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

Stem definitionDrug idCAS RN
gonadotropin-releasing-hormone (GnRH) inhibitors, peptides 1279 124904-93-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ganirelix
  • orgalutran
  • ganirelix acetate
Ganirelix is a GnRH antagonist, which modulates the hypothalamic-pituitary-gonadal axis by competitive binding to the GnRH receptors in the pituitary gland. As result a rapid, profound,reversible suppression of endogenous gonadotropins occurs, without initial stimulation as induced by GnRH agonists.
  • Molecular weight: 1570.35
  • Formula: C80H113ClN18O13
  • CLOGP: 1.55
  • LIPINSKI: 4
  • HAC: 31
  • HDO: 16
  • TPSA: 451.49
  • ALOGS: -5.47
  • ROTB: 44

Drug dosage:

DoseUnitRoute
0.25 mg P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.21 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.63 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.18 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 9.09 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 16, 2000 EMA N.V. ORGANON
July 29, 1999 FDA ORGANON USA INC

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
Ovarian hyperstimulation syndrome 3442.42 64.13 482 1983 3532 63483025
Ascites 675.65 64.13 179 2286 40549 63446008
Inappropriate schedule of product administration 167.18 64.13 81 2384 103884 63382673
Ovarian haemorrhage 163.95 64.13 25 2440 313 63486244
Ovarian enlargement 140.18 64.13 23 2442 471 63486086
Haemoperitoneum 139.54 64.13 30 2435 2711 63483846
Pleural effusion 90.68 64.13 52 2413 93158 63393399
Abdominal distension 88.77 64.13 50 2415 86565 63399992
Maternal exposure before pregnancy 86.40 64.13 25 2440 7578 63478979
Adnexal torsion 79.54 64.13 14 2451 440 63486117
Needle issue 74.61 64.13 24 2441 10352 63476205
Haemoconcentration 72.77 64.13 11 2454 129 63486428
No adverse event 71.58 64.13 34 2431 41371 63445186
Pelvic fluid collection 70.36 64.13 14 2451 862 63485695

FDA Adverse Event Reporting System (Male)

None

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
Ovarian hyperstimulation syndrome 3239.17 73.74 421 1370 3150 79739447
Ascites 641.92 73.74 174 1617 75388 79667209
Ovarian haemorrhage 171.20 73.74 24 1767 292 79742305
Ovarian enlargement 159.58 73.74 23 1768 345 79742252
Haemoperitoneum 119.51 73.74 26 1765 4317 79738280
Pleural effusion 95.91 73.74 52 1739 145210 79597387
Adnexal torsion 89.59 73.74 14 1777 369 79742228
Pelvic fluid collection 78.96 73.74 14 1777 805 79741792

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H01CC01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
HYPOTHALAMIC HORMONES
Anti-gonadotropin-releasing hormones
FDA PE N0000008638 Decreased GnRH Secretion
FDA MoA N0000175084 Gonadotropin Releasing Hormone Receptor Antagonists
MeSH PA D006727 Hormone Antagonists
FDA EPC N0000175839 Gonadotropin Releasing Hormone Receptor Antagonist

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

DiseaseRelationSNOMED_IDDOID
Ovulation induction indication 61285001
Prevention of Luteinizing Hormone Surge when undergoing Controlled Ovarian Hyperstimulation indication
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 12.09 acidic
pKa3 12.73 acidic
pKa4 13.33 acidic
pKa5 13.33 acidic
pKa6 13.78 acidic
pKa7 8.8 Basic
pKa8 8.2 Basic
pKa9 5.35 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 ANTAGONIST CHEMBL CHEMBL

External reference:

IDSource
4021229 VUID
N0000148673 NUI
D04302 KEGG_DRUG
129311-55-3 SECONDARY_CAS_RN
4021229 VANDF
4021230 VANDF
C0073629 UMLSCUI
CHEBI:135910 CHEBI
CHEMBL1251 ChEMBL_ID
DB06785 DRUGBANK_ID
C061018 MESH_SUPPLEMENTAL_RECORD_UI
3877 IUPHAR_LIGAND_ID
6830 INN_ID
IX503L9WN0 UNII
16130957 PUBCHEM_CID
259264 RXNORM
67714 MMSL
8280 MMSL
d04447 MMSL
008055 NDDF
008056 NDDF
116102008 SNOMEDCT_US
326088005 SNOMEDCT_US
395728002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0052-0301 INJECTION, SOLUTION 250 ug SUBCUTANEOUS NDA 23 sections
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0548-5001 INJECTION 250 ug SUBCUTANEOUS ANDA 23 sections
Ganirelix Acetate Human Prescription Drug Label 1 55566-1000 INJECTION, SOLUTION 250 ug SUBCUTANEOUS ANDA 19 sections
Fyremadel HUMAN PRESCRIPTION DRUG LABEL 1 55566-1010 INJECTION, SOLUTION 250 ug SUBCUTANEOUS ANDA 23 sections
Fyremadel HUMAN PRESCRIPTION DRUG LABEL 1 55566-1010 INJECTION, SOLUTION 250 ug SUBCUTANEOUS ANDA 23 sections
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 65219-028 INJECTION 250 ug SUBCUTANEOUS ANDA 23 sections
GANIRELIX ACETATE Human Prescription Drug Label 1 68083-472 INJECTION, SOLUTION 250 ug SUBCUTANEOUS ANDA 11 sections
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 71288-554 INJECTION, SOLUTION 250 ug SUBCUTANEOUS ANDA 23 sections
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 78206-138 INJECTION, SOLUTION 250 ug SUBCUTANEOUS NDA 23 sections
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 78206-138 INJECTION, SOLUTION 250 ug SUBCUTANEOUS NDA 23 sections
Ganirelix Acetate HUMAN PRESCRIPTION DRUG LABEL 1 78206-138 INJECTION, SOLUTION 250 ug SUBCUTANEOUS NDA 23 sections