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pretomanid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5344 | 187235-37-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Pretomanid Tablet is a nitroimidazooxazine antimycobacterial drug. Pretomanid kills actively replicating M. tuberculosis by inhibiting mycolic acid biosynthesis, thereby blocking cell wall production. Under anaerobic conditions, against non-replicating bacteria, pretomanid acts as a respiratory poison following nitric oxide release
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.691 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.138 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 67.453 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 4.140 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 8.700 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 23.770 | % | High | 1 |
| herg | hERG pIC50 | 5.075 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.289 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 6.607 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 11.230 | % | High | 1 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,GSK3B,ITK,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,PDK1,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PRKDC,STK33,TEK,TTK,ZAP70 | 30 | |||
| kinase-selectivity-class | AXL,DYRK1B,EIF2AK3,GRK2,PDK4 | 5 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.016 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.449 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 15.417 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 10.430 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.492 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 14.320 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.316 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 6.745 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 54.420 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 9.780 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 112.980 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 14, 2019 | FDA | MYLAN IRELAND LTD | |
| July 31, 2020 | EMA | MYLAN IRELAND LIMITED |
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 |
|---|---|---|---|---|---|---|
| Neuropathy peripheral | 77.44 | 62.00 | 26 | 315 | 136944 | 90491162 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Death | 130.53 | 43.38 | 77 | 465 | 471108 | 42149685 |
| Anaemia | 66.57 | 43.38 | 42 | 500 | 280236 | 42340557 |
| Neuropathy peripheral | 53.85 | 43.38 | 26 | 516 | 101827 | 42518966 |
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 |
|---|---|---|---|---|---|---|
| Death | 220.84 | 49.12 | 107 | 775 | 698762 | 109889655 |
| Neuropathy peripheral | 126.92 | 49.12 | 49 | 833 | 179228 | 110409189 |
| Anaemia | 114.32 | 49.12 | 64 | 818 | 547022 | 110041395 |
| Electrocardiogram QT prolonged | 63.59 | 49.12 | 26 | 856 | 108934 | 110479483 |
| Optic neuritis | 51.99 | 49.12 | 13 | 869 | 11134 | 110577283 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J04AK08 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Other drugs for treatment of tuberculosis |
| FDA EPC | N0000175483 | Antimycobacterial |
| FDA MoA | N0000190111 | Organic Anion Transporter 3 Inhibitors |
| CHEBI has role | CHEBI:33231 | antitubercular agent |
Related Drugs by ATC class:
J04AK Other drugs for treatment of tuberculosis 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Extensively drug resistant tuberculosis | indication | 710106005 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.39 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| 200MG | PRETOMANID | MYLAN IRELAND LTD | N212862 | Aug. 14, 2019 | RX | TABLET | ORAL | Aug. 14, 2024 | NEW CHEMICAL ENTITY |
| 200MG | PRETOMANID | MYLAN IRELAND LTD | N212862 | Aug. 14, 2019 | RX | TABLET | ORAL | Aug. 14, 2026 | INDICATED AS PART OF A COMBINATION REGIMEN WITH BEDAQUILINE AND LINEZOLID FOR THE TREATMENT OF ADULTS WITH PULMONARY EXTENSIVELY DRUG RESISTANT (XDR) OR TREATMENT-INTOLERANT OR NONRESPONSIVE MULTIDRUG-RESISTANT (MDR) TUBERCULOSIS (TB) |
| 200MG | PRETOMANID | MYLAN IRELAND LTD | N212862 | Aug. 14, 2019 | RX | TABLET | ORAL | Aug. 14, 2029 | GENERATING ANTIBIOTIC INCENTIVES NOW |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 2XOI31YC4N | UNII |
| 4038950 | VANDF |
| C4310440 | UMLSCUI |
| CHEBI:748780 | CHEBI |
| CHEMBL227875 | ChEMBL_ID |
| 456199 | PUBCHEM_CID |
| DB05154 | DRUGBANK_ID |
| D10722 | KEGG_DRUG |
| 9871 | INN_ID |
| C410767 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11172 | IUPHAR_LIGAND_ID |
| 789316005 | SNOMEDCT_US |
| 789321008 | SNOMEDCT_US |
| 321727 | MMSL |
| 37322 | MMSL |
| d09355 | MMSL |
| 018085 | NDDF |
| 2198359 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pretomanid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49502-476 | TABLET | 200 mg | ORAL | NDA | 30 sections |