Histrelin

SUPPRELIN LA is a GnRH agonist and an inhibitor of gonadotropin secretion when given continuously. It delivers approximately 65 mcg histrelin acetate per day.

• SUPPRELIN LA (histrelin acetate) subcutaneous implant is indicated for the treatment of children with central precocious puberty (CPP). Children with CPP (neurogenic or idiopathic) have an early onset of secondary sexual characteristics (earlier than 8 years of age in females and 9 years of age in males).

• SUPPRELIN LA is contraindicated in: Patients who are hypersensitive to gonadotropin releasing hormone (GnRH) or GnRH agonist analogs Pregnancy [see Use in Specific Populations ( 8.1 )] . History of hypersensitivity to gonadotropin releasing hormone (GnRH) or GnRH analogs ( 4 ).contraindicated

The recommended dose of SUPPRELIN LA is one implant every 12 months. The implant is inserted subcutaneously in the inner aspect of the upper arm and provides continuous release of histrelin for 12 months of hormonal therapy ( 2 ). 2.1 Recommended Dose The recommended dose of SUPPRELIN LA is one implant every 12 months. Each implant contains 50 mg histrelin acetate. The implant is inserted subcutaneously in the inner aspect of the upper arm and provides continuous release of histrelin acetate (65 mcg/day) for 12 months of hormonal therapy. SUPPRELIN LA should be removed after 12 months of therapy (the implant has been designed to allow for a few additional weeks of histrelin acetate release, in order to allow flexibility of medical appointments). At the time an implant is removed, another implant may be inserted to continue therapy. Discontinuation of SUPPRELIN LA should be considered at the discretion of the physician and at the appropriate time point for the onset of puberty (approximately 11 years for females and 12 years for males). 2.2 Recommended Procedure for Implant Insertion and Removal This procedure section is intended to provide guidance for the insertion and removal of SUPPRELIN LA. The actual procedure used, however, is at the discretion of the qualified healthcare provider performing the procedure. Insertion of a new implant can proceed using the following Suggested Insertion Procedure . If a previous SUPPRELIN LA implant must first be removed, please see the Suggested Removal Procedure instructions below.

Initial Agnostic Action: Initial transient increases of estradiol and/or testosterone may cause a temporary worsening of symptoms ( 5.1 ). Implant Breakage: Have been observed during implant removal. Monitor luteinizing hormone, follicle stimulating hormone or testosterone for suppression of CPP ( 5.2 , 5.6 ) Psychiatric Events: Have been reported in patients taking GnRH agonists. Events include emotional lability, such as crying, irritability, impatience, anger, and aggression. Monitor for development or worsening of psychiatric symptoms. ( 5.3 ) Convulsions: Have been observed in patients receiving GnRH agonists with or without a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies or tumors, and in patients on concomitant medications that have been associated with convulsions. ( 5.4 ) Severe Cutaneous Adverse Reactions: Have been reported in patients receiving GnRH agonists. Interrupt SUPPRELIN LA if signs or symptoms of severe cutaneous adverse reactions develop. Permanently discontinue SUPPRELIN LA if a severe cutaneous adverse reaction is confirmed. ( 5.5 ) Pseudotumor Cerebri (Idiopathic Intracranial Hypertension): Have been reported in pediatric patients receiving GnRH agonists. Monitor patients for headache, papilledema, and blurred vision. ( 5.6 ) 5.1 Initial Agonistic Action SUPPRELIN LA, like other GnRH agonists, initially causes a transient increase in serum concentrations of estradiol in females and testosterone in both sexes during the first week of treatment.

The following serious adverse reactions are described here and elsewhere in the label: Initial Agonist Action [see Warnings and Precautions ( 5.1 )] Implant Breakage [see Warnings and Precautions ( 5.2 )] Psychiatric Events [see Warnings and Precautions ( 5.3 )] Convulsions [see Warnings and Precautions ( 5.4 )] Severe Cutaneous Adverse Reactions [see Warnings and Precautions ( 5.5 )] Pseudotumor Cerebri (Idiopathic Intracranial Hypertension) [see Warnings and Precautions ( 5.6 )] The most common adverse reaction is implant site reaction (51.1%), including complications related to the insertion or removal of the implant ( 6 ). Adverse events related to suppression of endogenous sex steroid secretion may occur ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Endo at 1-800-462-3636 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Overall Adverse Reaction Profile The most common adverse reactions with SUPPRELIN LA involved the implant site. Local reactions after implant insertion include bruising, pain, soreness, erythema and swelling. During the early phase of therapy, gonadotropins and sex steroids rise above baseline because of the natural stimulatory effect of the drug. Therefore, an increase in clinical signs and symptoms may be observed [see Warnings and Precautions ( 5.1 )] .

Use of SUPPRELIN LA in children less than 2 years of age is not recommended ( 8.4 ). 8.1 Pregnancy Risk Summary SUPPRELIN LA is contraindicated during pregnancy [see Contraindications ( 4 )] since expected hormonal changes that occur with SUPPRELIN LA treatment increase the risk for pregnancy loss. The limited data with histrelin use in pregnant women are insufficient to determine a drug-associated risk for major birth defects or adverse developmental outcomes. Consistent with mechanism of action for SUPPRELIN LA [see Clinical Pharmacology ( 12.1 )], animal reproduction studies showed an increase in fetal loss at clinically relevant exposures. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data Histrelin acetate administered to pregnant rats during the period of organogenesis increased fetal mortality and post-implantation loss at doses of 1, 3, 5 or 15 mcg/kg/day, approximating clinical exposure based on body surface area. These dosages also reduced maternal body weight gain, stimulated ovarian follicular development, increased placental weight and caused abnormal morphology and an increase in fetal size.

Metabolism

Pharmacokinetics of histrelin after implantation of SUPPRELIN LA was evaluated in a total of 47 children with CPP (11 subjects in Study 1 and 36 subjects in Study 2). Patients were examined at 4 weeks after implant insertion and a few times throughout the treatment period.

There have been no reports of overdose in SUPPRELIN LA clinical trials. High doses of histrelin acetate injection in animal studies were generally associated only with effects attributed to the expected pharmacology. The method of drug delivery makes accidental or intentional overdosage unlikely.

• May 3, 2007NDANDA022058Endo Operations

1. 1Drug Ineffective13616%
2. 2Device Breakage11513%
3. 3Procedural Complication849.7%
4. 4Incorrect Drug Administration Duration667.6%
5. 5Incorrect Product Administration Duration586.7%
6. 6Rash465.3%
7. 7Implant Site Rash414.7%
8. 8Headache384.4%
9. 9Off Label Use323.7%
10. 10Weight Increased313.6%
11. 11Mood Swings283.2%
12. 12Device Expulsion273.1%
13. 13Implant Site Pain273.1%
14. 14Implant Site Infection232.7%
15. 15Rash Pruritic232.7%

The 10 most recently updated of 15 ClinicalTrials.gov registrations naming Histrelin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score, The Guidance Trial
  Active not recruiting · Phase 3 · Interventional · 2,050 enrolled · NRG Oncology
  NCT05050084updated 2026-05-04
• Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
  Active not recruiting · Phase 3 · Interventional · 2,753 enrolled · NRG Oncology
  NCT04513717updated 2026-05-04
• Stereotactic Body Radiation Therapy Plus Immediate or Delayed Androgen Receptor Pathway Inhibitor and Androgen Deprivation Therapy or Salvage Radiation Therapy for the Treatment of Prostate Cancer, DIVINE Trial
  Recruiting · Phase 2 · Interventional · 532 enrolled · Mayo Clinic
  NCT06378866updated 2026-04-20
• Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-directed Local Therapy for Oligometastatic pRosTate Cancer
  Recruiting · Phase 2 · Phase 3 · Interventional · 464 enrolled · VA Office of Research and Development
  NCT04787744updated 2026-04-08
• Skeletal Health and Bone Marrow Composition Among Youth
  Terminated · Interventional · 78 enrolled · Amy DiVasta, MD
  NCT04203381updated 2026-04-03
• Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer
  Recruiting · Phase 3 · Interventional · 1,273 enrolled · SWOG Cancer Research Network
  NCT03678025updated 2025-09-11
• Enzalutamide Versus Standard Androgen Deprivation Therapy for the Treatment Hormone Sensitive Prostate Cancer
  Completed · Phase 2 · Interventional · 19 enrolled · University of Colorado, Denver
  NCT02278185updated 2025-05-11
• A Study Called AWARENESS Using Data From Men in Alberta to Observe Treatment Patterns for Metastatic Castration-sensitive Prostate Cancer
  Completed · Observational · 960 enrolled · Bayer
  NCT05149131updated 2024-02-09
• Vantas Implant Retrieval Study
  Completed · Observational · 12 enrolled · Endo USA Inc., a Keenova Therapeutics Company
  NCT01013025updated 2024-01-02
• Study of Histrelin Subdermal Implant in Patients With Prostate Cancer
  Completed · Phase 3 · Interventional · 59 enrolled · Endo USA Inc., a Keenova Therapeutics Company
  NCT01394263updated 2024-01-02

Frequently asked questions

How does Histrelin work?

SUPPRELIN LA is a GnRH agonist and an inhibitor of gonadotropin secretion when given continuously. It delivers approximately 65 mcg histrelin acetate per day.

What is Histrelin used for?

According to FDA labeling, Histrelin carries indications including: SUPPRELIN LA (histrelin acetate) subcutaneous implant is indicated for the treatment of children with central precocious puberty (CPP). Children with CPP (neurogenic or idiopathic) have an early onset of secondary sexual characteristics (earlier than 8 years of age in females and 9 years of age in males).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Histrelin?

Histrelin is classified as Gonadotropin releasing hormone analogues, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Decreased Follicle Stimulating Hormone Secretion, Decreased GnRH Secretion, Decreased Luteinizing Hormone Secretion, Decreased Ovarian Estrogen Secretion, Decreased Testosterone Secretion.

What are the brand names for Histrelin?

Histrelin is marketed under brand names including Supprelin.

What are the contraindications for Histrelin?

Histrelin labeling lists contraindications including: SUPPRELIN LA is contraindicated in: Patients who are hypersensitive to gonadotropin releasing hormone (GnRH) or GnRH agonist analogs Pregnancy [see Use in Specific Populations ( 8.1 )] . History of hypersensitivity to gonadotropin releasing hormone (GnRH) or GnRH analogs ( 4 ).. Always consult the full prescribing information and a clinician.