Histrelin (Supprelin LA)_Dosage, benefits & legal status
Also known as Supprelin LA, Supprelin, Vantas, histrelin acetate, ORF-17070, RWJ-17070
A modified GnRH, nine amino acids long, released steadily from a small implant for a year. The implant has been FDA-approved for central precocious puberty since 2007, after a daily injection first approved in 1991; the adult prostate cancer version, Vantas, stopped being made in 2021.
Common vial size is what vendors typically sell, not a recommendation. Enter your own vial in the calculator.
What is Histrelin (Supprelin LA)?
Plain language first. The technical label stays, but it never stands alone.Overview
Puberty that starts years too early speeds up bone aging and can cut adult height, and this implant puts it on hold a year at a time. In the 36-child pivotal trial, the pituitary signal fell to prepubertal levels by month 1 in every child not treated before and stayed there through month 12; with yearly implants, predicted adult height in girls rose from 151.9 to 166.5 cm by month 60 (6 girls). Inserting and removing it is minor surgery, the trials had no comparison group, and implants broke in 22.1% of removals in the long-term study.
Histrelin is a nonapeptide GnRH analog: native GnRH with 1-benzyl-D-histidine in place of glycine 6, glycine 10 deleted and proline 9 capped as an ethylamide. Released at about 65 mcg a day from a nonbiodegradable hydrogel implant, it first stimulates and then desensitizes pituitary GnRH receptors, so LH, FSH and sex steroids fall to prepubertal levels. Supprelin LA (NDA 022058, now Endo) has been approved since May 3, 2007, for children with central precocious puberty; Vantas, a 50 mg implant for advanced prostate cancer, is discontinued.
What it's used for
A small implant placed under the skin of the inner upper arm to pause central precocious puberty in children, removed after 12 months and replaced if treatment continues. Vantas, the adult implant for prostate cancer, is no longer made.
How does Histrelin (Supprelin LA) work?
What it does in the body, and where.Histrelin is a more potent version of GnRH, the brain hormone that tells the pituitary to run puberty, and a nonstop supply of it switches that signal off.
- 01A brief surgeHistrelin binds GnRH receptors on the pituitary and at first makes it release more LH and FSH, the hormones that drive the ovaries and testes, so estradiol and testosterone rise during the first week. Suppression generally follows within 4 weeks.
- 02Switching offThe implant releases histrelin without a break. Under constant stimulation the receptors are downregulated and the pituitary stops responding, and LH falls to prepubertal levels within a month.
- 03Puberty on holdWith little LH and FSH, the ovaries or testes make much less estradiol or testosterone, so puberty stalls and bone age advances more slowly. It reverses: LH returned to pubertal levels about 6 months after the last implant came out.
What else is it used for?
Each group carries its own evidence level.Approved means regulators have cleared it for that purpose. Investigational means it is in trials. Early research means it is being studied and is not established.
Central precocious puberty, first year
FDA-approved- Human trial36 children (20 untreated, 16 previously treated): peak stimulated LH fell from 28.2 to 0.8 mIU/mL by month 1 in the untreated group, and all stayed below the 4 mIU/mL goal through month 12.
- Human trialA second study in 11 previously treated girls aged 3.7 to 11.0, reported only in the Supprelin LA label, gave consistent results.
- No dataBoth trials were single-arm and open-label, with no placebo or comparator.
Six years of yearly implants
FDA-approved- Human trialNo stimulated LH above 2.3 mIU/mL on treatment; LH back in the pubertal range about 6 months after the last implant came out.
- Human trialPredicted adult height in girls rose from 151.9 cm at baseline to 166.5 cm at month 60 (6 girls).
- No dataImplants broke in 25 of 113 removals (22.1%); one benign pituitary tumor was judged possibly related, and one death (bronchopneumonia with Dravet syndrome) unrelated.
One implant for two years
Early research- Human trial33 children (29 completed): peak LH 0.89 IU/L at both 12 and 24 months, with all suppressed; predicted adult height SDS improved from -1.50 to -1.03 (P = .02).
- No dataRemoval was difficult in 12 cases (39%), including 6 breakages, and 2 removals needed general anesthesia.
Advanced prostate cancer (Vantas)
FDA-approved- Human trial138 men: testosterone at or below 50 ng/dL by day 28 in all 134 evaluable, and in all 115 with a week-52 value; breakthrough in 4 (3%); PSA normal by week 24 in 93%.
- Human trialHot flashes in 65.5% of 171 men; insertion-site reactions in 19 of 138 (13.8%), all mild; implants pushed out through the incision in 8 of 171 men in the first 12 months.
Histrelin is often said to have been first approved in 2007. May 3, 2007, is right for Supprelin LA, but histrelin was first approved on December 24, 1991, as the daily Supprelin injection, and first as an implant on October 12, 2004 (Vantas). It is sometimes called a decapeptide; it has nine residues and ends in an ethylamide. Both implants hold 50 mg, but Supprelin LA releases about 65 mcg a day and Vantas about 50 (56.7 measured), so their figures should not be merged. The current Supprelin LA label gives no half-life; the 3.92 hours often quoted comes from the Vantas label, measured after an injection in healthy adults. Vantas is not a current option: Endo stopped making it in September 2021, even though FDA records show label updates as late as May 2026. Breakage is sometimes described as rare, yet implants broke in 22.1% of removals in the 6-year study. The $43,000 against $4,800 price gap often quoted is from 2021, not a current list price.
The published record
Papers and trials about Histrelin (Supprelin LA)
80 papers tagged human · 49 not reviews or lab · 8 clinical trial publications
15 registered trials · 2 with posted results
Furthest stage reached: Approved in the US
Counted from Europe PMC indexing, not read by a person; a human tag can land on reviews, commentary or lab papers; clinical trial publications is the narrower count.
At a glance
Four things to know about Histrelin (Supprelin LA)
Evidence
FDA-approved
Category
Sexual and hormonal
Common vial
Varies
Half-life
3.92 hours (Vantas label); the implant releases for 12 months
How much, and do you cycle it?
The range, and whether you take breaks.One 50 mg implant every 12 months, releasing about 65 mcg a day (label), once every 12 months. Continuous, one implant a year until the usual age of puberty FDA label
Each implant is removed after 12 months and can be replaced at the same visit, and treatment stops around age 11 in girls or 12 in boys. Hormone suppression reverses after removal.
How long does it stay in the body?
The half-life, and where the figure comes from.3.92 hours (Vantas label); the implant releases for 12 monthsFDA label
Terminal half-life 3.92 hours, plus or minus 1.01, after an injection under the skin in healthy adult volunteers, from the Vantas label. The current Supprelin LA label gives no half-life; it reports a median peak blood level of 0.43 ng/mL in 47 children, sustained in most. In men given Vantas, levels peaked at a median of 12 hours (1.10 ng/mL), and the implant delivered 92% as much drug as an injection. How long it acts is set by the implant, not by the half-life.
Source: Vantas US prescribing information, clinical pharmacology (the Supprelin LA label gives no half-life)
You can compare this against the whole library to see where it sits.
How is it given?
Dosing context and source notes.Supplied as an implant or depot, so there is nothing to mix or draw.
Label dose: 50 mg per formulation. Supprelin LA US prescribing information (DailyMed, Endo, 2025)
One 50 mg Supprelin LA implant every 12 months, releasing about 65 mcg of histrelin acetate a day. A doctor places it under the skin of the inner upper arm through a single small cut, usually under local anesthesia (the label leaves local anesthesia, sedation or general anesthesia to the doctor), using a single-use insertion tool, and closes the cut with absorbable stitches or adhesive strips. It is removed after 12 months (it is built to release for a few extra weeks), and a new implant can go into the same pocket or a new site in either arm at the same visit; if it cannot be felt, ultrasound, CT or MRI can find it, as it does not show on plain X-rays. Treatment stops at the doctor's discretion around the usual age of puberty (about 11 in girls and 12 in boys). LH, FSH and estradiol or testosterone are checked 1 month after insertion and then every 6 months, with height and bone age every 6 to 12 months. No kidney or liver adjustment is given. Supplied as one implant in a vial of saline with a separate implantation kit; the implant is kept refrigerated at 2 to 8°C. It is a fixed implant placed by a doctor, so there is nothing for the calculator to draw. Vantas, the discontinued prostate cancer implant, held the same 50 mg but released about 50 mcg a day.
How do you store it?
Before mixing, and after.Follow the storage on the product label.
Histrelin (Supprelin LA) is supplied as a finished product, so its label sets the storage. Pens, prefilled syringes, implants, tablets and ready-made solutions are used as supplied. Kits that include a powder are mixed just before the dose and usually used straight away, not kept for weeks. Many injectable products go in the fridge and must not be frozen, while others are kept at room temperature, so check the pack or ask the pharmacist.
What are the side effects and cautions?
Known cautions and warnings for this compound.Solubility, computed: 33% charged residues, 33% hydrophobic. Water usually sufficient.
A first-pass rule from peptide manufacturers' guidance. It does not account for disulfide bridges, salt form or how the powder was dried, and it predicts what should be easy rather than what will happen in your vial.
Who should avoid it
- Allergy to GnRH or to GnRH agonist drugs
- Pregnancy (fetal loss in animal studies at clinically relevant exposures)
- Not recommended in children under 2 years old (a label caution, not a formal contraindication)
Stop and get help
- A blistering or peeling rash, or a rash with fever and swollen glands (possible severe skin reaction)
- Severe headache, blurred or double vision, or loss of vision (possible raised pressure inside the skull)
- A seizure, or new depression or thoughts of self-harm
Common effects
- Implant-site reactions in 24 of 47 children (51.1%): discomfort, bruising, soreness, pain, tingling, itching, protrusion or swelling; there was no placebo arm
- Keloid scar, other scarring and suture complications in 3 children each (6.4%); site pain and post-procedure pain in 2 each (4.3%)
- Irregular vaginal bleeding in 2 children; single cases of headache, migraine, breast tenderness, gynecomastia, mood swings, weight gain and wound infection
- Implants broke in 25 of 113 removals (22.1%) over 6 years of yearly implants
Where this page says nothing is established, that means nobody has studied it, not that a compound is safe.
Is Histrelin (Supprelin LA) approved?
And where the numbers on this page come from.Yes. Histrelin (Supprelin LA) is FDA approved and available on prescription in the United States.
- Approval statusFDA-approved
- RouteImplant under the skin of the upper arm, placed by a doctor
- Checked18 October 2026
- DoseFrom the drug label. The manufacturer tested this range and a regulator reviewed it.
- Vial sizeFrom what vendors typically list; not a recommendation.
- SourcesSupprelin LA US prescribing information (DailyMed, Endo)Drugs@FDA, NDA 022058 (Supprelin LA)Drugs@FDA, NDA 021732 (Vantas)Vantas US prescribing information (2026)Drugs@FDA, NDA 019836 (Supprelin injection)FDA GSRS substance record, histrelin (UNII H50H3S3W74)FDA orphan drug designation, histrelin for central precocious pubertyEugster EA et al., Journal of Clinical Endocrinology and Metabolism 2007;92:1697-1704Silverman LA et al., Journal of Clinical Endocrinology and Metabolism 2015;100:2354-2363Lewis KA et al., Journal of Pediatrics 2013;163:1214-1216EMA, Vantas Article 29(4) referralHealth Canada summary basis of decision, VantasKFF Health News, hormone blocker prices (November 10, 2021)Endo completes acquisition of Indevus (March 23, 2009)
What has happened recently
Histrelin was first approved on December 24, 1991, as Supprelin, a daily injection under the skin (NDA 019836, a new molecular entity under priority review); Indevus later described it as previously approved for central precocious puberty, and all three strengths are discontinued. Vantas, a 50 mg yearly implant developed by Valera Pharmaceuticals, was approved on October 12, 2004, for palliative treatment of advanced prostate cancer and launched that November. Indevus agreed to buy Valera on December 12, 2006, completed the merger on April 18, 2007, and won approval of Supprelin LA (NDA 022058) for central precocious puberty on May 3, 2007, after an orphan designation on November 18, 2005; orphan exclusivity ended May 3, 2014. Endo completed its acquisition of Indevus on March 23, 2009, and Endo USA is the current labeler (label effective September 25, 2025). In September 2021 Endo told the FDA it had permanently stopped making Vantas after batches failed to meet standards; Drugs@FDA lists it as discontinued, though its label was still updated in 2025 and May 2026. There are no generics. Abroad, only the Vantas implant was approved: Denmark authorized it on November 17, 2005, an EU referral ended with a European Commission decision on July 30, 2007, for mutual recognition in Germany, Spain, Ireland, Italy and the UK, and Health Canada approved it on March 10, 2006. Whether it is still sold anywhere after the 2021 manufacturing stop is not established, and no approval of Supprelin LA outside the US was found.
You can compare this against the whole library, or read how to check a seller.
What else is like Histrelin (Supprelin LA)?
Others in Sexual and hormonal, side by side.If you're weighing Histrelin (Supprelin LA), it's worth reading Lanreotide (Somatuline Depot), Leuprolide (Lupron), and Lutetium-177 dotatate (Lutathera) in the same class.
A modified GnRH, nine amino acids long, released steadily from a small implant for a year. The implant has been FDA-approved for central precocious puberty since 2007, after a daily injection first approved in 1991; the adult prostate cancer version, Vantas, stopped being made in 2021.
- Dose
- One 50 mg implant every 12 months, releasing about 65 mcg a day (label)
- How often
- Once every 12 months
An approved monthly somatostatin shot that lowers growth hormone and slows some gut and pancreatic tumors.
- Dose
- 60 to 120 mg every 4 weeks (label)
- How often
- Every 4 weeks (6 to 8 weeks for some acromegaly patients)
The GnRH agonist that shuts hormones down by overstimulating them first.
- Dose
- Set by the label and the depot formulation
- How often
- Monthly to six-monthly depot
A peptide used as a delivery van: it finds tumor cells with somatostatin receptors and irradiates them from the inside.
- Dose
- 7.4 GBq every 8 weeks, 4 doses (label)
- How often
- Every 8 weeks, for 4 doses
Guides for this compound
- How to Reconstitute a Peptide
Mix peptide powder with bacteriostatic water, step by step.
- How to Read an Insulin Syringe
Read the units, convert to millilitres, and draw the exact dose.
- mcg vs mg: The Peptide Dosing Mistake to Avoid
Your vial says mg and your protocol says mcg. Here is the conversion and how to check it.
Sources
- Supprelin LA US prescribing information (DailyMed, Endo)(2025)Central precocious puberty; one 50 mg implant every 12 months releasing about 65 mcg a day; implant-site reactions 51.1% of 47 children; no half-life given.
- Drugs@FDA, NDA 022058 (Supprelin LA)(2025)Approved May 3, 2007; new formulation, orphan; labeling supplements through September 23, 2025; no generics.
- Drugs@FDA, NDA 021732 (Vantas)(2026)Approved October 12, 2004, for advanced prostate cancer; discontinued; labeling supplements to May 6, 2026.
- Vantas US prescribing information (2026)(2026)Half-life 3.92 hours after an injection in healthy volunteers; castrate testosterone by day 28 in 100% of 134 evaluable men; hot flashes 65.5%; implants extruded in 8 of 171 men.
- Drugs@FDA, NDA 019836 (Supprelin injection)(1991)First histrelin approval, December 24, 1991; new molecular entity; all strengths discontinued.
- FDA GSRS substance record, histrelin (UNII H50H3S3W74)(2026)C66H86N18O12, MW 1323.5; structure with 1-benzyl-D-histidine at 6 and proline ethylamide at 9.
- FDA orphan drug designation, histrelin for central precocious puberty(2007)Designated November 18, 2005; orphan exclusivity ended May 3, 2014.
- Eugster EA et al., Journal of Clinical Endocrinology and Metabolism 2007;92:1697-1704(2007)36 children: peak stimulated LH fell from 28.2 to 0.8 mIU/mL by month 1 in the 20 untreated; suppression held in all through month 12.
- Silverman LA et al., Journal of Clinical Endocrinology and Metabolism 2015;100:2354-2363(2015)Up to 6 years of yearly implants: no on-treatment LH above 2.3 mIU/mL; predicted adult height in girls 151.9 to 166.5 cm; breakage in 22.1% of removals (NCT00779103).
- Lewis KA et al., Journal of Pediatrics 2013;163:1214-1216(2013)33 children: one implant kept suppression for 2 years (peak LH 0.89 IU/L at 12 and 24 months); difficult removal in 39%.
- EMA, Vantas Article 29(4) referral(2007)Danish authorization November 17, 2005; positive CHMP opinion May 24, 2007; Commission decision July 30, 2007.
- Health Canada summary basis of decision, Vantas(2006)Notice of Compliance March 10, 2006, to Paladin Labs, for advanced hormone-dependent prostate cancer.
- KFF Health News, hormone blocker prices (November 10, 2021)(2021)Endo stopped making Vantas in September 2021; Supprelin LA about $43,000 an implant against about $4,800 for Vantas.
- Endo completes acquisition of Indevus (March 23, 2009)(2009)Supprelin LA and Vantas passed to Endo with Indevus.
Beyond these, 150 records are indexed. Browse the records