComorbidityRelative
• Patients with spinal metastases or urinary obstruction (prostate cancer)Disease SpecificRelative
• Pediatric patients (CPP)AgeRelative

Regulatory Status

• European UnionUnknownHistrelin implant not prominently approved via EMA centralized procedure; availability may vary by member state.
• United StatesApprovedApproved: Palliative treatment of advanced prostate cancer (Vantas), Treatment of children with central precocious puberty (Supprelin LA)FDA-approved; Supprelin LA holds Orphan Drug designation for CPP. Both are 12-month subcutaneous implants.
• United KingdomUnknownNot listed as a standard MHRA-approved product; other GnRH agonists (leuprolide, goserelin, triptorelin) are more commonly used in the UK.

FDA-approved. Vantas (histrelin acetate 50 mg implant) approved for advanced prostate cancer. Supprelin LA (histrelin acetate 50 mg implant) approved for CPP in children. Orphan Drug designation held for CPP indication.

Evidence & Sources

No sources recorded yet.