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

Stem definition	Drug id	CAS RN
pituitary hormone-release stimulating peptides	2975	76712-82-8

Description:

Molecule

Description

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:

Dose	Unit	Route
0.14	mg	implant

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Dec. 24, 1991	FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Procedural complication	205.97	71.84	36	489	5403	63483094
Incorrect product administration duration	197.06	71.84	39	486	11507	63476990
Device breakage	178.93	71.84	36	489	11506	63476991
Implant site rash	172.73	71.84	20	505	141	63488356

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Device breakage	115.46	50.84	18	156	2282	34954475
Incorrect product administration duration	95.49	50.84	17	157	4794	34951963
Procedural complication	70.89	50.84	13	161	4270	34952487
Device expulsion	61.06	50.84	7	167	79	34956678

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Incorrect product administration duration	201.06	56.04	38	449	11984	79731917
Device breakage	173.69	56.04	33	454	10642	79733259
Implant site rash	161.02	56.04	18	469	126	79743775
Procedural complication	157.19	56.04	29	458	7954	79735947
Device expulsion	77.39	56.04	20	467	25841	79718060
Implant site infection	64.74	56.04	11	476	1854	79742047

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
50MG	SUPPRELIN LA	ENDO PHARM	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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Gonadotropin-releasing hormone receptor	GPCR	P30968	GNRHR_HUMAN	AGONIST				CHEMBL	CHEMBL

External reference:

ID	Source
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
5733	INN_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
25077993	PUBCHEM_CID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SUPPRELINLA	HUMAN PRESCRIPTION DRUG LABEL	1	67979-002	IMPLANT	50 mg	SUBCUTANEOUS	NDA	25 sections
SUPPRELINLA	HUMAN PRESCRIPTION DRUG LABEL	1	67979-002	IMPLANT	50 mg	SUBCUTANEOUS	NDA	25 sections
Vantas	HUMAN PRESCRIPTION DRUG LABEL	1	67979-500	IMPLANT	50 mg	SUBCUTANEOUS	NDA	26 sections