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trientine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2738 | 112-24-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An ethylenediamine derivative used as stabilizer for EPOXY RESINS, as ampholyte for ISOELECTRIC FOCUSING and as chelating agent for copper in HEPATOLENTICULAR DEGENERATION.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.45 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 92.50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IRAK1,ITK,JAK1,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK7,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 55 | |||
| kinase-selectivity-class | AKT1,AKT2,AKT3,ALK,CAMK2A,CAMK2B,CAMK2D,CDK4,CHEK1,CHUK,CSF1R,DYRK1B,EIF2AK3,EPHB4,GAK,INSR,IRAK4,MAP3K7,MAP4K1,MAP4K3,MAPK7,MARK4,MELK,PAK1,PAK2,PAK4,PDK4,PDPK1,PRKACA,PRKCD,PTK2,SIK2,SIK3,STK33,SYK,TTK,ULK1,ULK2 | 38 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 25, 2019 | EMA | Univar BV | |
| Nov. 8, 1985 | FDA | ATON |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A16AX12 | ALIMENTARY TRACT AND METABOLISM OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS Various alimentary tract and metabolism products |
| FDA MoA | N0000020075 | Copper Chelating Activity |
| FDA MoA | N0000175472 | Metal Chelating Activity |
| MeSH PA | D002614 | Chelating Agents |
| MeSH PA | D064449 | Sequestering Agents |
| CHEBI has role | CHEBI:35842 | antirheumatic drug |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| FDA EPC | N0000194014 | Copper Chelator |
Related Drugs by ATC class:
A16AX Various alimentary tract and metabolism products 23 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Wilson's disease | indication | 88518009 | |
| Plaque psoriasis | indication | 200965009 | |
| Scalp psoriasis | indication | 238608008 | |
| Renal cell carcinoma | indication | 702391001 | DOID:4450 |
| Psoriasis | off-label use | 9014002 | DOID:8893 |
| Hypocalcemia | contraindication | 5291005 | |
| Acute hemorrhage | contraindication | 8573003 | |
| Congenital ichthyosis of skin | contraindication | 13059002 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Hypervitaminosis D | contraindication | 27712000 | DOID:9971 |
| Proteinuria | contraindication | 29738008 | DOID:576 |
| Torsades de pointes | contraindication | 31722008 | |
| Guttate psoriasis | contraindication | 37042000 | |
| Gastrointestinal fistula | contraindication | 37831005 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Hypokalemia | contraindication | 43339004 | |
| Gastrointestinal perforation | contraindication | 51875005 | |
| Hepatic failure | contraindication | 59927004 | |
| Diarrhea | contraindication | 62315008 | |
| Hypercalcemia | contraindication | 66931009 | DOID:12678 |
| Disorder of calcium metabolism | contraindication | 71638002 | DOID:10575 |
| Hypercalciuria | contraindication | 71938000 | |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Pancreatitis | contraindication | 75694006 | DOID:4989 |
| Iron deficiency anemia | contraindication | 87522002 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Angina pectoris | contraindication | 194828000 | |
| Pustular psoriasis | contraindication | 200973000 | |
| Drug-induced hepatitis | contraindication | 235876009 | |
| Telangiectasia disorder | contraindication | 247479008 | |
| Cerebral hemorrhage | contraindication | 274100004 | |
| Pregnancy, function | contraindication | 289908002 | |
| Thromboembolic disorder | contraindication | 371039008 | |
| Adrenal cortical hypofunction | contraindication | 386584007 | DOID:10493 |
| Surgical procedure | contraindication | 387713003 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Atrophoderma | contraindication | 399979006 | |
| Peripheral vascular disease | contraindication | 400047006 | |
| UGT1A1*28 polymorphism | contraindication | 430235005 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Acute Thromboembolic Stroke | 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 | 10.93 | Basic |
| pKa2 | 6.93 | Basic |
| pKa3 | 6.19 | Basic |
| pKa4 | 5.58 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 300MG | CUVRIOR | ORPHALAN | N215760 | April 28, 2022 | RX | TABLET | ORAL | 11072577 | May 3, 2039 | A METHOD FOR THE TREATMENT OF ADULT PATIENTS WITH STABLE WILSON’S DISEASE WHO ARE DE-COPPERED AND TOLERANT TO PENICILLAMINE |
| 300MG | CUVRIOR | ORPHALAN | N215760 | April 28, 2022 | RX | TABLET | ORAL | 12358861 | May 3, 2039 | A METHOD FOR THE TREATMENT OF ADULT PATIENTS WITH STABLE WILSONS DISEASE WHO ARE DE-COPPERED AND TOLERANT TO PENICILLAMINE |
| 300MG | CUVRIOR | ORPHALAN | N215760 | April 28, 2022 | RX | TABLET | ORAL | 12358862 | May 3, 2039 | A METHOD FOR THE TREATMENT OF ADULT PATIENTS WITH STABLE WILSONS DISEASE WHO ARE DE-COPPERED AND TOLERANT TO PENICILLAMINE |
| 300MG | CUVRIOR | ORPHALAN | N215760 | April 28, 2022 | RX | TABLET | ORAL | 12662445 | May 3, 2039 | A METHOD FOR THE TREATMENT OF ADULT PATIENTS WITH STABLE WILSONS DISEASE WHO ARE DE-COPPERED AND TOLERANT TO PENICILLAMINE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 300MG | CUVRIOR | ORPHALAN | N215760 | April 28, 2022 | RX | TABLET | ORAL | April 28, 2029 | TREATMENT OF ADULT PATIENTS WITH STABLE WILSON’S DISEASE WHO ARE DE-COPPERED AND TOLERANT TO PENICILLAMINE |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Carbonic anhydrase 2 | Enzyme | Ki | 4.19 | CHEMBL | |||||
| Carbonic anhydrase 1 | Enzyme | Ki | 4 | CHEMBL | |||||
| Carbonic anhydrase 4 | Enzyme | Ki | 4.46 | CHEMBL | |||||
| Carbonic anhydrase 9 | Enzyme | Ki | 4.41 | CHEMBL | |||||
| Carbonic anhydrase 12 | Enzyme | Ki | 4.24 | CHEMBL | |||||
| Carbonic anhydrase 5A, mitochondrial | Enzyme | Ki | 4.42 | CHEMBL | |||||
| Carbonic anhydrase 5B, mitochondrial | Enzyme | Ki | 4.31 | CHEMBL | |||||
| Carbonic anhydrase 7 | Enzyme | Ki | 4.35 | CHEMBL | |||||
| Carbonic anhydrase 3 | Enzyme | Ki | 4.32 | CHEMBL | |||||
| Carbonic anhydrase 6 | Enzyme | Ki | 4.37 | CHEMBL | |||||
| Carbonic anhydrase 14 | Enzyme | Ki | 4.92 | CHEMBL | |||||
| Carbonic anhydrase 13 | Enzyme | Ki | 4.28 | CHEMBL | |||||
| Carbonic anhydrase 15 | Enzyme | Ki | 4.23 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019956 | VUID |
| N0000148041 | NUI |
| D00736 | KEGG_DRUG |
| 38260-01-4 | SECONDARY_CAS_RN |
| 4017951 | VANDF |
| 4019956 | VANDF |
| 4042163 | VANDF |
| C0040976 | UMLSCUI |
| CHEBI:39501 | CHEBI |
| 104 | PDB_CHEM_ID |
| CHEMBL609 | ChEMBL_ID |
| DB06824 | DRUGBANK_ID |
| CHEMBL3989777 | ChEMBL_ID |
| D014266 | MESH_DESCRIPTOR_UI |
| 5565 | PUBCHEM_CID |
| 4664 | INN_ID |
| SJ76Y07H5F | UNII |
| 10798 | RXNORM |
| 269581 | MMSL |
| 36945 | MMSL |
| 40736 | MMSL |
| 5623 | MMSL |
| d01416 | MMSL |
| 001093 | NDDF |
| 004541 | NDDF |
| 018063 | NDDF |
| 109102003 | SNOMEDCT_US |
| 109103008 | SNOMEDCT_US |
| 1149496005 | SNOMEDCT_US |
| 373456001 | SNOMEDCT_US |
| CHEMBL5095420 | ChEMBL_ID |
| 4961-40-4 | SECONDARY_CAS_RN |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Syprine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-2120 | CAPSULE | 250 mg | ORAL | NDA | 23 sections |
| Trientine Hydrochloride | Human Prescription Drug Label | 1 | 16571-810 | CAPSULE | 250 mg | ORAL | ANDA | 20 sections |
| Trientine Hydrochloride | Human Prescription Drug Label | 1 | 16571-810 | CAPSULE | 250 mg | ORAL | ANDA | 20 sections |
| Trientine Hydrochloride | Human Prescription Drug Label | 1 | 16571-812 | CAPSULE | 500 mg | ORAL | ANDA | 20 sections |
| Trientine Hydrochloride | Human Prescription Drug Label | 1 | 16571-812 | CAPSULE | 500 mg | ORAL | ANDA | 20 sections |
| Trientine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-470 | CAPSULE | 250 mg | ORAL | ANDA | 23 sections |
| TRIENTINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-683 | CAPSULE | 250 mg | ORAL | ANDA | 20 sections |
| Trientine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-459 | CAPSULE | 250 mg | ORAL | ANDA | 19 sections |
| Trientine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49884-060 | CAPSULE | 250 mg | ORAL | ANDA | 15 sections |
| Trientine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68475-200 | CAPSULE | 250 mg | ORAL | ANDA | 20 sections |
| Trientine hydrochloride | Human Prescription Drug Label | 1 | 72205-008 | CAPSULE | 250 mg | ORAL | ANDA | 20 sections |
| CUVRIOR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 81802-001 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 29 sections |