AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
Try a sample question
Select a question to fill the search bar, then submit it or edit it first.
AI can make mistakes. Verify answers against the original sources before relying on them.
pemafibrate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| clofibrate derivatives, peroxisome proliferator activated receptor-alpha(PPAR-alpha) agonists | 5248 | 848259-27-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Pemafibrate is a selective PPAR-alpha modulator (SPPARM-alpha) that has antihyperlipidaemic activity.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| CL (Clearance) | 4.28 mL/min/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| Vd (Volume of distribution) | 0.91 L/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| BA (Bioavailability) | 0.62 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.178 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 8.531 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 77.983 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 9.594 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.200 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.480 | % | High | 1 |
| herg | hERG pIC50 | 4.769 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 25.061 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 68.865 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.260 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK | 18 | |||
| kinase-selectivity-class | AXL,BRAF,DYRK1B,EIF2AK3,GRK2,MAP2K6 | 6 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 3.724 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 21.038 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 26.915 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.350 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 29.854 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.470 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.023 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 63.826 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 17.510 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.240 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 575.440 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 3, 2017 | PMDA | Kowa |
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 | C10AB12 | CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Fibrates |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35679 | antilipemic drug |
| CHEBI has role | CHEBI:62868 | hepatoprotective agent |
| CHEBI has role | CHEBI:70782 | PPARα agonist |
| CHEBI has role | CHEBI:35821 | anticholesteremic drug |
Related Drugs by ATC class:
C10AB Fibrates 11 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dyslipidemia | indication | 370992007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.58 | acidic |
| pKa2 | 1.94 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor alpha | Nuclear hormone receptor | AGONIST | EC50 | 9 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Peroxisome proliferator-activated receptor gamma | Nuclear hormone receptor | AGONIST | EC50 | 5.96 | SCIENTIFIC LITERATURE | ||||
| Peroxisome proliferator-activated receptor delta | Nuclear hormone receptor | AGONIST | EC50 | 5.80 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 17VGG92R23 | UNII |
| C4547051 | UMLSCUI |
| CHEMBL247951 | ChEMBL_ID |
| 11526038 | PUBCHEM_CID |
| DB15212 | DRUGBANK_ID |
| D10711 | KEGG_DRUG |
| CHEMBL3545412 | ChEMBL_ID |
| 9692 | INN_ID |
| C540740 | MESH_SUPPLEMENTAL_RECORD_UI |
| CHEBI:228365 | CHEBI |
| P7F | PDB_CHEM_ID |
| 17VGG92R23 | INXIGHT DRUGS |
Pharmaceutical products:
None