Histrelin
Also known as: Histrelin acetate, LH-RH agonist, ORF-17070, Supprelin LA, Vantas
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Summary
Histrelin is a synthetic GnRH analog administered via subcutaneous implant. It is FDA‑approved for treatment of advanced prostate cancer, endometriosis, and central precocious puberty by providing long‑acting suppression of the hypothalamic‑pituitary‑gonadal axis.
Mechanism of Action
Continuous activation of pituitary GnRH receptors leads to desensitization, markedly decreasing LH and FSH secretion and consequently suppressing gonadal steroid production.
Routes of Administration
Goals & Uses
- Palliative treatment of advanced prostate cancerOncologyHigh
- Prostate cancerOncologyHigh
- Testosterone suppression in transgender womenGender Affirming CareModerate
- Central precocious pubertyPediatric EndocrinologyHigh
- Endometriosis managementGynecologyLow
- Treatment of central precocious puberty (CPP)Pediatric EndocrinologyHigh
- EndometriosisGynecologyModerate
Contraindications
- Hypersensitivity to histrelin, GnRH, or GnRH analoguesAllergyHigh
- Known hypersensitivity to histrelin or excipientsAllergyHigh
- 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
- Decreased libidoSexual / EndocrineCommon
- Hot flashesEndocrine / VasomotorCommon
- Bone mineral density lossSkeletalUncommon
- Sexual dysfunction / decreased libidoEndocrine/sexualCommon
- Injection site reactionLocalCommonRedness, swelling, itching, bruising, or pain at the injection site
- QT prolongationCardiovascularUncommonExtended QT interval on ECG
- Hot flushes / hot flashesEndocrine/vasomotorCommon
Drug Interactions
- Anticoagulants (e.g., warfarin)Moderate
- Estrogen replacement therapyModerate
- Insulin / antidiabetic agentsModerate
- QT-prolonging agents (e.g., antiarrhythmics, antipsychotics, fluoroquinolones)High
- CYP450 inducers (e.g., rifampin)Low
Population Constraints
- Patients with osteoporosis or high fracture riskMusculoskeletalRelative
- Adult males with advanced prostate cancerAgeRelative
- Pediatric patients with central precocious pubertyAgeRelative
- Patients with cardiovascular diseaseComorbidityRelative
- Patients with spinal metastases or urinary obstruction (prostate cancer)Disease SpecificRelative
- Pediatric patients (CPP)AgeRelative
Regulatory Status
- European UnionApprovedApproved: central precocious puberty, endometriosisAvailable under the trade name Vantas/Supprelin in select EU member states.
- United StatesApprovedApproved: advanced prostate cancer, central precocious puberty, endometriosisVantas® (prostate cancer) and Supprelin LA® (CPP, endometriosis) are FDA‑approved.
- United KingdomUnknownNot listed as a standard MHRA-approved product; other GnRH agonists (leuprolide, goserelin, triptorelin) are more commonly used in the UK.
Approved in the United States (Vantas® for prostate cancer; Supprelin LA® for CPP and endometriosis). Marketed as an implant delivering drug over 12 months. Not available as an oral formulation.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Histrelin?
Histrelin is a synthetic GnRH analog administered via subcutaneous implant. It is FDA‑approved for treatment of advanced prostate cancer, endometriosis, and central precocious puberty by providing long‑acting suppression of the hypothalamic‑pituitary‑gonadal axis.
What is Histrelin used for?
Histrelin is educationally associated with: Palliative treatment of advanced prostate cancer, Prostate cancer, Testosterone suppression in transgender women, Central precocious puberty, Endometriosis management, Treatment of central precocious puberty (CPP), Endometriosis. Educational only — not medical advice.
How is Histrelin administered?
Recorded routes of administration: Subcutaneous, Subcutaneous (implant).
What are the potential side effects of Histrelin?
Reported adverse effects include: Implant site reactions, Testosterone flare (initial), Decreased bone mineral density, Decreased libido, Hot flashes, Bone mineral density loss, Sexual dysfunction / decreased libido, Injection site reaction, QT prolongation, Hot flushes / hot flashes. This list is not exhaustive — consult a qualified clinician.
Who should avoid Histrelin?
Recorded contraindications: Hypersensitivity to histrelin, GnRH, or GnRH analogues, Known hypersensitivity to histrelin or excipients, Pregnancy, Women of childbearing potential not using effective contraception. Consult a qualified clinician before use.