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Supprelin LA (histrelin acetate) subcutaneous implant

Summary about Supprelin LA

Supprelin long-acting (LA) is a sterile, non-biodegradable, diffusion-controlled, MedLaunchTM polymer reservoir containing histrelin acetate, a synthetic nonapeptide analog of the naturally occurring gonadotropin releasing hormone (GnRH) possessing a greater potency than the natural sequence hormone.

Supprelin LA is designed to deliver approximately 65 mcg histrelin acetate per day over 12 months. The implant looks like a small thin flexible tube and consists of a 50-mg histrelin acetate drug core inside a 3.5 cm by 3 mm, cylindrical, MedLaunchTM polymer reservoir.

Figure 1: Supprelin LA implantation kit (Source:

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). They also show a significantly advanced bone age that can result in diminished adult height attainment.

Prior to initiation of treatment, a clinical diagnosis of CPP should be confirmed by measurement of blood concentrations of total sex steroids, luteinizing hormone (LH) and follicle stimulating hormone (FSH) following stimulation with a GnRH analog, and assessment of bone age versus chronological age. Baseline evaluations should include height and weight measurements, diagnostic imaging of the brain (to rule out intracranial tumor), pelvic/testicular/adrenal ultrasound (to rule out steroid secreting tumors), human chorionic gonadotropin levels (to rule out a chorionic gonadotropin secreting tumor), and adrenal steroids to exclude congenital adrenal hyperplasia.

Supprelin LA is contraindicated in patients who are hypersensitive to gonadotropin releasing hormone (GnRH) or GnRH agonist analogs and in females who are or may become pregnant while receiving the drug. Supprelin LA may cause fetal harm or spontaneous abortion when administered to pregnant patients. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus.

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, with worsening or onset of new symptoms during this period. Within 4 weeks of therapy, gonadal steroid suppression occurs and manifestations of puberty decrease.



Implant insertion and removal is a surgical procedure and should utilize aseptic technique. Careful adherence to the recommended insertion and removal procedures is recommended to avoid potential complications. Proper surgical technique is critical in minimizing adverse events related to the insertion and the removal of the histrelin implant. On occasion, localizing and/or removal of implant products have been difficult and imaging techniques were used including ultrasound, CT, or MRI (this implant is not radiopaque). In some cases, the implant broke during removal and multiple pieces were recovered. Rare events of spontaneous extrusion have been observed in clinical trials. During Supprelin LA treatment, patients should be evaluated for evidence of clinical and biochemical suppression of CPP manifestation.

Psychiatric events have been reported in patients taking GnRH agonists, including Supprelin LA. Postmarketing reports with this class of drugs include symptoms of emotional lability, such as crying, irritability, impatience, anger, and aggression. Depression, including rare reports of suicidal ideation and attempt, has been reported for GnRH agonists, including Supprelin LA, in children treated for central precocious puberty. Many, but not all, of these patients had a history of psychiatric illness or other comorbidities with an increased risk of depression. Monitor for development or worsening of psychiatric symptoms during treatment with Supprelin LA.

Postmarketing reports of convulsions have been observed in patients receiving GnRH agonists, including Supprelin LA. Reports with GnRH agonists have included patients with a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies or tumors, and patients on concomitant medications that have been associated with convulsions such as bupropion and SSRIs. Convulsions have also been reported in patients in the absence of any of the conditions mentioned above.

LH, FSH and estradiol or testosterone should be monitored at 1 month post implantation, then every 6 months. Every 6-12 months, height and bone age should be assessed.

In clinical trials, the most common adverse reactions involved the implant site and included discomfort, bruising, soreness, pain, tingling, itching, erythema, and implant area protrusion and swelling.

The safety and effectiveness in pediatric patients under the age of 2 years have not been established. The use of Supprelin LA in children under 2 years is not recommended.


Supprelin LA (histrelin acetate)

Active Ingredient

Histrelin acetate

Administration Route


Alcohol Warning

No data about interaction

Available Strength

SUPPRELIN LA is a sterile, nonbiodegradable, diffusion-controlled, hydrogel polymer reservoir drug delivery system designed to deliver histrelin acetate continuously for 12 months after subcutaneous implantation. The sterile implant contains 50 mg histrelin acetate and delivers approximately 65 mcg histrelin acetate per day over 12 months.

Breastfeeding Warning

Not indicated for use in adult women.

Excreted into human milk: Unknown
Excreted into animal milk: Data not available

The effects in the nursing infant are unknown.

Clinical Pharmacology


Long-term treatment with histrelin acetate suppresses the LH response to GnRH causing LH levels to decrease to prepubertal levels within 1 month of treatment. As a result, serum concentrations of sex steroids (estrogen or testosterone) also decrease. Consequently, secondary sexual development ceases to progress in most patients. Additionally, linear growth velocity is slowed which improves the chance of attaining predicted adult height


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. Median serum histrelin concentrations remained above the limit of quantification for the treatment period. Histrelin acetate levels were sustained throughout the study period for most subjects. The median of maximum serum histrelin concentrations over the study period was 0.43 ng/mL, which is expected to maintain gonadotropins at prepubertal levels. There was no apparent pharmacokinetic difference between naïve subjects to a LHRH agonist treatment and subjects who had previous treatment with a LHRH agonist.


Approximate Retail Price according to

Subcutaneous implant:

  • 50 mg (1 implant): $37,194.78

Dosage Form

Subcutaneous implant

Dose Schedule

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.

Drug Class

L02AE – Gonadotropin releasing hormone analogues

Drug Unit


Food Warning

No formal drug-drug, drug-food, or drug-herb interaction studies were performed with SUPPRELIN LA

Included In
Health Insurance Plan

The majority of patients enrolled in the SHARES Copay Assistance Program pay $10 a year for SUPPRELIN® LA. For those who exceed the $2,000 amount, they may be eligible for additional assistance.

Find out more here

Interacting Drugs

Overview: No formal drug-drug, drug-food, or drug-herb interaction studies were performed with SUPPRELIN LA.

Drug-Laboratory Interactions: Therapy with SUPPRELIN LA results in suppression of the pituitary-gonadal system. Results of diagnostic tests of pituitary gonadotropic and gonadal functions conducted during and after SUPPRELIN LA therapy may be affected. SUPPRELIN LA decreased mean serum insulin-like growth factor-1 (IGF-1) levels by approximately 11% in one study. SUPPRELIN LA increased the serum concentration of dehydroepiandrosterone (DHEA) in 8 of 36 patients in another study

Is Available Generically

No. There is currently no therapeutically equivalent version of Supprelin LA available.

Is Proprietary


Label Details

Legal Status


Is not subject to the Controlled Substances Act.


Endo Pharmaceuticals Solutions Inc.

Maximum Intake

One implant per year

Mechanism of Action

Histrelin is a gonadotropin releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant that delivers continuous therapeutic doses. Following an initial stimulatory phase with increased circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a transient increase in concentration of gonadal steroids (testosterone and dihydrotestosterone in males), continuous administration of histrelin acetate results in decreased levels of LH and FSH due to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes.

Non Proprietary Name

Histrelin acetate


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.

Pregnancy Category

US FDA pregnancy category X: Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.

Pregnancy Warning

This drug can cause fetal harm when administered to a pregnant woman. Spontaneous abortions may occur. Major fetal abnormalities, increased fetal mortality, decreased fetal weights, and reduced fertility have been observed in animal studies. In nonclinical studies, histrelin was teratogenic and fetotoxic.

Prescribing Info

Prescription Status

Prescription drug

Proprietary Name

Supprelin LA

Related Drugs

Bicalutamide, Leuprolide, Triptorelin, Goserelin, Buserelin




Initial Agonistic Action: Initial transient increases of estradiol and/or testosterone may cause a temporary worsening of symptoms