Gonadorelin

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

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The FDA has approved gonadorelin in the past (Factrel — gonadorelin hydrochloride for diagnostic use; LutrePulse — gonadorelin acetate for ovulation induction), but both brand products were voluntarily withdrawn by manufacturers and are no longer available. The approved status on record means gonadorelin is NOT subject to the FDA Category 2 bulk drug substance prohibition that applies to unapproved peptides. Compounding pharmacies operating under Section 503A of the FD&C Act can prepare gonadorelin by prescription for individual patients. The PCAC (Pharmacy Compounding Advisory Committee) is reviewing GnRH-related substances in the context of the July 23–24 2026 meeting (docket FDA-2025-N-6895) concerning 503A bulk drug substance nominations; the outcome may further clarify the compounding pathway. The compound carries fda19=false.

Confirmed high-severity market-integrity event (enforcement / recall / counterfeit)

Transparent blend · bci-1.0 · never paid-placement

Primary name

Gonadorelin

Origin

Gonadorelin is a synthetic replicate of the endogenous hypothalamic gonadotropin-releasing hormone (GnRH, also termed LHRH), a 10-amino-acid peptide first isolated and sequenced by Schally and Guillemin (Nobel Prize 1977). The compound is chemically identical to the human native sequence (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2), with CAS 33515-09-2. It was previously marketed as Factrel (gonadorelin hydrochloride, Wyeth) and LutrePulse (gonadorelin acetate) in the United States, both subsequently withdrawn from the market by their manufacturers; no FDA-approved formulation is currently available for human use in the US despite the original approved status on record.

Registry IDs

PubChem CID

638793

CAS

33515-09-2

InChIKey

XLXSAKCOAKORKW-AQJXLSMYSA-N

ChEMBL

CHEMBL1007

Molecular formula

C55H75N17O13

Molar mass

1182.3 g/mol

Monoisotopic

1181.57302551 Da

InChIKey

XLXSAKCOAKORKW-AQJXLSMYSA-N

Appearance

White to off-white lyophilized powder

Solubility

Freely soluble in water; soluble in dilute acetic acid. Molecular weight 1182.3 …

Sequence not available in current seed.

Stability: The native decapeptide sequence is susceptible to endopeptidase degradation in solution. Lyophilized form is stable under recommended cold-chain conditions. Rec

Vial sizes

1 mg · 2 mg

Purity grades

≥98% (HPLC)

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• Gonadorelin binds the GnRH receptor, a Gq/11-coupled seven-transmembrane G-protein-coupled receptor expressed on anterior pituitary gonadotroph cells, activating phospholipase C and triggering inositol-1,4,5-trisphosphate-mediated intracellular calcium mobilization together with protein kinase C activation
• The resulting signal cascade drives both the acute secretion of pre-formed LH and FSH and the longer-term transcription and synthesis of gonadotropin subunits
• Critically, the biological effect is pattern-dependent: pulsatile receptor stimulation (mimicking the natural hypothalamic pulse interval of approximately 60–120 minutes) sustains gonadotropin release and downstream gonadal steroidogenesis, whereas continuous or non-pulsatile receptor occupancy causes rapid receptor desensitization, downregulation, and paradoxical suppression of LH, FSH, and sex steroids
• This dichotomy underpins both its therapeutic use in hypogonadotropic hypogonadism and the pharmacological principle behind long-acting GnRH agonist analogues used for androgen deprivation

Pharmacokinetics (ADME)

Half-life

IV distribution half-life approximately 2–10 minutes; terminal half-life approximately 10–40 minutes. After subcutaneous administration, absorption from the depot site extends effective half-life to approximately 30–60 minutes.

Clearance

Rapid proteolysis by plasma and tissue endopeptidases to constituent amino acids and small inactive peptides; excreted primarily via urine. Hepatic first-pass metabolism is substantial.

PK–PD note: The ultrashort plasma half-life is physiologically appropriate: rapid clearance permits inter-pulse troughs that prevent receptor desensitization. Pulsatile pump delivery (e.g., every 90–120 minutes) …

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Spermatogenesis of Male Patients with Congenital Hypogonadotropic Hypogonadism Receiving Pulsatile Gonadotropin-Releasing Hormone Therapy Versus Gonadotropin Therapy: A Systematic Review and Meta-Analysis (World J Mens Health) — Anchoring systematic review/meta-analysis; pooled spermatogenesis rate 77% (95% CI 63-87%) for pulsatile GnRH vs 68% (95% CI 58-77%) for HCG/HMG across 48 + 16 studies.
• Zhang L et al. The Pulsatile Gonadorelin Pump Induces Earlier Spermatogenesis Than Cyclical Gonadotropin Therapy in CHH Men (Am J Mens Health, 2018) — Nonrandomized comparative study, 28 males; PGP median spermatogenesis 6 mo vs 14 mo CGT (p=0.01). Not an RCT.
• [Spermatogenesis of pulsatile gonadotropin-releasing hormone infusion versus gonadotropin therapy in male idiopathic hypogonadotropic hypogonadism] (PubMed) — Comparative study; spermatogenesis success 50% (20/40) GnRH vs 28.8% (15/52) HCG/HMG (P=0.038).
• DrugBank DB00644 — Gonadorelin: Uses, Interactions, Mechanism of Action — Reference pharmacology: synthetic GnRH used to test gonadotrope/pituitary function; GnRH receptor agonist.

5 registered trials — 1 currently recruiting.

Phase 2
NCT00383656
Pulsatile GnRH in Anovulatory Infertility

UNKNOWN

Phase 3
NCT00667069
Triptorelin and Radiation Therapy in Treating Patients Who Have Undergone Surgery for Intermediate-Risk Stage III or Stage IV Prostate Cancer

COMPLETED

—
NCT02440802
Evaluation and Predictive Value of Genetic Polymorphisms in the Management of Hormonal Treatment of Prostate Cancer

UNKNOWN

NA
NCT03680053
Comparison of the Live Birth Rate Between the PPOS and the GnRH Antagonist Protocol in Patients Undergoing IVF

TERMINATED

Phase 2
NCT03942653
Androgen Deprivation Therapy (ADT) and Pembrolizumab for Advanced Stage Androgen Receptor-positive Salivary Gland Carcinoma

RECRUITING

Summary (literature)

The safety profile of gonadorelin is well-characterized from historical clinical use under the Factrel and LutrePulse approvals. Common adverse effects documented in clinical literature include local injection site reactions (pain, swelling, erythema), flushing, headache, and mil…

WADA status

Prohibited at all times (in-competition and out-of-competition) under WADA 2026 Prohibited List, Section S2 — Peptide Hormones, Growth Factors, Related Substanc…

Dominant research route: Subcutaneous (pulsatile infusion) and intravenous (diagnostic bolus) are the dominant studied routes in the licensed literature.

Human diagnostic use (LH-response pituitary function test); IV bolus 100 µg with serial LH sampling at 15/30/45/60/120 min

Bioavailability: Plasma half-life ~2–8 min (Handelsman & Swerdloff, 1986, Endocrine Reviews) following IV administration; Wikipedia/DrugBank cite 10–40 min elimination half-life; rapid enzymatic hydrolysis limits systemic exposure

IV is a licensed diagnostic route per the UK emc SmPC (Gonadorelin 100 micrograms powder for injection) for evaluating gonadotrope functional capacity; not a therapeutic dosing protocol.

Human diagnostic bolus and pulsatile SC infusion via portable pump (5–20 µg per pulse every 90–120 min) for hypothalamic hypogonadotropic hypogonadism

Bioavailability: Effective half-life estimated ~30–60 min after SC injection due to slower absorption from depot; pulsatile SC delivery approximates physiological GnRH secretion

SC is a licensed route in the emc SmPC (100 µg bolus) and is the route used in marketed pulsatile-infusion products (e.g., Lutrepulse) for GnRH-deficient infertility; described as study context only.

Human observational studies of intranasal gonadorelin (LH-RH) for undescended testis and for eliciting LH surges in amenorrheic patients

Bioavailability: Reduced bioavailability relative to injection; intranasal GnRH shown to elicit and maintain elevated plasma LH in pretreated amenorrheic patients (Potashnik et al., 1980). Note: the related GnRH agonist nafarelin has intranasal bioavailability ~2.8% (range 1.2–5.6%), cited as analogue context only.

Intranasal gonadorelin has been studied as a non-invasive alternative; efficacy reported in small case series/observational reports, not as a first-line licensed route for native gonadorelin in current SmPCs.

In vitro gastrointestinal/colonic stability assays of GnRH and analogues (e.g., [D-Ser(4)]-gonadorelin) in simulated gastric/colonic fluids and faecal bacterial models

Bioavailability: Native GnRH is vulnerable to enzymatic hydrolysis in vivo (Wikipedia/DrugBank: metabolism = hydrolysis); peptide drugs of this class are rapidly degraded in the GI tract, and oral delivery is not an established route for gonadorelin

Oral-stability data (not oral-absorption): in vitro GI/colonic stability studies of GnRH analogues indicate rapid enzymatic degradation; no oral bioavailability figure for native gonadorelin was sourced.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Weekly median $/mg from the live vendor crawl.

Researched storefront prices, bucketed

p25 $8.18 · median $9.50 · p75 $11.86 · 7 researched vendors

Legit, COA-backed band: $7.90–$10.00/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$62

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Independent labs cited for this compound

One compound-specific recall identified: APS Pharmacy (Drug Depot, LLC) voluntary recall of compounded 'gonadorelin acetate' (March 2022) for lack of sterility assurance. No gonadorelin-specific finished-product recalls from NDA/ANDA holders were found.

Buyer red-flag checklist

• Compounded gonadorelin acetate was subject to a 2022 sterility-assurance recall (APS Pharmacy) — non-sterile injectable risk.
• Bulk Gonadorelin HCl API is listed on FDA Import Alert 66-66, authorizing detention without physical examination of shipments from non-compliant foreign manufacturers.
• Unregulated online 'research peptide' vendors sell gonadorelin acetate without FDA oversight; sterility, potency, and identity controls are not guaranteed for non-compounded, non-pharmacy sources.
• Gonadorelin is a GnRH decapeptide; degradation and dosing inconsistency are documented concerns across the broader compounded-peptide category.

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No gonadorelin-specific independent lab underdosing prevalence data (Janoshik/MZ Biolabs/Finnrick aggregates) was located in this research pass.

• APIs That Appear To Be Misbranded Under 502(f)(1) Because They Do Not Meet The Requirements For The Labeling Exemptions In 21 CFR 201.122. Gonadorelin HCl listed under charge code 64 M - S 03 (Active Pharm Ingred/Chems for Further Manufacturing). Authorizes detention without physical examination (DWPE) of bulk API shipments from Red-Listed foreign manufacturers.66-66
• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Prohibited — S2.2.1 (Peptide Hormones, Growth Factors, Related Substances and Mimetics; testosterone-stimulating peptides in males). Gonadorelin (GnRH) explicitly named in the 2026 Prohibited List along with its agonist analogues. In force 1 January 2026.

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• TRT-clinic promotion bias (clinics reportedly framing gonadorelin as 'better than HCG' amid HCG unavailability)
• Self-experimentation anecdote bias
• Vendor-affiliated content in bodybuilding forums
• HCG-shortage-driven substitution bias inflating gonadorelin adoption

Manually researched from reddit— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

Synthetic decapeptide identical to endogenous GnRH; stimulates pituitary LH and FSH release in a pulse-dependent manner and is used clinically in reproductive medicine. Approximately 307 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Previously FDA-approved (Factrel, LutrePulse); both products withdrawn from market; no currently marketed approved formulation; compoundable via 503A. Research use only.

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