nabumetone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| cannabinoid receptors agonists | 1863 | 42924-53-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 125.15 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 35 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 24, 1991 | FDA |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 87.03 | 13.20 | 173 | 10507 | 310514 | 63167828 |
| Retinopathy | 35.83 | 13.20 | 15 | 10665 | 3104 | 63475238 |
| Periarticular disorder | 26.21 | 13.20 | 5 | 10675 | 53 | 63478289 |
| Rubella | 25.87 | 13.20 | 6 | 10674 | 171 | 63478171 |
| Off label use | 24.37 | 13.20 | 48 | 10632 | 674414 | 62803928 |
| Depression | 22.99 | 13.20 | 79 | 10601 | 196413 | 63281929 |
| Emotional distress | 20.00 | 13.20 | 26 | 10654 | 32523 | 63445819 |
| Cerebrovascular accident | 19.85 | 13.20 | 51 | 10629 | 107973 | 63370369 |
| Gastrooesophageal reflux disease | 19.52 | 13.20 | 47 | 10633 | 95592 | 63382750 |
| Systemic lupus erythematosus | 18.58 | 13.20 | 6 | 10674 | 208912 | 63269430 |
| Glossodynia | 18.05 | 13.20 | 4 | 10676 | 178872 | 63299470 |
| Alopecia | 17.05 | 13.20 | 19 | 10661 | 337517 | 63140825 |
| Anxiety | 16.21 | 13.20 | 76 | 10604 | 217465 | 63260877 |
| Wound | 15.78 | 13.20 | 4 | 10676 | 163259 | 63315083 |
| Drug intolerance | 14.91 | 13.20 | 18 | 10662 | 308643 | 63169699 |
| Hepatic enzyme increased | 14.48 | 13.20 | 8 | 10672 | 202320 | 63276022 |
| Injection site pain | 14.14 | 13.20 | 51 | 10629 | 129749 | 63348593 |
| Psoriasis | 13.90 | 13.20 | 39 | 10641 | 86918 | 63391424 |
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 |
|---|---|---|---|---|---|---|
| Splenic embolism | 50.53 | 17.75 | 10 | 4134 | 189 | 34952598 |
| Sideroblastic anaemia | 47.90 | 17.75 | 10 | 4134 | 249 | 34952538 |
| Vitamin B1 decreased | 45.25 | 17.75 | 10 | 4134 | 328 | 34952459 |
| Diaphragmatic injury | 41.68 | 17.75 | 8 | 4136 | 128 | 34952659 |
| Coronary artery disease | 34.19 | 17.75 | 35 | 4109 | 48270 | 34904517 |
| Implant site infection | 33.63 | 17.75 | 10 | 4134 | 1080 | 34951707 |
| Marrow hyperplasia | 32.99 | 17.75 | 10 | 4134 | 1153 | 34951634 |
| Autoimmune haemolytic anaemia | 32.31 | 17.75 | 14 | 4130 | 4482 | 34948305 |
| Granuloma | 29.66 | 17.75 | 12 | 4132 | 3239 | 34949548 |
| Granulomatous liver disease | 29.64 | 17.75 | 8 | 4136 | 609 | 34952178 |
| Pain | 27.62 | 17.75 | 69 | 4075 | 204606 | 34748181 |
| Mycobacterial infection | 26.00 | 17.75 | 10 | 4134 | 2364 | 34950423 |
| Psoriatic arthropathy | 25.24 | 17.75 | 20 | 4124 | 19778 | 34933009 |
| Renal atrophy | 24.49 | 17.75 | 8 | 4136 | 1177 | 34951610 |
| Pulmonary granuloma | 22.48 | 17.75 | 8 | 4136 | 1522 | 34951265 |
| Intervertebral disc degeneration | 21.88 | 17.75 | 12 | 4132 | 6405 | 34946382 |
| Drug abuser | 21.08 | 17.75 | 10 | 4134 | 3944 | 34948843 |
| Upper gastrointestinal haemorrhage | 20.84 | 17.75 | 20 | 4124 | 25498 | 34927289 |
| Ankylosing spondylitis | 20.55 | 17.75 | 11 | 4133 | 5593 | 34947194 |
| Psoriasis | 20.29 | 17.75 | 24 | 4120 | 38788 | 34913999 |
| Splenic infarction | 20.11 | 17.75 | 8 | 4136 | 2067 | 34950720 |
| Generalised oedema | 19.03 | 17.75 | 14 | 4130 | 12394 | 34940393 |
| Injury | 18.39 | 17.75 | 17 | 4127 | 20670 | 34932117 |
| Pulseless electrical activity | 17.97 | 17.75 | 11 | 4133 | 7200 | 34945587 |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 94.08 | 13.68 | 159 | 11161 | 298757 | 79434311 |
| Splenic embolism | 48.10 | 13.68 | 10 | 11310 | 202 | 79732866 |
| Sideroblastic anaemia | 45.29 | 13.68 | 10 | 11310 | 271 | 79732797 |
| Coronary artery disease | 45.20 | 13.68 | 51 | 11269 | 65423 | 79667645 |
| Diaphragmatic injury | 40.24 | 13.68 | 8 | 11312 | 128 | 79732940 |
| Retinopathy | 38.42 | 13.68 | 16 | 11304 | 3875 | 79729193 |
| Vitamin B1 decreased | 38.38 | 13.68 | 10 | 11310 | 553 | 79732515 |
| Depression | 35.38 | 13.68 | 88 | 11232 | 216702 | 79516366 |
| Off label use | 33.70 | 13.68 | 48 | 11272 | 907167 | 78825901 |
| Marrow hyperplasia | 27.79 | 13.68 | 10 | 11310 | 1638 | 79731430 |
| Emotional distress | 27.34 | 13.68 | 31 | 11289 | 39938 | 79693130 |
| Rubella | 27.26 | 13.68 | 6 | 11314 | 160 | 79732908 |
| Implant site infection | 26.59 | 13.68 | 10 | 11310 | 1855 | 79731213 |
| Drug abuser | 26.03 | 13.68 | 14 | 11306 | 5999 | 79727069 |
| Anxiety | 24.26 | 13.68 | 84 | 11236 | 248428 | 79484640 |
| Autoimmune haemolytic anaemia | 24.22 | 13.68 | 15 | 11305 | 8365 | 79724703 |
| Granulomatous liver disease | 22.15 | 13.68 | 8 | 11312 | 1325 | 79731743 |
| Pain | 22.13 | 13.68 | 173 | 11147 | 703629 | 79029439 |
| Myocardial infarction | 21.34 | 13.68 | 66 | 11254 | 184063 | 79549005 |
| Cerebrovascular accident | 21.19 | 13.68 | 59 | 11261 | 155233 | 79577835 |
| Febrile neutropenia | 20.41 | 13.68 | 4 | 11316 | 230995 | 79502073 |
| Mycobacterial infection | 20.08 | 13.68 | 10 | 11310 | 3658 | 79729410 |
| Renal atrophy | 19.70 | 13.68 | 8 | 11312 | 1817 | 79731251 |
| Drug withdrawal syndrome | 18.94 | 13.68 | 24 | 11296 | 34694 | 79698374 |
| Injury | 18.91 | 13.68 | 37 | 11283 | 77459 | 79655609 |
| Gastrooesophageal reflux disease | 18.78 | 13.68 | 44 | 11276 | 104202 | 79628866 |
| Pulmonary granuloma | 18.54 | 13.68 | 8 | 11312 | 2113 | 79730955 |
| Psoriasis | 17.45 | 13.68 | 39 | 11281 | 89548 | 79643520 |
| Drug dependence | 17.38 | 13.68 | 25 | 11295 | 40744 | 79692324 |
| Granuloma | 17.04 | 13.68 | 12 | 11308 | 8285 | 79724783 |
| Neutropenia | 16.81 | 13.68 | 10 | 11310 | 287700 | 79445368 |
| Intervertebral disc degeneration | 15.77 | 13.68 | 15 | 11305 | 15770 | 79717298 |
| General physical health deterioration | 15.48 | 13.68 | 10 | 11310 | 275228 | 79457840 |
| Injection site pain | 14.54 | 13.68 | 46 | 11274 | 129792 | 79603276 |
| Meniscus injury | 14.39 | 13.68 | 10 | 11310 | 6758 | 79726310 |
| Splenic infarction | 14.39 | 13.68 | 8 | 11312 | 3656 | 79729412 |
| Spinal stenosis | 13.89 | 13.68 | 14 | 11306 | 15777 | 79717291 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M01AX01 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Other antiinflammatory and antirheumatic agents, non-steroids |
| FDA CS | M0001335 | Anti-Inflammatory Agents, Non-Steroidal |
| FDA MoA | N0000000160 | Cyclooxygenase Inhibitors |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D052246 | Cyclooxygenase 2 Inhibitors |
| MeSH PA | D016861 | Cyclooxygenase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory agent |
| CHEBI has role | CHEBI:50266 | Prodrugs |
| CHEBI has role | CHEBI:50629 | COX-2 inhibitor |
| FDA EPC | N0000175722 | Nonsteroidal Anti-inflammatory Drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Rheumatoid arthritis | indication | 69896004 | DOID:7148 |
| Osteoarthritis | indication | 396275006 | |
| Ankylosing spondylitis | off-label use | 9631008 | DOID:7147 |
| Juvenile rheumatoid arthritis | off-label use | 410795001 | |
| Alcoholism | contraindication | 7200002 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Acute gastric ulcer with perforation | contraindication | 19850005 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Acute nephropathy | contraindication | 58574008 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Coronary artery bypass graft | contraindication | 232717009 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Pregnancy, function | contraindication | 289908002 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Smokes tobacco daily | contraindication | 449868002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 3.34 | WOMBAT-PK | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.73 | DRUG MATRIX | |||||
| Cytochrome P450 1A2 | Enzyme | IC50 | 5.30 | DRUG MATRIX | |||||
| Amine oxidase [flavin-containing] A | Enzyme | IC50 | 6.00 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| 4020284 | VUID |
| N0000148161 | NUI |
| D00425 | KEGG_DRUG |
| 4020284 | VANDF |
| C0068334 | UMLSCUI |
| CHEBI:76252 | CHEBI |
| NBO | PDB_CHEM_ID |
| CHEMBL1070 | ChEMBL_ID |
| DB00461 | DRUGBANK_ID |
| D000077430 | MESH_DESCRIPTOR_UI |
| 4409 | PUBCHEM_CID |
| 7245 | IUPHAR_LIGAND_ID |
| 4855 | INN_ID |
| LW0TIW155Z | UNII |
| 31448 | RXNORM |
| 41877 | MMSL |
| 5142 | MMSL |
| d00310 | MMSL |
| 003622 | NDDF |
| 108508000 | SNOMEDCT_US |
| 386859000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-1657 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 28 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-1658 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 28 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0185-0145 | TABLET | 500 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0185-0146 | TABLET | 750 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-5843 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-5844 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3670 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3670 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3671 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 26 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3671 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 26 sections |
| Nabumetone 500 mg | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0722-7076 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 28 sections |
| Nabumetone 750 mg | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0722-7077 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 28 sections |
| Nabumetone 1000 mg | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0722-7078 | TABLET, FILM COATED | 1000 mg | ORAL | ANDA | 28 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-003 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-120 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 28 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-271 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-273 | TABLET | 500 mg | ORAL | ANDA | 25 sections |
| RELAFEN DS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 15370-170 | TABLET | 1000 mg | ORAL | ANDA | 30 sections |
| RELAFEN DS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 15370-170 | TABLET | 1000 mg | ORAL | ANDA | 30 sections |
| NABUMETONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-160 | TABLET | 750 mg | ORAL | ANDA | 25 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-230 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-231 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-077 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 28 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-078 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33358-251 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33358-252 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 35356-687 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 28 sections |
| NABUMETONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42549-523 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 23 sections |
| NABUMETONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42549-648 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 29 sections |
| Nabumetone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-859 | TABLET, FILM COATED | 750 mg | ORAL | ANDA | 28 sections |