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

Stem definitionDrug idCAS RN
4993 881681-00-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vonoprazan
  • vonoprazan fumarate
  • takecab
  • TAK-438
a potassium-competitive proton pump blocker for the treatment of acid-related disorders. Its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19 was investigated. Accordingly, it is recommended to use tocilizumabin combination with dexamethasone (or another corticosteroid at an equivalent dose) in certain hospitalized patients who are exhibiting rapid respiratory decompensation caused by COVID-19.
  • Molecular weight: 345.39
  • Formula: C17H16FN3O2S
  • CLOGP: 2.54
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 63.99
  • ALOGS: -3.85
  • ROTB: 4

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 26, 2014 PMDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hepatic function abnormal 72.93 28.42 31 1726 32650 50570717
Platelet count decreased 68.84 28.42 43 1714 100683 50502684
Decreased appetite 42.55 28.42 43 1714 200880 50402487
Anaemia 36.11 28.42 44 1713 252412 50350955
Cardiac failure 33.99 28.42 25 1732 76015 50527352
Interstitial lung disease 29.59 28.42 20 1737 53156 50550211

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Interstitial lung disease 105.47 25.22 60 2055 57658 29514754
Hepatic function abnormal 64.10 25.22 38 2077 39221 29533191
Oesophagitis 37.82 25.22 18 2097 11905 29560507
Renal impairment 35.66 25.22 36 2079 81297 29491115
Radiation pneumonitis 31.57 25.22 10 2105 2219 29570193
Cerebral infarction 30.40 25.22 20 2095 24655 29547757
Adrenal insufficiency 29.91 25.22 15 2100 11099 29561313
Cardiac failure 29.21 25.22 32 2083 79255 29493157
Cholangitis acute 27.56 25.22 7 2108 702 29571710
Immune-mediated enterocolitis 25.85 25.22 8 2107 1645 29570767

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Interstitial lung disease 127.28 23.27 79 4104 97653 64396896
Hepatic function abnormal 120.89 23.27 66 4117 64247 64430302
Platelet count decreased 69.76 23.27 69 4114 167642 64326907
Cardiac failure 57.88 23.27 56 4127 132317 64362232
Decreased appetite 55.48 23.27 79 4104 281210 64213339
Renal impairment 53.24 23.27 54 4129 134963 64359586
Cerebral infarction 47.86 23.27 31 4152 41013 64453536
Neutrophil count decreased 38.18 23.27 35 4148 77161 64417388
Hypergastrinaemia 37.79 23.27 7 4176 173 64494376
Enterocolitis 36.21 23.27 17 4166 12001 64482548
Pneumonia aspiration 35.57 23.27 30 4153 59241 64435308
Anaemia 33.60 23.27 75 4108 378605 64115944
Immune-mediated enterocolitis 30.80 23.27 10 4173 2646 64491903
Pneumonia bacterial 29.77 23.27 16 4167 15019 64479530
Adrenal insufficiency 28.73 23.27 18 4165 22469 64472080
Radiation pneumonitis 28.59 23.27 10 4173 3318 64491231
Oesophagitis 26.84 23.27 17 4166 21613 64472936
Marasmus 26.82 23.27 7 4176 861 64493688
Liver disorder 25.99 23.27 24 4159 53327 64441222
Cholangitis 25.69 23.27 13 4170 10789 64483760
Malignant neoplasm progression 25.62 23.27 34 4149 112837 64381712
Myelosuppression 25.34 23.27 17 4166 23813 64470736
Enterocolitis haemorrhagic 25.19 23.27 8 4175 1972 64492577
Disseminated intravascular coagulation 25.00 23.27 19 4164 32329 64462220
Cholangitis acute 24.20 23.27 7 4176 1261 64493288
KL-6 increased 23.75 23.27 4 4179 56 64494493
Erythema multiforme 23.73 23.27 14 4169 15687 64478862

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A02BC08 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Proton pump inhibitors
ATC A02BD14 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Combinations for eradication of Helicobacter pylori
ATC A02BD15 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Combinations for eradication of Helicobacter pylori

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Duodenal ulcer disease indication 51868009 DOID:1724
Gastro-esophageal reflux disease with esophagitis indication 266433003
Gastric ulcer indication 397825006 DOID:10808




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.09 Basic
pKa2 2.72 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
500MG;500MG;EQ 20MG BASE VOQUEZNA TRIPLE PAK PHATHOM N215152 May 3, 2022 RX CAPSULE, TABLET, TABLET ORAL May 3, 2027 NEW CHEMICAL ENTITY
500MG;EQ 20MG BASE VOQUEZNA DUAL PAK PHATHOM N215153 May 3, 2022 RX CAPSULE, TABLET ORAL May 3, 2027 NEW CHEMICAL ENTITY
500MG;500MG;EQ 20MG BASE VOQUEZNA TRIPLE PAK PHATHOM N215152 May 3, 2022 RX CAPSULE, TABLET, TABLET ORAL May 3, 2032 GENERATING ANTIBIOTIC INCENTIVES NOW
500MG;EQ 20MG BASE VOQUEZNA DUAL PAK PHATHOM N215153 May 3, 2022 RX CAPSULE, TABLET ORAL May 3, 2032 GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Potassium-transporting ATPase Transporter INHIBITOR Ki 8 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
1R5L3J156G UNII
D10466 KEGG_DRUG
881681-01-2 SECONDARY_CAS_RN
C4080009 UMLSCUI
CHEBI:136048 CHEBI
HKT PDB_CHEM_ID
CHEMBL2079130 ChEMBL_ID
15981397 PUBCHEM_CID
DB11739 DRUGBANK_ID
CHEMBL2064032 ChEMBL_ID
9535 INN_ID
C552956 MESH_SUPPLEMENTAL_RECORD_UI
11549 IUPHAR_LIGAND_ID

Pharmaceutical products:

None