histrelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: -4.08
  • LIPINSKI: 3
  • HAC: 30
  • HDO: 16
  • TPSA: 446.86
  • ALOGS: -4.73
  • ROTB: 34

Drug dosage:

DoseUnitRoute
0.14 mg implant

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

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
Incorrect product administration duration 285.09 66.93 56 568 19266 90608557
Procedural complication 237.19 66.93 40 584 5838 90621985
Device breakage 214.64 66.93 42 582 14002 90613821
Implant site rash 173.99 66.93 20 604 161 90627662

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
Incorrect product administration duration 121.23 60.90 21 164 5859 42615291
Device breakage 109.56 60.90 18 167 3631 42617519
Procedural complication 72.83 60.90 13 172 4206 42616944
Delayed puberty 64.05 60.90 8 177 223 42620927

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
Incorrect product administration duration 213.75 58.64 42 494 20456 110568307
Device breakage 179.10 58.64 34 502 13735 110575028
Implant site rash 162.48 58.64 18 518 149 110588614
Procedural complication 162.31 58.64 29 507 8376 110580387
Device expulsion 78.42 58.64 20 516 30871 110557892
Implant site infection 65.95 58.64 11 525 2092 110586671

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Related Drugs by ATC class:

L02AE Gonadotropin releasing hormone analogues 5 drugs

Drug Use | Suggest Off label Use Form| |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




🐶 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 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG SUPPRELIN LA ENDO OPERATIONS N022058 May 3, 2007 RX IMPLANT SUBCUTANEOUS 8062652 June 16, 2026 METHOD OF TREATMENT OF CHILDREN WITH CENTRAL PRECOCIOUS PUBERTY

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
CHEBI:5739 CHEBI
CHEMBL1201255 ChEMBL_ID
CHEMBL1200509 ChEMBL_ID
C029256 MESH_SUPPLEMENTAL_RECORD_UI
3884 IUPHAR_LIGAND_ID
DB06788 DRUGBANK_ID
H50H3S3W74 UNII
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
C0121902 UMLSCUI
5733 INN_ID
25077993 PUBCHEM_CID
H50H3S3W74 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SUPPRELINLA HUMAN PRESCRIPTION DRUG LABEL 1 67979-002 IMPLANT 50 mg SUBCUTANEOUS NDA 25 sections