gonadorelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
pituitary hormone-release stimulating peptides 2958 33515-09-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gonadorelin
  • Luteinizing hormone-releasing factor (swine)
  • hypocrine
  • fertagyl
  • gonadorelin hydrochloride
  • gonadorelin acetate
  • gonadorelin HCl
  • gonadorelin diacetate tetrahydrate
A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.
  • Molecular weight: 1182.31
  • Formula: C55H75N17O13
  • CLOGP: -6.31
  • LIPINSKI: 3
  • HAC: 30
  • HDO: 17
  • TPSA: 472.13
  • ALOGS: -4.33
  • ROTB: 31

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 30, 1982 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Metastases to bone 122.94 56.44 31 642 20988 63467361
Neutropenia 114.97 56.44 49 624 174956 63313393
Ovarian hyperstimulation syndrome 103.40 56.44 20 653 3994 63484355

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Recalled product administered 68.19 37.15 10 255 531 34956135

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Metastases to bone 101.31 43.22 27 754 24400 79719207
Ovarian hyperstimulation syndrome 94.63 43.22 18 763 3553 79740054
Neutropenia 86.50 43.22 46 735 287664 79455943
Carcinoembryonic antigen increased 45.35 43.22 9 772 2200 79741407
Meningeal disorder 44.74 43.22 7 774 436 79743171

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H01CA01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
HYPOTHALAMIC HORMONES
Gonadotropin-releasing hormones
ATC V04CM01 VARIOUS
DIAGNOSTIC AGENTS
OTHER DIAGNOSTIC AGENTS
Tests for fertility disturbances
CHEBI has role CHEBI:63533 gonadotropin releasing hormone agonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Amenorrhea indication 14302001 DOID:13938
Diagnostic Test for Gonadotropin Deficiency indication




🐶 Veterinary Drug Use

SpeciesUseRelation
Cattle Reproductive synchrony programs Indication
Cattle Ovarian cysts Indication

🐶 Veterinary products

ProductApplicantIngredients
CYSTORELIN Boehringer lngelheim Animal Health USA Inc. 1
Factrel, Factrel Injection Zoetis Inc. 1
Fertelin, OvaCyst Bimeda Animal Health Limited 1
FERTAGYL Intervet Inc. 1
Gonabreed Parnell Technologies Pty. Ltd. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 11.9 acidic
pKa3 12.71 acidic
pKa4 12.88 acidic
pKa5 13.24 acidic
pKa6 13.32 acidic
pKa7 13.61 acidic
pKa8 13.97 acidic
pKa9 10.75 Basic
pKa10 6.69 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Gonadotropin-releasing hormone receptor GPCR AGONIST IC50 8 CHEMBL CHEMBL
Gonadotropin-releasing hormone receptor GPCR IC50 8.70 CHEMBL
Lutropin-choriogonadotropic hormone receptor GPCR Ki 8.90 CHEMBL

External reference:

IDSource
4019767 VUID
N0000147858 NUI
D00988 KEGG_DRUG
51952-41-1 SECONDARY_CAS_RN
4018487 VANDF
4018488 VANDF
4019767 VANDF
C0023610 UMLSCUI
CHEBI:5520 CHEBI
CHEMBL1007 ChEMBL_ID
CHEMBL1200511 ChEMBL_ID
CHEMBL1200516 ChEMBL_ID
DB00644 DRUGBANK_ID
3627 INN_ID
52699-48-6 SECONDARY_CAS_RN
9O7312W37G UNII
638793 PUBCHEM_CID
1298838 RXNORM
4796 MMSL
4797 MMSL
d00573 MMSL
002108 NDDF
002109 NDDF
004782 NDDF
008305 NDDF
008306 NDDF
325995009 SNOMEDCT_US
397197007 SNOMEDCT_US
412193007 SNOMEDCT_US
49869009 SNOMEDCT_US
75969007 SNOMEDCT_US
96365009 SNOMEDCT_US
D007987 MESH_DESCRIPTOR_UI

Pharmaceutical products:

None