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 |
|---|---|
|
Synonyms:
|
A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE with D-tryptophan substitution at residue 6.
|
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 |
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 | 205.65 | 48.21 | 38 | 956 | 3206 | 50600924 |
| Needle issue | 192.02 | 48.21 | 41 | 953 | 7234 | 50596896 |
| Disease progression | 180.03 | 48.21 | 68 | 926 | 95798 | 50508332 |
| Product use complaint | 132.79 | 48.21 | 24 | 970 | 1778 | 50602352 |
| Off label use | 124.47 | 48.21 | 89 | 905 | 474337 | 50129793 |
| Product prescribing issue | 120.93 | 48.21 | 21 | 973 | 1235 | 50602895 |
| Progesterone increased | 91.19 | 48.21 | 11 | 983 | 41 | 50604089 |
| Osteonecrosis of jaw | 60.31 | 48.21 | 23 | 971 | 32503 | 50571627 |
| Product physical issue | 52.55 | 48.21 | 13 | 981 | 4319 | 50599811 |
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 | 83.27 | 26.48 | 32 | 2096 | 12532 | 29559867 |
| Product prescribing issue | 57.76 | 26.48 | 14 | 2114 | 1153 | 29571246 |
| Femoral neck fracture | 54.24 | 26.48 | 16 | 2112 | 2787 | 29569612 |
| Osteonecrosis of jaw | 52.49 | 26.48 | 25 | 2103 | 16485 | 29555914 |
| Syringe issue | 45.48 | 26.48 | 15 | 2113 | 3763 | 29568636 |
| Needle issue | 42.33 | 26.48 | 15 | 2113 | 4668 | 29567731 |
| Metastases to bone | 37.71 | 26.48 | 17 | 2111 | 9881 | 29562518 |
| Hot flush | 36.81 | 26.48 | 19 | 2109 | 14851 | 29557548 |
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 |
|---|---|---|---|---|---|---|
| Needle issue | 162.21 | 25.58 | 43 | 2531 | 9229 | 64486929 |
| Ovarian hyperstimulation syndrome | 132.02 | 25.58 | 29 | 2545 | 2816 | 64493342 |
| Osteonecrosis of jaw | 100.73 | 25.58 | 43 | 2531 | 39782 | 64456376 |
| Progesterone increased | 83.57 | 25.58 | 11 | 2563 | 40 | 64496118 |
| Product use complaint | 77.57 | 25.58 | 17 | 2557 | 1629 | 64494529 |
| Prostatic specific antigen increased | 73.74 | 25.58 | 23 | 2551 | 8737 | 64487421 |
| Product prescribing issue | 57.12 | 25.58 | 14 | 2560 | 2187 | 64493971 |
| Syringe issue | 47.88 | 25.58 | 14 | 2560 | 4272 | 64491886 |
| Incorrect dose administered | 45.53 | 25.58 | 29 | 2545 | 60736 | 64435422 |
| Femoral neck fracture | 41.84 | 25.58 | 15 | 2559 | 8709 | 64487449 |
| Product physical issue | 41.78 | 25.58 | 12 | 2562 | 3437 | 64492721 |
| Metastases to bone | 41.70 | 25.58 | 19 | 2555 | 20416 | 64475742 |
| Off label use | 40.47 | 25.58 | 82 | 2492 | 632724 | 63863434 |
| Product reconstitution quality issue | 34.22 | 25.58 | 6 | 2568 | 179 | 64495979 |
| Product deposit | 29.61 | 25.58 | 6 | 2568 | 393 | 64495765 |
| Hot flush | 29.57 | 25.58 | 20 | 2554 | 46215 | 64449943 |
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 | ARBOR PHARMS LLC | 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 | AGONIST | EC50 | 9.03 | WOMBAT-PK | CHEMBL | |||
| Gonadotropin-releasing hormone receptor | GPCR | 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 |
| 140194-24-7 | SECONDARY_CAS_RN |
| 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 |
Pharmaceutical products:
None