fexinidazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiprotozoals and radiosensitizers, metronidazole derivatives | 5466 | 59729-37-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Studies with Trypanosoma brucei and other protozoans suggest that, like for other nitrocontaining drugs, the nitroreductase (NTR) enzyme plays an important role in the bioactivation of fexinidazole resulting in generation of reactive amines and damage to DNA and proteins. The activity of fexinidazole and its metabolites (M1 and M2) is trypanocidal and appears to be concentration and time dependent. However, the precise mechanism by which fexinidazole and the two metabolites exhibit activity against T. brucei is not known.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.44 | g | O |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 16, 2021 | FDA | SANOFI |
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 | P01CA03 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS Nitroimidazole derivatives |
| FDA CS | M0014907 | Nitroimidazoles |
| FDA EPC | N0000175435 | Nitroimidazole Antimicrobial |
| FDA MoA | N0000182137 | Cytochrome P450 2D6 Inhibitors |
| FDA MoA | N0000182138 | Cytochrome P450 1A2 Inhibitors |
| FDA MoA | N0000182139 | Cytochrome P450 2B6 Inhibitors |
| FDA MoA | N0000182140 | Cytochrome P450 2C19 Inhibitors |
| FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
| FDA MoA | N0000187061 | Organic Cation Transporter 2 Inhibitors |
| FDA MoA | N0000187064 | Cytochrome P450 2B6 Inducers |
| FDA MoA | N0000190107 | Organic Anion Transporting Polypeptide 1B1 Inhibitors |
| FDA MoA | N0000190108 | Organic Anion Transporting Polypeptide 1B3 Inhibitors |
| FDA MoA | N0000190110 | Organic Anion Transporter 1 Inhibitors |
| FDA MoA | N0000190111 | Organic Anion Transporter 3 Inhibitors |
| FDA MoA | N0000190115 | Cytochrome P450 3A5 Inhibitors |
| FDA MoA | N0000191266 | Cytochrome P450 1A2 Inducers |
| FDA MoA | N0000191423 | Multidrug and Toxin Extrusion Transporter 1 Inhibitors |
| FDA MoA | N0000193932 | Multidrug and Toxin Extrusion Transporter 2 K Inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human African trypanosomiasis (HAT) due to Trypanosoma brucei gambiense | indication | 27031003 | DOID:10112 |
| Hepatic impairment | contraindication | 59927004 |
🐶 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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 600MG | FEXINIDAZOLE | SANOFI | N214429 | July 16, 2021 | RX | TABLET | ORAL | July 16, 2026 | NEW CHEMICAL ENTITY |
| 600MG | FEXINIDAZOLE | SANOFI | N214429 | July 16, 2021 | RX | TABLET | ORAL | July 16, 2028 | FOR THE TREATMENT OF BOTH THE FIRST-STAGE (HEMOLYMPHATIC) AND SECOND-STAGE (MENINGOENCEPHALITIC) HUMAN AFRICAN TRYPANOSOMIASIS (HAT) DUE TO TRYPANOSOMA BRUCEI GAMBIENSE IN PATIENTS 6 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 20 KG |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 306ERL82IR | UNII |
| D11252 | KEGG_DRUG |
| C0060304 | UMLSCUI |
| CHEMBL1631694 | ChEMBL_ID |
| 68792 | PUBCHEM_CID |
| DB12265 | DRUGBANK_ID |
| 4142 | INN_ID |
| 018813 | NDDF |
| 1179076004 | SNOMEDCT_US |
| 890462007 | SNOMEDCT_US |
| 4040717 | VANDF |
| 2564146 | RXNORM |
| 39720 | MMSL |
| d09773 | MMSL |
| C038307 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Fexinidazole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0024-4512 | TABLET | 600 mg | ORAL | NDA | 32 sections |
| Fexinidazole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0024-4512 | TABLET | 600 mg | ORAL | NDA | 32 sections |