tenoxicam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
anti-inflammatory, isoxicam derivatives 2595 59804-37-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tenoxicam
  • mobiflex
  • Molecular weight: 337.37
  • Formula: C13H11N3O4S2
  • CLOGP: 1.61
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 99.60
  • ALOGS: -3.12
  • ROTB: 2

Drug dosage:

DoseUnitRoute
20 mg O
20 mg P
20 mg R

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.80 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.10 % Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.19 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.03 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 67 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.591 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 13.032 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 24.717 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.276 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 5.100 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 4.880 % High 1
herg hERG pIC50 4.149 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 2.985 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.639 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.560 % High 1
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,KIT,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK7,MAPK9,MARK4,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 49
kinase-selectivity-class ACVR2A,ACVR2B,AURKB,AURKC,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,ERBB2,GRK2,IRAK1,MAP2K3,MAP2K6,MAPK12,MAPK7,MARK4,PRKDC,SIK2,STK10,STK33,SYK,TEK,TTK 25
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 7.816 High 1
mh-clint Mouse hepatocyte intrinsic clearance 6.383 High 1
mppb Mouse plasma protein binding (% unbound) 4.150 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.099 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 Moderate 0.70
pppb Pig plasma protein binding (% unbound) 3.660 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.285 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 93.220 % High 1
rppb Rat plasma protein binding (% unbound) 0.720 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 961.612 uM High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1987 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

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
Sebaceous gland disorder 57.27 54.69 6 233 68 110588992

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M01AC02 MUSCULO-SKELETAL SYSTEM
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS
Oxicams
MeSH PA D000700 Analgesics
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D016861 Cyclooxygenase Inhibitors
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018712 Analgesics, Non-Narcotic
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35481 non-narcotic analgesic
CHEBI has role CHEBI:35493 antipyretic
CHEBI has role CHEBI:35544 EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor

Related Drugs by ATC class:

M01AC Oxicams 4 drugs

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

DiseaseRelationSNOMED_IDDOID
Arthritis indication 3723001 DOID:848




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.25 acidic
pKa2 8.43 acidic
pKa3 5.18 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Prostaglandin G/H synthase 2 Enzyme WOMBAT-PK
Prostaglandin G/H synthase 1 Enzyme IC50 5.94 DRUG MATRIX

External reference:

IDSource
D01767 KEGG_DRUG
C0076096 UMLSCUI
CHEBI:32192 CHEBI
CHEMBL302795 ChEMBL_ID
DB00469 DRUGBANK_ID
C032801 MESH_SUPPLEMENTAL_RECORD_UI
54677971 PUBCHEM_CID
4915 INN_ID
Z1R9N0A399 UNII
196497 RXNORM
003632 NDDF
329913008 SNOMEDCT_US
395898001 SNOMEDCT_US

Pharmaceutical products:

None