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

Stem definition	Drug id	CAS RN
pituitary hormone-release stimulating peptides	2968	57773-63-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: triptorelin arvekap triptoreline tryptorelin triptorelin pamoate triptorelin acetate	A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE with D-tryptophan substitution at residue 6. Molecular weight: 1311.47 Formula: C64H82N18O13 CLOGP: -4.59 LIPINSKI: 3 HAC: 31 HDO: 18 TPSA: 487.92 ALOGS: -4.63 ROTB: 33

Molecule

Description

Molfile Inchi Smiles

Synonyms:

triptorelin
arvekap
triptoreline
tryptorelin
triptorelin pamoate
triptorelin acetate

A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE with D-tryptophan substitution at residue 6.

Molecular weight: 1311.47
Formula: C64H82N18O13
CLOGP: -4.59
LIPINSKI: 3
HAC: 31
HDO: 18
TPSA: 487.92
ALOGS: -4.63
ROTB: 33

Drug dosage:

Dose	Unit	Route
0.13	mg	P
0.10	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	41.70 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.40 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.67 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.81 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	10 mg/mL	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
June 15, 2000	FDA	ACTAVIS LABS UT INC

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
Ovarian hyperstimulation syndrome	1356.28	40.03	210	1812	3804	63483196
Needle issue	322.69	40.03	73	1949	10303	63476697
Ascites	240.18	40.03	77	1945	40651	63446349
Syringe issue	132.59	40.03	28	1994	2841	63484159
Disease progression	131.15	40.03	68	1954	122690	63364310
Product use complaint	119.23	40.03	25	1997	2449	63484551
Off label use	115.74	40.03	123	1899	674339	62812661
Product prescribing issue	94.66	40.03	21	2001	2678	63484322
Progesterone increased	85.85	40.03	11	2011	41	63486959
Haemoperitoneum	83.45	40.03	19	2003	2722	63484278
Product administration error	83.10	40.03	30	1992	22367	63464633
Product physical issue	58.04	40.03	16	2006	4964	63482036
Product reconstitution quality issue	57.50	40.03	8	2014	62	63486938
Ovarian enlargement	54.59	40.03	10	2012	484	63486516
Product administration interrupted	53.89	40.03	15	2007	4821	63482179
Incorrect dose administered	49.26	40.03	28	1994	59940	63427060
Osteonecrosis of jaw	47.78	40.03	23	1999	35100	63451900
Haemoconcentration	44.53	40.03	7	2015	133	63486867
Vaginal haemorrhage	43.54	40.03	20	2002	27467	63459533

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
Prostatic specific antigen increased	136.70	22.87	51	3116	14629	34939135
Osteonecrosis of jaw	80.56	22.87	37	3130	17852	34935912
Syringe issue	68.89	22.87	24	3143	5640	34948124
Needle issue	55.79	22.87	21	3146	6144	34947620
Femoral neck fracture	52.00	22.87	17	3150	3290	34950474
Anaemia	50.89	22.87	82	3085	233253	34720511
Hot flush	47.63	22.87	26	3141	18040	34935724
Product prescribing issue	45.89	22.87	14	3153	2165	34951599
Respiratory tract infection bacterial	39.89	22.87	12	3155	1770	34951994
Respiratory tract infection viral	39.82	22.87	13	3154	2504	34951260
Metastases to bone	39.43	22.87	20	3147	11950	34941814
Metastasis	29.97	22.87	12	3155	4132	34949632
Hepatitis fulminant	26.43	22.87	11	3156	4179	34949585
Congestive cardiomyopathy	26.06	22.87	13	3154	7497	34946267
Blood testosterone increased	26.04	22.87	8	3159	1265	34952499
Product reconstitution quality issue	25.55	22.87	5	3162	118	34953646
Product use complaint	25.11	22.87	8	3159	1424	34952340
Meningioma	25.09	22.87	8	3159	1428	34952336
Death	23.46	22.87	84	3083	397965	34555799

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
Ovarian hyperstimulation syndrome	1164.52	23.02	197	4290	3374	79736527
Needle issue	254.77	23.02	71	4416	12997	79726904
Syringe issue	135.49	23.02	37	4450	6261	79733640
Ascites	133.64	23.02	71	4416	75491	79664410
Prostatic specific antigen increased	125.58	23.02	39	4448	10347	79729554
Osteonecrosis of jaw	116.14	23.02	54	4433	43172	79696729
Progesterone increased	79.78	23.02	11	4476	40	79739861
Product use complaint	74.52	23.02	19	4468	2464	79737437
Haemoperitoneum	59.67	23.02	18	4469	4325	79735576
Product reconstitution quality issue	57.48	23.02	10	4477	199	79739702
Anaemia	55.92	23.02	94	4393	444921	79294980
Ovarian enlargement	51.83	23.02	10	4477	358	79739543
Product administration error	50.84	23.02	28	4459	31818	79708083
Incorrect dose administered	44.82	23.02	36	4451	76594	79663307
Product prescribing issue	43.92	23.02	14	4473	4031	79735870
Respiratory tract infection bacterial	43.71	23.02	12	4475	2065	79737836
Product physical issue	39.40	23.02	13	4474	4172	79735729
Respiratory tract infection viral	39.17	23.02	13	4474	4246	79735655
Haemoconcentration	38.30	23.02	7	4480	186	79739715
Femoral neck fracture	38.18	23.02	16	4471	9968	79729933
Metastases to bone	37.67	23.02	21	4466	24406	79715495
Off label use	35.91	23.02	122	4365	907093	78832808
Hot flush	34.70	23.02	27	4460	54850	79685051
Product deposit	30.60	23.02	7	4480	574	79739327
Congestive cardiomyopathy	29.39	23.02	14	4473	11766	79728135
Product administration interrupted	28.43	23.02	10	4477	3889	79736012
Incorrect route of product administration	28.40	23.02	20	4467	34909	79704992
Pelvic fluid collection	28.21	23.02	7	4480	812	79739089
Adnexal torsion	27.80	23.02	6	4481	377	79739524
Type 2 diabetes mellitus	25.52	23.02	23	4464	57099	79682802
Product dose omission issue	24.21	23.02	47	4440	247490	79492411
Asthenia	23.93	23.02	73	4414	511616	79228285

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L02AE04	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	antineoplastic agents
CHEBI has role	CHEBI:49323	contraceptive drugs
CHEBI has role	CHEBI:63533	gonadotropin releasing hormone agonists
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018931	Antineoplastic Agents, Hormonal
MeSH PA	D003270	Contraceptive Agents
MeSH PA	D003271	Contraceptive Agents, Female
MeSH PA	D000080066	Contraceptive Agents, Hormonal
MeSH PA	D008186	Luteolytic Agents
MeSH PA	D012102	Reproductive Control Agents

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

Disease	Relation	SNOMED_ID	DOID
Advanced Prostatic Carcinoma	indication
Urinary tract obstruction	contraindication	7163005	DOID:5200
Hypercholesterolemia	contraindication	13644009
Hypertensive disorder	contraindication	38341003	DOID:10763
Spinal cord compression	contraindication	71286001
Diabetes mellitus	contraindication	73211009	DOID:9351
Hyperglycemia	contraindication	80394007	DOID:4195
Kidney disease	contraindication	90708001	DOID:557
Disease of liver	contraindication	235856003	DOID:409
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

Species	Use	Relation
Swine	Synchronization of the time of insemination	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
OvuGel	United-AH II LLC	1

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	12.81	acidic
pKa4	12.82	acidic
pKa5	13.17	acidic
pKa6	13.43	acidic
pKa7	13.43	acidic
pKa8	13.86	acidic
pKa9	10.75	Basic
pKa10	6.69	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 22.5MG BASE/VIAL	TRIPTODUR KIT	AZURITY	N208956	June 29, 2017	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	June 29, 2024	TREATMENT OF PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH CENTRAL PRECOCIOUS PUBERTY

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	EC50	9.03		WOMBAT-PK	CHEMBL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_RAT	AGONIST	Ki	8.80		IUPHAR

External reference:

ID	Source
4021400	VUID
N0000148818	NUI
D06247	KEGG_DRUG
124508-66-3	SECONDARY_CAS_RN
4021400	VANDF
4021401	VANDF
C0077275	UMLSCUI
CHEBI:63633	CHEBI
CHEMBL1201334	ChEMBL_ID
CHEMBL1200554	ChEMBL_ID
D017329	MESH_DESCRIPTOR_UI
DB06825	DRUGBANK_ID
1177	IUPHAR_LIGAND_ID
5711	INN_ID
9081Y98W2V	UNII
25074470	PUBCHEM_CID
236538	RXNORM
15638	MMSL
33432	MMSL
d04696	MMSL
004107	NDDF
006246	NDDF
008312	NDDF
008313	NDDF
009526	NDDF
327370004	SNOMEDCT_US
395915003	SNOMEDCT_US
425731006	SNOMEDCT_US
427385009	SNOMEDCT_US
140194-24-7	SECONDARY_CAS_RN

Pharmaceutical products:

None