halofantrine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1350 | 69756-53-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
used in treatment of mild to moderate acute malaria
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 49.96 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 6.30 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 24, 1992 | FDA | GLAXOSMITHKLINE |
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 | P01BX01 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Other antimalarials |
| FDA EPC | N0000175482 | Antimalarial |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000962 | Antimalarials |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vivax malaria | indication | 27052006 | DOID:12978 |
| Falciparum malaria | indication | 62676009 | DOID:14067 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Prolonged QT interval | contraindication | 111975006 | |
| Atrioventricular Conduction Defect | 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 | 12.53 | acidic |
| pKa2 | 9.06 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 5.12 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021108 | VUID |
| N0000148563 | NUI |
| D02485 | KEGG_DRUG |
| 36167-63-2 | SECONDARY_CAS_RN |
| 4021108 | VANDF |
| 4024114 | VANDF |
| C0120726 | UMLSCUI |
| CHEBI:5612 | CHEBI |
| CHEMBL1107 | ChEMBL_ID |
| CHEMBL1200901 | ChEMBL_ID |
| DB01218 | DRUGBANK_ID |
| C023768 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10019 | IUPHAR_LIGAND_ID |
| 4749 | INN_ID |
| Q2OS4303HZ | UNII |
| 37393 | PUBCHEM_CID |
| 151844 | RXNORM |
| 17110 | MMSL |
| 46102 | MMSL |
| d04842 | MMSL |
| 003977 | NDDF |
| 003978 | NDDF |
| 108681001 | SNOMEDCT_US |
| 108682008 | SNOMEDCT_US |
| 372527008 | SNOMEDCT_US |
Pharmaceutical products:
None