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 3203.54 61.37 452 1913 3212 56286490
Ascites 638.09 61.37 171 2194 37373 56252329
Inappropriate schedule of product administration 178.19 61.37 81 2284 83306 56206396
Ovarian haemorrhage 162.35 61.37 25 2340 308 56289394
Ovarian enlargement 138.70 61.37 23 2342 464 56289238
Haemoperitoneum 138.42 61.37 30 2335 2600 56287102
Abdominal distension 87.48 61.37 49 2316 77577 56212125
Maternal exposure before pregnancy 87.13 61.37 25 2340 6798 56282904
Pleural effusion 83.08 61.37 49 2316 85431 56204271
Adnexal torsion 80.71 61.37 14 2351 372 56289330
No adverse event 73.23 61.37 34 2331 36340 56253362
Pelvic fluid collection 69.83 61.37 14 2351 827 56288875
Needle issue 68.52 61.37 22 2343 8716 56280986
Haemoconcentration 67.88 61.37 10 2355 89 56289613

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 2987.25 72.72 391 1323 2849 70923881
Ascites 611.04 72.72 166 1548 67381 70859349
Ovarian haemorrhage 169.60 72.72 24 1690 290 70926440
Ovarian enlargement 158.34 72.72 23 1691 338 70926392
Haemoperitoneum 119.30 72.72 26 1688 4045 70922685
Adnexal torsion 91.17 72.72 14 1700 304 70926426
Pleural effusion 88.37 72.72 49 1665 132815 70793915
Pelvic fluid collection 79.43 72.72 14 1700 722 70926008

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
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
129311-55-3 SECONDARY_CAS_RN
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 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