Peptifact

Gonadorelin Dosage: Every Human Dose Record Is a Pump Schedule, and the Interval Matters More Than the Amount

Both US human gonadorelin products are discontinued. Every current US label for the molecule is a cattle label. The human dose record is 1-20 micrograms per pulse delivered by pump every 90 to 120 minutes, and the interval is not a detail: continuous exposure to the same molecule suppresses the hormones that pulsatile exposure releases.

Robert F · Edited by Caroline S · Published 2026-09-21

Illustration: An open insulated shipping box with a clear glass vial containing lyophilized powder.
Illustration

Gonadorelin has a dose record with an unusual shape. The amounts in it are small and consistent — single-digit to low-double-digit micrograms. What varies, and what almost nothing written about this compound carries, is the interval, and the interval is the part that decides whether the molecule switches the pituitary on or off.

Before that, a fact about the label situation that is easy to get wrong in the other direction.

There is no current US human label for this molecule

Both US human products are discontinued. From Drugs@FDA, read on 21 September 2026:

Application Brand Sponsor Strengths Marketing status
NDA 018123 FACTREL Hikma 0.1 mg, 0.2 mg, 0.5 mg per vial Discontinued
NDA 019687 LUTREPULSE KIT Ferring 0.8 mg, 3.2 mg per vial Discontinued

The approvals are still in the database. The products are not on the market. Those are two different statements, and a page that cites "an FDA-approved drug" without checking the second one is describing a filing cabinet rather than a pharmacy.

Every current US gonadorelin label is a cattle label

A DailyMed search for gonadorelin on the same date returns five current labels:

Label Holder Species
FACTREL Injection Zoetis Cattle
GONABREED Parnell Technologies Cattle
CYSTORELIN Boehringer Ingelheim Animal Health Cattle
FERTAGYL Merck Animal Health Cattle
OVACYST Bimeda Cattle

All five. The brand name FACTREL now belongs to a Zoetis product for dairy cows, which is why a search for the historic human brand lands on a livestock label without anything on the page announcing the change.

The CYSTORELIN warnings section reads, in its entirety:

Not for use in humans.

So the only currently labelled doses of gonadorelin in the United States are these:

Product Indication Dose
CYSTORELIN Cystic ovaries, lactating dairy and beef cows 100 μg (2 mL) per cow, intravenous or intramuscular
CYSTORELIN Reproductive synchrony, with cloprostenol 100 μg per cow IM at Day 0, second dose 30–72 h after the cloprostenol injection
FACTREL Ovarian follicular cysts 2 mL as a single intramuscular injection
FACTREL Fixed-time AI with dinoprost 100–200 μg (2–4 mL) per cow IM, two doses 6–8 days apart around the prostaglandin

These are real doses in a real regulatory document, and they establish nothing about a person.

The human record: micrograms per pulse, by pump

The human literature is not a label literature. It is a small set of endocrinology trials, and in all of them the delivery device is part of the dose.

Source Population Dose Interval Route
J Clin Endocrinol Metab 2015;100(7):2793–9 (PMID 25978110) 12 adolescent boys with hypogonadotropic hypogonadism 8–10 μg every 90 min subcutaneous, pump
Eur J Endocrinol 1994;131(4):347–54 (PMID 7921222) men 5–20 μg every 120 min subcutaneous
Lancet 1987;2(8558):552–5 (PMID 2887840) girls and boys with delayed puberty 1–2 μg (girls), 2–4 μg (boys) per pulse
Fertil Steril 1985;43(4):599–608 (PMID 3921412) boys with idiopathic delayed puberty 25 μg IV test dose; then 2 μg every 2½ h subcutaneous
J Clin Endocrinol Metab 1984;59(4):739–46 (PMID 6384253) 14 hypogonadotropic patients 5 μg bolus; 3.17 μg/h infusion SC and IV compared

The 2015 trial is the most recent and the most complete. Twelve patients at Beijing Children's Hospital received 8–10 μg of gonadotropin-releasing hormone subcutaneously every 90 minutes using a pump, for 12 to 14 months, alongside 22 patients on intramuscular human chorionic gonadotropin. The gonadorelin arm showed larger testicular volume; testosterone and penile length did not differ significantly between the arms.

Note what the dose figure is attached to in every row: a pump, a schedule, and a duration measured in months.

The interval is the pharmacology

This is the part worth being precise about, because it inverts.

Pulsatile gonadotropin-releasing hormone stimulates the pituitary to release luteinising hormone and follicle-stimulating hormone. A continuous stimulus at the same receptor desensitises it and blocks that release.

Kumar and Sharma, J Hum Reprod Sci 2014;7(3):170–4, state it in exactly those terms: pituitary stimulation with pulsatile GnRH induces both FSH and LH, and pituitary gonadotropin secretions are blocked upon desensitisation when a continuous GnRH stimulus is provided.

That mechanism is not a footnote. It is the entire basis of the GnRH-agonist class — the drugs given precisely to shut down sex-hormone production, which achieve it by delivering the same signalling molecule without the gaps. The molecule does not change. The schedule does.

So a gonadorelin figure quoted without its interval has lost the variable that determines the direction of the effect. A microgram number on its own is not a dose for this compound in the way it is for most of the compounds on this site's dosage chart — it is half of one.

Route changes the curve, and that was measured

Handelsman and colleagues ran the comparison in 1984 because pulsatile treatment was producing deficient responses by the subcutaneous route in contrast to the intravenous route, and nobody knew whether bioavailability alone explained it.

Fourteen hypogonadotropic patients, 5 μg boluses:

Intravenous Subcutaneous
Peak plasma IR-GnRH 400 pg/mL 93.5 pg/mL
Return to baseline < 60 min > 120 min

The subcutaneous route produced a lower, later, flatter curve — lower between 1 and 5 minutes, higher between 30 and 90 minutes. For a hormone whose effect depends on the pituitary seeing a sharp pulse followed by a gap, a flattened curve is not a smaller dose of the same thing.

What the record does not contain

No study in this site's sources administered gonadorelin to healthy adults on a once- or twice-weekly schedule. The human trials are in people with a specific hypothalamic defect, dosed around the clock by pump for months, with an endpoint — puberty, testicular volume, ovulation — that the deficiency itself defines.

The half-life chart carries this compound with the same caveat, and how to read a dosing claim sets out why a figure detached from its schedule and population is not a transferable number. The comparison this compound is most often set against, human chorionic gonadotropin, has its own record on this site's HCG dosage page, and it is a genuinely different document: an approved drug with a current human label.

Method

Drugs@FDA was queried through the openFDA API on 21 September 2026 for application numbers NDA 018123 and NDA 019687 and for products matching the brand names FACTREL and LUTREPULSE; marketing status is quoted from the product records returned. The DailyMed SPL service was queried the same day for drug_name=gonadorelin; five labels were returned and each title is reproduced above with its holder. The CYSTORELIN and FACTREL veterinary dose and warning text is quoted from those labels directly. Every human figure is cited to the paper it was read from by PMID, journal, volume and page, and each abstract was opened rather than taken from a result list. Nothing on this page is a dosing instruction.

Frequently asked questions

What is the dose of gonadorelin?

There is no current US human label to read a dose from, because both US human products are discontinued. In the published human literature the dose is stated per pulse and is small: 8 to 10 micrograms subcutaneously every 90 minutes by pump in a 2015 trial in twelve adolescent boys, 5 to 20 micrograms every 120 minutes in a 1994 study in men, 1 to 4 micrograms per pulse in children. The only current US labelled figure for the molecule is a veterinary one, 100 to 200 micrograms per cow intramuscularly. This site reports those figures as record and none of them as guidance.

Is gonadorelin an approved drug?

It was, and the approvals still exist on paper while the products do not. Drugs@FDA lists FACTREL under NDA 018123 in 0.1, 0.2 and 0.5 mg vials and LUTREPULSE KIT under NDA 019687 in 0.8 and 3.2 mg vials, and every one of those five product entries is marked Discontinued. An approval number is not evidence that a product is on the market, and anyone citing gonadorelin as an approved human drug should say which product and check its marketing status.

Why are all the gonadorelin labels veterinary?

Because the human products left the market and the cattle products did not. A DailyMed search on 21 September 2026 returns five current gonadorelin labels, from Zoetis, Parnell, Boehringer Ingelheim Animal Health, Merck Animal Health and Bimeda, all for reproductive use in cows. One of them, CYSTORELIN, carries the warning 'Not for use in humans.' The brand name FACTREL now belongs to a cattle product, which means a search for the historic human brand lands on a livestock label.

Does the dosing interval of gonadorelin matter?

It is the single most consequential variable in the record, more than the amount. Pulsatile delivery of gonadotropin-releasing hormone stimulates the pituitary to release luteinising hormone and follicle-stimulating hormone. A continuous stimulus at the same receptor desensitises it and blocks that release, which is the documented mechanism of the GnRH-agonist drug class used to suppress sex hormones. Every human dose in the published record is specified with its interval attached, most of them at 90 or 120 minutes, and a figure quoted without its interval has lost the part that determines the direction of the effect.

What is the half-life of gonadorelin?

Short, and the route changes the shape of the curve rather than only its height. The clearest published human comparison is Handelsman and colleagues in 1984: after a 5 microgram bolus, plasma immunoreactive GnRH peaked at 400 picograms per millilitre intravenously and 93.5 subcutaneously, and returned to baseline in under 60 minutes intravenously against more than 120 minutes subcutaneously. The same paper records that pulsatile treatment produced deficient responses by the subcutaneous route compared with the intravenous route, which is why it was run.

Is gonadorelin the same as an HCG alternative?

They are different molecules acting at different points, and the published trials treat them as alternatives to be compared rather than as substitutes. Gonadorelin is gonadotropin-releasing hormone and acts on the pituitary; human chorionic gonadotropin acts at the receptor further down, on the gonad. The 2015 trial in adolescent boys with hypogonadotropic hypogonadism ran both arms — twelve patients on pulsatile pump gonadorelin, twenty-two on intramuscular human chorionic gonadotropin — and reported larger testicular volume in the gonadorelin arm, with no significant difference in testosterone or penile length between the groups. That is one small non-randomised comparison in adolescents, not a general finding about adults.

Why is a cattle label in a dosage record at all?

Because it is the only current US label this molecule has, and omitting it would leave the impression that no labelled dose exists. A veterinary label is a real regulatory document with real pharmacology behind it, and the CYSTORELIN label carries acute toxicity figures in mice, rats and dogs that no human label ever published. What it cannot do is establish a human dose, and it says so itself in four words in its warnings section. Both statements belong on the page.