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artemisinin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antimalarial agents, artemisinin related compounds | 3871 | 63968-64-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
antimalarial from Chinese medicinal herb Artemisia annua
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.05 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 12.20 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.557 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.286 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 104.232 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 21.330 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.160 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 5.520 | % | High | 1 |
| herg | hERG pIC50 | 4.968 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.656 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 25.645 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.810 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK4,PRKDC,TEK | 16 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.929 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 71.285 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.650 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.576 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.970 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 55.847 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 9.340 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2.600 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 16.904 | uM | High | 1 |
Approvals:
None
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 | P01BE01 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Artemisinin and derivatives, plain |
| ATC | P01BF07 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Artemisinin and derivatives, combinations |
| ATC | P01BF08 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Artemisinin and derivatives, combinations |
| MeSH PA | D000890 | Anti-Infective Agents |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:38068 | antimalarial |
| CHEBI has role | CHEBI:76924 | plant metabolite |
Related Drugs by ATC class:
P01BE Artemisinin and derivatives, plain 4 drugs
P01BF Artemisinin and derivatives, combinations 11 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Falciparum malaria | indication | 62676009 | DOID:14067 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Enzyme | IC50 | 5.70 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| D02481 | KEGG_DRUG |
| C0052430 | UMLSCUI |
| CHEBI:223316 | CHEBI |
| A1EUW | PDB_CHEM_ID |
| CHEMBL269671 | ChEMBL_ID |
| DB13132 | DRUGBANK_ID |
| C031327 | MESH_SUPPLEMENTAL_RECORD_UI |
| 68827 | PUBCHEM_CID |
| 9954 | IUPHAR_LIGAND_ID |
| 5954 | INN_ID |
| 9RMU91N5K2 | UNII |
| 2367409 | RXNORM |
| 019140 | NDDF |
| 895350006 | SNOMEDCT_US |
| 96106001 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ArtemiC Rescue | HUMAN OTC DRUG LABEL | 4 | 83278-001 | SPRAY, SUSPENSION | 0.60 g | ORAL | unapproved drug other | 11 sections |