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carotegrast methyl 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| integrin antagonists | 5688 | 401905-67-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Carotegrast methyl is a small-molecule alpha4 integrin antagonist which received its first approval in Japan for the treatment of moderate ulcerative colitis in patients who had inadequate response to 5-aminosalicylic acid. The active metabolite of carotegrast methyl exerts an anti-inflammatory effect by blocking the interaction of alpha4beta1 or alpha4beta7 integrins and their ligands, VCAM-1 and MAd-CAM-1, thereby inhibiting the adhesion of inflammatory cells, including T cells, to vascular endothelial cells and extravasation into inflammatory sites.
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Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,JAK3,KIT,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 | 53 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DDR1,EIF2AK3,GRK2,MAPK7,PDK4,SIK2,STK33,TEK | 11 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 28, 2022 | PMDA | EA Pharma Co., Ltd. |
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:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ulcerative colitis | indication | 64766004 | DOID:8577 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Integrin alpha-4/beta-1 | Adhesion | ANTAGONIST | Kd | 9.79 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Integrin alpha-4/beta-7 | Adhesion | ANTAGONIST | Kd | 9.34 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| C000588820 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10510 | IUPHAR_LIGAND_ID |
| DB16119 | DRUGBANK_ID |
| C5432284 | UMLSCUI |
| C5418324 | UMLSCUI |
| 401904-75-4 | SECONDARY_CAS_RN |
| D09799 | KEGG_DRUG |
| 9872780 | PUBCHEM_CID |
| 10120218 | PUBCHEM_CID |
| 10511 | IUPHAR_LIGAND_ID |
| OYK17DYO9M | UNII |
| 9224 | INN_ID |
| Y1HYC6SO3F | UNII |
Pharmaceutical products:
None