loxoprofen Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
anti-inflammatory agents, ibuprofen derivatives 1615 68767-14-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • loxoprofen sodium hydrate
  • loxonin
  • loxoprofen
  • loxoprofen sodium
  • sodium loxoprofen
  • Molecular weight: 246.31
  • Formula: C15H18O3
  • CLOGP: 1.97
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 54.37
  • ALOGS: -3.57
  • ROTB: 4

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 23, 2006 PMDA Lead Chemical Co., Ltd.

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
Acute kidney injury 199.24 48.09 64 615 28058 2329348
Hepatic function abnormal 191.92 48.09 45 634 6047 2351359
Stevens-Johnson syndrome 142.01 48.09 33 646 4226 2353180
Platelet count decreased 132.20 48.09 41 638 15772 2341634
Pyrexia 131.35 48.09 56 623 53652 2303754
Renal impairment 113.76 48.09 33 646 10059 2347347
Gastric ulcer haemorrhage 108.26 48.09 20 659 820 2356586
Blood creatinine increased 107.97 48.09 32 647 10501 2346905
Aspartate aminotransferase increased 102.28 48.09 32 647 12580 2344826
Blood urea increased 89.27 48.09 22 657 3583 2353823
Anaemia 86.99 48.09 37 642 34755 2322651
Alanine aminotransferase increased 86.78 48.09 29 650 14003 2343403
Drug eruption 86.33 48.09 21 658 3238 2354168
Vomiting 83.47 48.09 45 634 71557 2285849
Interstitial lung disease 81.10 48.09 24 655 7788 2349618
Nausea 79.44 48.09 51 628 112138 2245268
Liver disorder 76.70 48.09 22 657 6392 2351014
Decreased appetite 73.02 48.09 31 648 28860 2328546
Malaise 67.58 48.09 36 643 55549 2301857
Melaena 67.08 48.09 18 661 4088 2353318
Blood lactate dehydrogenase increased 65.14 48.09 17 662 3467 2353939
Altered state of consciousness 63.42 48.09 17 662 3843 2353563
Blood pressure decreased 52.68 48.09 18 661 9218 2348188
Depressed level of consciousness 52.03 48.09 17 662 7587 2349819
Disseminated intravascular coagulation 51.47 48.09 14 665 3336 2354070
Dizziness 49.57 48.09 30 649 58635 2298771
Gamma-glutamyltransferase increased 48.66 48.09 15 664 5547 2351859
Gastric ulcer 48.18 48.09 13 666 3003 2354403

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
Pyrexia 142.02 48.09 63 532 46337 1699849
Interstitial lung disease 141.54 48.09 42 553 9654 1736532
Hepatic function abnormal 122.34 48.09 35 560 7039 1739147
Acute kidney injury 118.01 48.09 51 544 34893 1711293
Gastric ulcer 102.85 48.09 25 570 2660 1743526
Liver disorder 93.33 48.09 27 568 5609 1740577
Gastric ulcer haemorrhage 91.58 48.09 19 576 980 1745206
Platelet count decreased 75.23 48.09 30 565 16493 1729693
Renal impairment 72.60 48.09 27 568 12287 1733899
Melaena 64.64 48.09 20 575 5190 1740996
Stevens-Johnson syndrome 59.55 48.09 17 578 3340 1742846
Blood creatinine increased 58.82 48.09 24 571 13922 1732264
Decreased appetite 58.40 48.09 28 567 23843 1722343
Peritonitis 58.30 48.09 16 579 2723 1743463
Drug eruption 57.25 48.09 16 579 2910 1743276
Rash 56.29 48.09 32 563 38661 1707525
Renal disorder 56.25 48.09 17 578 4069 1742117
Blood lactate dehydrogenase increased 53.65 48.09 16 579 3659 1742527
Alanine aminotransferase increased 51.29 48.09 21 574 12257 1733929
Haemoglobin decreased 50.87 48.09 23 572 17091 1729095
Aspartate aminotransferase increased 50.45 48.09 20 575 10736 1735450
Anaemia 49.99 48.09 27 568 29430 1716756
Blood urea increased 49.73 48.09 16 579 4695 1741491
Gastrointestinal haemorrhage 48.25 48.09 21 574 14246 1731940
Blood alkaline phosphatase increased 48.20 48.09 16 579 5179 1741007

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
CHEBI has role CHEBI:35481 non-narcotic analgesic
CHEBI has role CHEBI:35493 antipyretic
CHEBI has role CHEBI:50266 prodrug
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Rheumatoid arthritis indication 69896004 DOID:7148

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.37 acidic

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 1 Enzyme INHIBITOR IC50 5.19 CHEMBL KEGG DRUG
Prostaglandin G/H synthase 2 Enzyme INHIBITOR IC50 5 CHEMBL KEGG DRUG

External reference:

IDSource
C0065199 UMLSCUI
D08149 KEGG_DRUG
3583H0GZAP UNII
5410 INN_ID
18991000122102 SNOMEDCT_US
28908 RXNORM
008162 NDDF
3965 PUBCHEM_CID
CHEBI:76172 CHEBI
CHEMBL19299 ChEMBL_ID
CHEMBL66552 ChEMBL_ID
80382-23-6 SECONDARY_CAS_RN
DB09212 DRUGBANK_ID
C040656 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None