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benznidazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiprotozoals and radiosensitizers, metronidazole derivatives | 322 | 22994-85-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Benznidazole inhibits the synthesis of DNA, RNA, and proteins within the T. cruzi parasite. Studies suggest that benznidazole is reduced by a Type I nitroreductase (NTR) enzyme of T. cruzi producing a series of short-lived intermediates that may promote damage to several macromolecules including DNA. In mammalian cells, however, benznidazole is metabolized by reduction of the nitro group to an amino group by a Type II NTR enzyme. The precise mechanism of action is not known. Benznidazole is active against all three stages, trypomastigotes, amastigotes, and epimastigotes, of T. cruzi. However, the sensitivity of T. cruzi strains to benznidazole, from different geographic regions, may vary.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.40 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 100 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK7,MAPK9,MARK4,MET,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 42 | |||
| kinase-selectivity-class | AXL,GRK2,PDK4 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 29, 2017 | FDA | CHEMO RESEARCH SL |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| American trypanosomiasis | 64.87 | 60.87 | 7 | 39 | 627 | 110588626 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | P01CA02 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS Nitroimidazole derivatives |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| MeSH PA | D007155 | Immunologic Factors |
| MeSH PA | D007166 | Immunosuppressive Agents |
| MeSH PA | D009153 | Mutagens |
| MeSH PA | D009676 | Noxae |
| MeSH PA | D014344 | Trypanocidal Agents |
| CHEBI has role | CHEBI:35820 | antiprotozoal drug |
| CHEBI has role | CHEBI:36335 | trypanocidal drug |
| CHEBI has role | CHEBI:70868 | antileishmanial agent |
Related Drugs by ATC class:
P01CA Nitroimidazole derivatives 1 drug
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Infection by Trypanosoma cruzi | indication | 77506005 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.65 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D02489 | KEGG_DRUG |
| 18994 | RXNORM |
| C0053230 | UMLSCUI |
| CHEBI:133833 | CHEBI |
| CHEMBL110 | ChEMBL_ID |
| DB11989 | DRUGBANK_ID |
| 31593 | PUBCHEM_CID |
| C009999 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3541 | INN_ID |
| YC42NRJ1ZD | UNII |
| 261813 | MMSL |
| 27035 | MMSL |
| d07580 | MMSL |
| 4037055 | VANDF |
| 008175 | NDDF |
| 714091003 | SNOMEDCT_US |
| 714092005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Benznidazole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0642-7463 | TABLET | 12.50 mg | ORAL | NDA | 31 sections |
| Benznidazole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0642-7464 | TABLET | 100 mg | ORAL | NDA | 31 sections |