buserelin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
pituitary hormone-release stimulating peptides 436 57982-77-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • buserelin
  • etilamide
  • receptal
A potent synthetic analog of GONADOTROPIN-RELEASING HORMONE with D-serine substitution at residue 6, glycine10 deletion, and other modifications.
  • Molecular weight: 1239.45
  • Formula: C60H86N16O13
  • CLOGP: -1.45
  • LIPINSKI: 3
  • HAC: 29
  • HDO: 16
  • TPSA: 438.27
  • ALOGS: -4.51
  • ROTB: 33

Drug dosage:

DoseUnitRoute
0.11 mg implant
1.20 mg N
1.50 mg P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.02 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1984 YEAR INTRODUCED

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 93.82 80.08 13 45 3179 46682825

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

Pharmacologic Action:

SourceCodeDescription
ATC L02AE01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
MeSH PA D005300 Fertility Agents, Female
MeSH PA D012102 Reproductive Control Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 11.9 acidic
pKa3 12.86 acidic
pKa4 13.14 acidic
pKa5 13.23 acidic
pKa6 13.59 acidic
pKa7 10.75 Basic
pKa8 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 EC50 10.52 IUPHAR IUPHAR
Lutropin-choriogonadotropic hormone receptor GPCR Kd 8.57 WOMBAT-PK
Gonadotropin-releasing hormone receptor GPCR AGONIST EC50 10.05 IUPHAR

External reference:

IDSource
N0000170309 NUI
D07259 KEGG_DRUG
C0006456 UMLSCUI
CHEBI:135907 CHEBI
CHEMBL2110824 ChEMBL_ID
DB06719 DRUGBANK_ID
D002064 MESH_DESCRIPTOR_UI
4045 INN_ID
50224 PUBCHEM_CID
3860 IUPHAR_LIGAND_ID
PXW8U3YXDV UNII
1825 RXNORM
003708 NDDF
008310 NDDF
327301004 SNOMEDCT_US
395744006 SNOMEDCT_US

Pharmaceutical products:

None