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cepharanthine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5375 | 481-49-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The mechanism of action of cepharanthine is multifactorial. The drug exerts membrane effects (modulation of efflux pumps, membrane rigidification) as well as different intracellular and nuclear effects. Cepharanthine interferes with several metabolic axes, primarily with the AMP-activated protein kinase (AMPK) and NFkappaB signaling pathways. In particular, the anti-inflammatory effects of cepharanthine rely on AMPK activation and NFkappaB inhibition.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.160 | Moderate | 0.70 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.495 | Moderate | 0.70 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 29.242 | 10^-6 cm/s | Moderate | 0.70 |
| dh-clint | Dog hepatocyte intrinsic clearance | 36.475 | uL/min/10^6 cells | Moderate | 0.70 |
| dppb | Dog plasma protein binding (% unbound) | 6.050 | % | Moderate | 0.70 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 21.050 | % | Moderate | 0.70 |
| herg | hERG pIC50 | 5.772 | pIC50 | Moderate | 0.70 |
| hh-clint | Human hepatocyte intrinsic clearance | 18.880 | uL/min/10^6 cells | Moderate | 0.70 |
| hlm-clint | Human liver microsomal intrinsic clearance | 51.761 | uL/min/mg protein | Moderate | 0.70 |
| hppb | Human plasma protein binding (% unbound) | 5.680 | % | Moderate | 0.70 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK,ZAP70 | 44 | |||
| kinase-selectivity-class | ACVR2B | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.682 | Moderate | 0.70 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 141.906 | Moderate | 0.70 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.050 | Moderate | 0.70 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.799 | Moderate | 0.70 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 17.550 | % | Moderate | 0.70 |
| rh-clint | Rat hepatocyte intrinsic clearance | 197.242 | uL/min/10^6 cells | Moderate | 0.70 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 33.900 | % | Moderate | 0.70 |
| rppb | Rat plasma protein binding (% unbound) | 5.410 | % | Moderate | 0.70 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 213.304 | uM | Moderate | 0.70 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1951 | PMDA |
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 |
|---|---|---|
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D000972 | Antineoplastic Agents, Phytogenic |
| MeSH PA | D011837 | Radiation-Protective Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| MeSH PA | D020011 | Protective Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Alopecia | indication | 56317004 | DOID:987 |
| Leukopenia | indication | 84828003 | DOID:615 |
| Aptyalism | indication | 87715008 | |
| Snake bite - wound | indication | 283840005 | |
| Coronavirus infection | off-label use | 186747009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.38 | Basic |
| pKa2 | 7.62 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| 5'-AMP-activated protein kinase catalytic subunit alpha-1 | Kinase | INHIBITOR | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Nuclear factor NF-kappa-B p105 subunit | Cytosolic other | INHIBITOR | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Small conductance calcium-activated potassium channel protein 3 | Ion channel | Ki | 5.96 | CHEMBL | |||||
| Small conductance calcium-activated potassium channel protein 2 | Ion channel | Ki | 5.88 | CHEMBL | |||||
| Trypanothione reductase | Enzyme | Ki | 5.12 | CHEMBL | |||||
| Replicase polyprotein 1ab | Enzyme | IC50 | 7 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 7592YJ0J6T | UNII |
| C0055082 | UMLSCUI |
| CHEBI:3546 | CHEBI |
| CHEMBL449782 | ChEMBL_ID |
| 10206 | PUBCHEM_CID |
| DB16824 | DRUGBANK_ID |
| CHEMBL2074948 | ChEMBL_ID |
| C006947 | MESH_SUPPLEMENTAL_RECORD_UI |
| D01035 | KEGG_DRUG |
Pharmaceutical products:
None