benznidazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 29, 2017 | FDA | CHEMO RESEARCH SL |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Cross sensitivity reaction | 36.37 | 24.61 | 4 | 3 | 2158 | 63486857 |
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 | 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 drugs |
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 100MG | BENZNIDAZOLE | CHEMO RESEARCH SL | N209570 | Aug. 29, 2017 | RX | TABLET | ORAL | Aug. 29, 2024 | FOR USE IN CHILDREN AGES 2 TO 12 YEARS OLD WITH CHAGAS DISEASE |
| 12.5MG | BENZNIDAZOLE | CHEMO RESEARCH SL | N209570 | Aug. 29, 2017 | RX | TABLET | ORAL | Aug. 29, 2024 | FOR USE IN CHILDREN AGES 2 TO 12 YEARS OLD WITH CHAGAS DISEASE |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D02489 | KEGG_DRUG |
| 18994 | RXNORM |
| C0053230 | UMLSCUI |
| CHEBI:133833 | CHEBI |
| CHEMBL110 | ChEMBL_ID |
| DB11989 | DRUGBANK_ID |
| C009999 | MESH_SUPPLEMENTAL_RECORD_UI |
| 31593 | PUBCHEM_CID |
| 3541 | INN_ID |
| YC42NRJ1ZD | UNII |
| 261813 | MMSL |
| 27035 | MMSL |
| d07580 | MMSL |
| 714091003 | SNOMEDCT_US |
| 714092005 | SNOMEDCT_US |
| 4037055 | VANDF |
| 008175 | NDDF |
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 | 0642-7463 | TABLET | 12.50 mg | ORAL | NDA | 31 sections |
| Benznidazole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0642-7464 | TABLET | 100 mg | ORAL | NDA | 31 sections |
| Benznidazole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0642-7464 | TABLET | 100 mg | ORAL | NDA | 31 sections |