fexinidazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antiprotozoals and radiosensitizers, metronidazole derivatives 5466 59729-37-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fexinidazole
  • HOE 239
  • fexinidazole winthrop
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.
  • Molecular weight: 279.31
  • Formula: C12H13N3O3S
  • CLOGP: 2.38
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 72.87
  • ALOGS: -3.48
  • ROTB: 5

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.44 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

IDSource
306ERL82IR UNII
D11252 KEGG_DRUG
C0060304 UMLSCUI
CHEMBL1631694 ChEMBL_ID
68792 PUBCHEM_CID
DB12265 DRUGBANK_ID
2564146 RXNORM
39720 MMSL
d09773 MMSL
1179076004 SNOMEDCT_US
890462007 SNOMEDCT_US
4040717 VANDF
018813 NDDF
C038307 MESH_SUPPLEMENTAL_RECORD_UI
4142 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fexinidazole HUMAN PRESCRIPTION DRUG LABEL 1 0024-4512 TABLET 600 mg ORAL NDA 32 sections