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GnRH antagonist

Ganirelix

Published evidence · coverage incomplete
Anatomical contextAnatomy connections are not mapped yet.

No body region is highlighted until this profile has a supported anatomical connection. This does not mean the peptide has no biological effects.

Read published mechanism findings ↓

At a glance

What is it—and why does it matter?

Ganirelix acetate is a 10–amino-acid synthetic peptide that functions as a GnRH antagonist. As a competitive GnRH-receptor antagonist at pituitary gonadotrophs, ganirelix produces rapid and reversible suppression of gonadotropin release. Discontinuation of ganirelix is followed by full recovery of pituitary LH and FSH levels within 48 hours, consistent with reversible antagonism. Contraindication: ganirelix acetate injection should not be used when pregnancy is known or suspected.

Sources for this introduction: [1] [2] [3] [4]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

Identity

Ganirelix acetate is a 10–amino-acid synthetic peptide that functions as a GnRH antagonist.

Sources[1]dailymedGanirelix Acetate InjectionGanirelix Acetate Injection is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH).[2]dailymedGanirelix Acetate InjectionGanirelix Acetate Injection is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH).
Source records
2
Regulatory records
2

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Ganirelix Acetate Injection is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH).”

    Ganirelix Acetate Injection · DESCRIPTION

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e
  2. supports · Source-backed record
    “Ganirelix Acetate Injection is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH).”

    Ganirelix Acetate Injection · DESCRIPTION

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227

How does it work?

Target, response, and disposition.

Mechanism

As a competitive GnRH-receptor antagonist at pituitary gonadotrophs, ganirelix produces rapid and reversible suppression of gonadotropin release.

Sources[1]dailymedGanirelix Acetate InjectionGanirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion.[2]dailymedGanirelix Acetate InjectionGanirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion.[3]dailymedFyremadel®(ganirelix acetate) injectionGanirelix acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion.
Source records
3
Regulatory records
3

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion.”

    Ganirelix Acetate Injection · CLINICAL PHARMACOLOGY

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e
  2. supports · Source-backed record
    “Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion.”

    Ganirelix Acetate Injection · CLINICAL PHARMACOLOGY

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227
  3. supports · Source-backed record
    “Ganirelix acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion.”

    Fyremadel®(ganirelix acetate) injection · CLINICAL PHARMACOLOGY

    dailymed:5f0908b5-3551-47fd-95f7-3669b0dff7f1:7d92ae5b6ed9:7d92ae5b6ed9

Pharmacokinetics

Mass balance data after a 1 mg IV [14C]-ganirelix dose show near-complete recovery over 288 h, primarily via feces (75.1%) with additional urinary recovery (22.1%).

Sources[2]dailymedGanirelix Acetate InjectionOn average, 97.2% of the total radiolabeled Ganirelix Acetate dose is recovered in the feces and urine (75.1% and 22.1%, respectively) over 288 h following intravenous single dose administration of 1 mg [14C]-Ganirelix Acetate.
Reported result
Total recovery 97.2%; feces 75.1%; urine 22.1% (over 288 h)
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “On average, 97.2% of the total radiolabeled Ganirelix Acetate dose is recovered in the feces and urine (75.1% and 22.1%, respectively) over 288 h following intravenous single dose administration of 1 mg [14C]-Ganirelix Acetate.”

    Ganirelix Acetate Injection · Excretion

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227

Pharmacokinetics

After one 250 mcg SC injection, ganirelix shows high systemic availability (mean absolute bioavailability 91.1%) in healthy women.

Sources[2]dailymedGanirelix Acetate InjectionThe mean absolute bioavailability of Ganirelix Acetate following a single 250 mcg subcutaneous injection to healthy female volunteers is 91.1%.[3]dailymedFyremadel®(ganirelix acetate) injectionThe mean absolute bioavailability of ganirelix acetate following a single 250 mcg subcutaneous injection to healthy female volunteers is 91.1%.
Reported result
Mean absolute bioavailability: 91.1%
Source records
2
Regulatory records
2

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The mean absolute bioavailability of Ganirelix Acetate following a single 250 mcg subcutaneous injection to healthy female volunteers is 91.1%.”

    Ganirelix Acetate Injection · Absorption

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227
  2. supports · Source-backed record
    “The mean absolute bioavailability of ganirelix acetate following a single 250 mcg subcutaneous injection to healthy female volunteers is 91.1%.”

    Fyremadel®(ganirelix acetate) injection · Absorption

    dailymed:5f0908b5-3551-47fd-95f7-3669b0dff7f1:7d92ae5b6ed9:7d92ae5b6ed9

Pharmacokinetics

Across the 125 to 500 mcg dose range, ganirelix shows dose-proportional pharmacokinetics.

Sources[1]dailymedGanirelix Acetate InjectionThe pharmacokinetics of Ganirelix Acetate are dose-proportional in the dose range of 125 to 500 mcg.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The pharmacokinetics of Ganirelix Acetate are dose-proportional in the dose range of 125 to 500 mcg.”

    Ganirelix Acetate Injection · Pharmacokinetics

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e

Pharmacokinetics

Across 125–500 mcg, ganirelix exposure changes proportionally with dose, consistent with linear pharmacokinetics in this range.

Sources[2]dailymedGanirelix Acetate InjectionThe pharmacokinetics of Ganirelix Acetate are dose-proportional in the dose range of 125 to 500 mcg.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The pharmacokinetics of Ganirelix Acetate are dose-proportional in the dose range of 125 to 500 mcg.”

    Ganirelix Acetate Injection · Pharmacokinetics

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227

Pharmacokinetics

Ganirelix exhibits high in vitro binding to human plasma proteins (81.9%).

Sources[2]dailymedGanirelix Acetate InjectionIn vitroprotein binding to human plasma is 81.9%.
Reported result
Protein binding: 81.9% (in vitro)
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “In vitroprotein binding to human plasma is 81.9%.”

    Ganirelix Acetate Injection · Distribution

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227

What has been studied?

What the evidence says.

Study findings

The pituitary suppression of gonadotropins caused by ganirelix is reversible, with LH and FSH fully recovering within 48 hours after discontinuation.

Sources[2]dailymedGanirelix Acetate InjectionUpon discontinuation of Ganirelix Acetate, pituitary LH and FSH levels are fully recovered within 48 hours.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Upon discontinuation of Ganirelix Acetate, pituitary LH and FSH levels are fully recovered within 48 hours.”

    Ganirelix Acetate Injection · CLINICAL PHARMACOLOGY

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227

Study findings

Ganirelix produces greater suppression of pituitary luteinizing hormone (LH) secretion than follicle-stimulating hormone (FSH).

Sources[1]dailymedGanirelix Acetate InjectionThe suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH.”

    Ganirelix Acetate Injection · CLINICAL PHARMACOLOGY

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e

Study findings

Discontinuation of ganirelix is followed by full recovery of pituitary LH and FSH levels within 48 hours, consistent with reversible antagonism.

Sources[1]dailymedGanirelix Acetate InjectionUpon discontinuation of Ganirelix Acetate, pituitary LH and FSH levels are fully recovered within 48 hours.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Upon discontinuation of Ganirelix Acetate, pituitary LH and FSH levels are fully recovered within 48 hours.”

    Ganirelix Acetate Injection · CLINICAL PHARMACOLOGY

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e

Studied populations

No pharmacokinetic characterization is provided for special populations (geriatric, pediatric, renal impairment, hepatic impairment).

Sources[1]dailymedGanirelix Acetate InjectionThe pharmacokinetics of Ganirelix Acetate Injection have not been determined in special populations such as geriatric, pediatric, renally impaired and hepatically impaired patients (seePRECAUTIONS).
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The pharmacokinetics of Ganirelix Acetate Injection have not been determined in special populations such as geriatric, pediatric, renally impaired and hepatically impaired patients (seePRECAUTIONS).”

    Ganirelix Acetate Injection · Special Populations

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e

Risks and interactions

Risks, organized for scanning.

Contraindications

Contraindication: ganirelix acetate injection should not be used when pregnancy is known or suspected.

Sources[3]dailymedFyremadel®(ganirelix acetate) injectionKnown or suspected pregnancy (seePRECAUTIONS).
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Known or suspected pregnancy (seePRECAUTIONS).”

    Fyremadel®(ganirelix acetate) injection · CONTRAINDICATIONS

    dailymed:5f0908b5-3551-47fd-95f7-3669b0dff7f1:7d92ae5b6ed9:7d92ae5b6ed9

Products and regulatory status

Same ingredient. Different records.

Regulatory status

Approved use: ganirelix acetate injection is indicated to inhibit premature luteinizing hormone surges in women undergoing controlled ovarian hyperstimulation.

Sources[3]dailymedFyremadel®(ganirelix acetate) injectionGanirelix acetate injection is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Ganirelix acetate injection is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.”

    Fyremadel®(ganirelix acetate) injection · INDICATIONS AND USAGE

    dailymed:5f0908b5-3551-47fd-95f7-3669b0dff7f1:7d92ae5b6ed9:7d92ae5b6ed9

Regulatory status

The labeled indication for ganirelix acetate injection is prevention (inhibition) of premature luteinizing hormone surges during controlled ovarian hyperstimulation protocols.

Sources[1]dailymedGanirelix Acetate InjectionGanirelix Acetate Injection is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.[2]dailymedGanirelix Acetate InjectionGanirelix Acetate Injection is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.
Source records
2
Regulatory records
2

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Ganirelix Acetate Injection is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.”

    Ganirelix Acetate Injection · INDICATIONS AND USAGE

    dailymed:32fb74ff-993a-49fe-8943-e029372b863e:8542cf802e5e:8542cf802e5e
  2. supports · Source-backed record
    “Ganirelix Acetate Injection is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation.”

    Ganirelix Acetate Injection · INDICATIONS AND USAGE

    dailymed:37a8e041-9751-665a-1965-765f7ff21922:c8a608743227:c8a608743227

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, interaction, safety
  • 38 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (22), assurance_score_below_0.72 (13), current_regulatory_source_required (7), extraction_ambiguity (35), high_risk_requires_regulatory_or_two_independent_sources (13), no_direct_support (34)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. Ganirelix Acetate Injection ↗

    dailymed · published 2025-11-13 · retrieved 2026-09-04T19:33:35Z

  2. Ganirelix Acetate Injection ↗

    dailymed · published 2026-03-18 · retrieved 2026-09-04T19:33:36Z

  3. Fyremadel®(ganirelix acetate) injection ↗

    dailymed · published 2025-01-06 · retrieved 2026-09-04T19:33:35Z

Publication history and provenance

Version 2 · Automated assessment · 2026-09-04T19:33:36Z

5276d44c3d11dddf7201fa97043a88cf88a4a49f6a9565a0455bec8bc1dddc48