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

Stem definitionDrug idCAS RN
pituitary hormone-release stimulating peptides 2975 76712-82-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vantas
  • Luteinizing hormone-releasing factor (pig)
  • histrelin acetate
  • histrelin
gonadotropin releasing hormone agonist
  • Molecular weight: 1323.53
  • Formula: C66H86N18O12
  • CLOGP: -1.90
  • LIPINSKI: 3
  • HAC: 30
  • HDO: 16
  • TPSA: 446.86
  • ALOGS: -4.73
  • ROTB: 34

Drug dosage:

DoseUnitRoute
0.14 mg implant

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 24, 1991 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
Procedural complication 178.20 74.88 32 410 4898 46680722
Device breakage 174.55 74.88 35 407 9657 46675963
Implant site rash 163.39 74.88 19 423 120 46685500
Incorrect product administration duration 151.07 74.88 31 411 9546 46676074

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
Device breakage 138.29 58.52 22 268 1598 29950590
Procedural complication 79.00 58.52 16 274 4481 29947707
Device expulsion 64.60 58.52 8 282 88 29952100
Incorrect product administration duration 63.20 58.52 13 277 3909 29948279

Pharmacologic Action:

SourceCodeDescription
ATC L02AE05 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
FDA MoA N0000175654 Gonadotropin Releasing Hormone Receptor Agonists
FDA EPC N0000175655 Gonadotropin Releasing Hormone Receptor Agonist
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:63533 gonadotrophin releasing hormone agonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Precocious puberty indication 400179000
Advanced Prostatic Carcinoma indication
Hypercholesterolemia contraindication 13644009
Hypertensive disorder contraindication 38341003 DOID:10763
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Pregnancy, function contraindication 289908002
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Smokes tobacco daily contraindication 449868002
Vertebral Metastases contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 11.9 acidic
pKa3 12.79 acidic
pKa4 12.97 acidic
pKa5 13.16 acidic
pKa6 13.43 acidic
pKa7 13.89 acidic
pKa8 10.75 Basic
pKa9 7.01 Basic
pKa10 6.41 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 CHEMBL CHEMBL

External reference:

IDSource
D02369 KEGG_DRUG
220810-26-4 SECONDARY_CAS_RN
4025439 VANDF
4025440 VANDF
4025500 VANDF
C0121902 UMLSCUI
CHEBI:5739 CHEBI
CHEMBL1201255 ChEMBL_ID
CHEMBL1200509 ChEMBL_ID
DB06788 DRUGBANK_ID
C029256 MESH_SUPPLEMENTAL_RECORD_UI
3884 IUPHAR_LIGAND_ID
5733 INN_ID
H50H3S3W74 UNII
25077993 PUBCHEM_CID
1294622 RXNORM
4829 MMSL
60923 MMSL
d00575 MMSL
004142 NDDF
004143 NDDF
008318 NDDF
008319 NDDF
109049002 SNOMEDCT_US
109050002 SNOMEDCT_US
126198004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SUPPRELINLA HUMAN PRESCRIPTION DRUG LABEL 1 67979-002 IMPLANT 50 mg SUBCUTANEOUS NDA 24 sections
Vantas HUMAN PRESCRIPTION DRUG LABEL 1 67979-500 IMPLANT 50 mg SUBCUTANEOUS NDA 26 sections