tafenoquine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| quinoline derivatives | 3578 | 106635-80-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tafenoquine, an 8-aminoquinoline antimalarial, is active against all the stages of Plasmodium species that include the hypnozoite (dormant stage) in the liver. Studies in vitro with the erythrocytic forms of Plasmodium falciparum suggest that tafenoquine may exert its effect by inhibiting hematin polymerization and inducing apoptotic like death of the parasite. In addition to its effect on the parasite, tafenoquine causes red blood cell shrinkage in vitro. The molecular target of tafenoquine is not known.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.54 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 20, 2018 | 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 | P01BA07 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Aminoquinolines |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000962 | Antimalarials |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| CHEBI has role | CHEBI:36335 | trypanocidal drugs |
| CHEBI has role | CHEBI:38068 | antimalarials |
| CHEBI has role | CHEBI:68495 | Type I cell-death inducers |
| CHEBI has role | CHEBI:70868 | antileishmanial drugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malaria | indication | 61462000 | DOID:12365 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.77 | Basic |
| pKa2 | 2.92 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 100MG BASE | ARAKODA | 60 DEGREES PHARMS | N210607 | Aug. 8, 2018 | RX | TABLET | ORAL | 10342791 | Dec. 2, 2035 | FOR THE ORAL PREVENTION/PROPHYLAXIS OF MALARIA IN ADULTS, COMPRISING A THREE-PHASE DOSING REGIMEN CONSISTING OF A LOADING/INITIAL DOSE, A MAINTENANCE/EXPOSURE DOSE, AND A TERMINAL/POST-EXPOSURE DOSE |
| EQ 100MG BASE | ARAKODA | 60 DEGREES PHARMS | N210607 | Aug. 8, 2018 | RX | TABLET | ORAL | 10888558 | Dec. 2, 2035 | FOR THE ORAL PREVENTION/PROPHYLAXIS OF MALARIA IN ADULTS, COMPRISING A THREE-PHASE DOSING REGIMEN CONSISTING OF A LOADING/INITIAL DOSE, A MAINTENANCE/EXPOSURE DOSE, AND A TERMINAL/POST-EXPOSURE DOSE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 100MG BASE | ARAKODA | 60 DEGREES PHARMS | N210607 | Aug. 8, 2018 | RX | TABLET | ORAL | July 20, 2023 | NEW CHEMICAL ENTITY |
| EQ 150MG BASE | KRINTAFEL | GLAXOSMITHKLINE | N210795 | July 20, 2018 | RX | TABLET | ORAL | July 20, 2023 | NEW CHEMICAL ENTITY |
| EQ 150MG BASE | KRINTAFEL | GLAXOSMITHKLINE | N210795 | July 20, 2018 | RX | TABLET | ORAL | July 20, 2025 | INDICATED FOR THE RADICAL CURE (PREVENTION OF RELAPSE) OF PLASMODIUM VIVAX MALARIA IN PATIENTS AGED 16 YEARS AND OLDER WHO ARE RECEIVING APPROPRIATE ANTIMALARIAL THERAPY FOR ACUTE P. VIVAX INFECTION |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D10490 | KEGG_DRUG |
| 106635-81-8 | SECONDARY_CAS_RN |
| 4037963 | VANDF |
| C0903411 | UMLSCUI |
| CHEBI:135752 | CHEBI |
| H3F | PDB_CHEM_ID |
| CHEMBL298470 | ChEMBL_ID |
| CHEMBL2364635 | ChEMBL_ID |
| DB06608 | DRUGBANK_ID |
| C055852 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9722 | IUPHAR_LIGAND_ID |
| 7835 | INN_ID |
| 262P8GS9L9 | UNII |
| 115358 | PUBCHEM_CID |
| 2054023 | RXNORM |
| 286549 | MMSL |
| 287722 | MMSL |
| 34723 | MMSL |
| d08853 | MMSL |
| 017662 | NDDF |
| 017663 | NDDF |
| 773181000 | SNOMEDCT_US |
| 773236009 | SNOMEDCT_US |
| 773237000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Krintafel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0889 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 29 sections |
| Krintafel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0889 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 29 sections |
| Krintafel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0889 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 29 sections |
| Arakoda | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71475-257 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 29 sections |
| Arakoda | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71475-257 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 29 sections |