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GnRH

Gonadorelin

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?

The product’s synthetic gonadorelin is described as matching the endogenous bovine hypothalamic releasing factor both chemically and physiologically. Administration of this gonadorelin product stimulates endogenous LH secretion. Target-animal safety data reported that repeated intramuscular dosing (1000 mcg gonadorelin diacetate tetrahydrate for five consecutive days) produced no effects on hematology or clinical chemistries in normally cycling dairy cattle. The dosage form and route are an injectable solution intended for intramuscular administration.

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

The product’s synthetic gonadorelin is described as matching the endogenous bovine hypothalamic releasing factor both chemically and physiologically.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionSynthetic gonadorelin is physiologically and chemically identical to the endogenous bovine hypothalamic releasing factor.
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
    “Synthetic gonadorelin is physiologically and chemically identical to the endogenous bovine hypothalamic releasing factor.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · DESCRIPTION:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Identity

The labeled concentration is 50 micrograms of synthetic gonadorelin per mL, present as the hydrochloride salt.

Sources[2]dailymedFactrel®Injection50 mcg gonadorelin per mL (as gonadorelin hydrochloride)
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
    “50 mcg gonadorelin per mL (as gonadorelin hydrochloride)”

    Factrel®Injection · Untitled section

    dailymed:1451663c-b85a-4b45-8b27-6d572d0032f9:989d90e9723f:989d90e9723f

Identity

CYSTORELIN is formulated as gonadorelin diacetate tetrahydrate (50 mcg/mL), providing 43 mcg/mL gonadorelin, and is intended for intramuscular or intravenous administration as indicated.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionCYSTORELIN®is a sterile solution containing 43 mcg/mL of gonadorelin (GnRH) as 50 mcg/mL gonadorelin diacetate tetrahydrate suitable for intramuscular or intravenous administration according to the indication.
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
    “CYSTORELIN®is a sterile solution containing 43 mcg/mL of gonadorelin (GnRH) as 50 mcg/mL gonadorelin diacetate tetrahydrate suitable for intramuscular or intravenous administration according to the indication.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · DESCRIPTION:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Identity

The excipients include sodium chloride (0.6%) and benzyl alcohol (2%) in an aqueous solution; benzyl alcohol functions as a preservative.

Sources[2]dailymedFactrel®Injectionin aqueous formulation containing 0.6% sodium chloride and 2% benzyl alcohol (as a preservative).
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 aqueous formulation containing 0.6% sodium chloride and 2% benzyl alcohol (as a preservative).”

    Factrel®Injection · DESCRIPTION

    dailymed:1451663c-b85a-4b45-8b27-6d572d0032f9:989d90e9723f:989d90e9723f

How does it work?

Target, response, and disposition.

Mechanism

Physiologically, gonadorelin functions as a hypothalamic releasing factor that stimulates anterior pituitary secretion of gonadotropins, including luteinizing hormone (LH) and follicle stimulating hormone (FSH).

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionGonadorelin is the hypothalamic releasing factor responsible for the release of gonadotropins (e.g., luteinizing hormone [LH], follicle stimulating hormone [FSH]) from the anterior pituitary.
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
    “Gonadorelin is the hypothalamic releasing factor responsible for the release of gonadotropins (e.g., luteinizing hormone [LH], follicle stimulating hormone [FSH]) from the anterior pituitary.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · DESCRIPTION:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Mechanism

As gonadotropin releasing hormone (GnRH), gonadorelin stimulates the anterior pituitary to release gonadotropins LH and FSH.

Sources[2]dailymedFactrel®InjectionGonadorelin is the gonadotropin releasing hormone (GnRH) which is produced by the hypothalamus and causes the release of the gonadotropin luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary.
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
    “Gonadorelin is the gonadotropin releasing hormone (GnRH) which is produced by the hypothalamus and causes the release of the gonadotropin luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary.”

    Factrel®Injection · DESCRIPTION

    dailymed:1451663c-b85a-4b45-8b27-6d572d0032f9:989d90e9723f:989d90e9723f

Mechanism

Administration of this gonadorelin product stimulates endogenous LH secretion.

Sources[2]dailymedFactrel®InjectionFACTREL Injection induces release of endogenous luteinizing hormone (LH)
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
    “FACTREL Injection induces release of endogenous luteinizing hormone (LH)”

    Factrel®Injection · MECHANISM OF ACTION

    dailymed:1451663c-b85a-4b45-8b27-6d572d0032f9:989d90e9723f:989d90e9723f

Pharmacokinetics

A cell-free human plasma stability measurement reported CHEMBL1007 half-life (T1/2) as 0.05 hr.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1007Assay: Half life in human plasma Assay format: cell-free format Standard result: T1/2 = 0.05 hr
Reported result
T1/2 = 0.05 hr
Source records
1
Independent studies
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
    “Assay: Half life in human plasma Assay format: cell-free format Standard result: T1/2 = 0.05 hr”

    ChEMBL activities for CHEMBL1007 · Activity 13356492

    chembl-activities:chembl1007:352cf8582749:352cf8582749

Pharmacokinetics

A cell-based stability assay in human Caco-2 cell homogenates at 200 uM measured CHEMBL1007 degradation kinetics by LC-MS and reported a half-life of 0.5433 hr.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1007Assay: Half life in human Caco2 cell homogenates at 200 uM by LC-MS analysis Assay format: cell-based format Standard result: T1/2 = 0.5433 hr
Reported result
T1/2 = 0.5433 hr
Source records
1
Independent studies
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
    “Assay: Half life in human Caco2 cell homogenates at 200 uM by LC-MS analysis Assay format: cell-based format Standard result: T1/2 = 0.5433 hr”

    ChEMBL activities for CHEMBL1007 · Activity 13356501

    chembl-activities:chembl1007:352cf8582749:352cf8582749

What has been studied?

What the evidence says.

Studied populations

The labeled target species is cattle; use in other species is not indicated here.

Sources[2]dailymedFactrel®InjectionFor use in cattle only
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
    “For use in cattle only”

    Factrel®Injection · Untitled section

    dailymed:1451663c-b85a-4b45-8b27-6d572d0032f9:989d90e9723f:989d90e9723f

Risks and interactions

Risks, organized for scanning.

Safety findings

Target-animal safety data reported that repeated intramuscular dosing (1000 mcg gonadorelin diacetate tetrahydrate for five consecutive days) produced no effects on hematology or clinical chemistries in normally cycling dairy cattle.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionThe intramuscular administration of 1000 mcg gonadorelin diacetate tetrahydrate on five (5) consecutive days to normally cycling dairy cattle had no effect on hematology or clinical chemistries.
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 intramuscular administration of 1000 mcg gonadorelin diacetate tetrahydrate on five (5) consecutive days to normally cycling dairy cattle had no effect on hematology or clinical chemistries.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · TARGET ANIMAL SAFETY:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Products and regulatory status

Same ingredient. Different records.

Regulatory status

The label indicates co-use with cloprostenol sodium for estrous-cycle synchronization to enable fixed-time artificial insemination in lactating dairy and beef cows.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionCYSTORELIN is indicated for use with cloprostenol sodium to synchronize estrous cycles to allow for fixed time artificial insemination (FTAI) in lactating dairy cows and beef cows.
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
    “CYSTORELIN is indicated for use with cloprostenol sodium to synchronize estrous cycles to allow for fixed time artificial insemination (FTAI) in lactating dairy cows and beef cows.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · INDICATIONS FOR USE:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Regulatory status

The labeled use includes treatment of ovarian follicular cysts specifically in dairy cattle.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionCYSTORELIN is indicated for the treatment of ovarian follicular cysts in dairy cattle.
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
    “CYSTORELIN is indicated for the treatment of ovarian follicular cysts in dairy cattle.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · INDICATIONS FOR USE:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Administration context

The practical clinical context.

Administration

The dosage form and route are an injectable solution intended for intramuscular administration.

Sources[2]dailymedFactrel®InjectionSolution for Intramuscular Injection.
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
    “Solution for Intramuscular Injection.”

    Factrel®Injection · Untitled section

    dailymed:1451663c-b85a-4b45-8b27-6d572d0032f9:989d90e9723f:989d90e9723f

Dose records

In reproductive synchrony programs, CYSTORELIN is dosed intramuscularly at 100 mcg gonadorelin diacetate tetrahydrate (2 mL) per cow.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionThe intramuscular dosage of CYSTORELIN is 100 mcg gonadorelin diacetate tetrahydrate (2 mL) per cow
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 intramuscular dosage of CYSTORELIN is 100 mcg gonadorelin diacetate tetrahydrate (2 mL) per cow”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · DOSAGE AND ADMINISTRATION:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Dose records

The labeled dose for cystic ovaries is 100 mcg gonadorelin diacetate tetrahydrate delivered as 2 mL per cow, administered intravenously or intramuscularly.

Sources[3]dailymedCYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable SolutionThe intravenous or intramuscular dosage of CYSTORELIN is 100 mcg gonadorelin diacetate tetrahydrate (2 mL) per cow.
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 intravenous or intramuscular dosage of CYSTORELIN is 100 mcg gonadorelin diacetate tetrahydrate (2 mL) per cow.”

    CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution · DOSAGE AND ADMINISTRATION:

    dailymed:50cf9edb-f318-41d2-9b98-6ea3410e8128:90e3b756118e:90e3b756118e

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: contraindication, effect, interaction
  • 50 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (35), assurance_score_below_0.72 (8), current_regulatory_source_required (10), extraction_ambiguity (43), extraction_confidence_not_high (4), high_risk_requires_regulatory_or_two_independent_sources (14), no_direct_support (43)

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

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL1007 ↗

    chembl-activities · published 2026-08-27 · retrieved 2026-08-27T19:16:08Z

  2. Factrel®Injection ↗

    dailymed · published 2026-08-18 · retrieved 2026-09-04T19:33:55Z

  3. CYSTORELIN®(gonadorelin)50 mcg/mL gonadorelin diacetate tetrahydrate Injectable Solution ↗

    dailymed · published 2025-08-05 · retrieved 2026-09-04T19:33:55Z

Publication history and provenance

Version 3 · Automated assessment · 2026-09-04T19:33:55Z

d20f458c3bbb474199b0f0fbf67c3fb87534e9dbd5b53c586ea00d1454a332be