Mofebutazone is a non-steroidal anti-inflammatory drug (NSAID) that was first synthesized in the 1950s. It is a derivative of phenylbutazone and shares a similar mechanism of action. Mofebutazone inhibits the production of prostaglandins, which are involved in pain and inflammation. It was once widely used to treat various inflammatory conditions, including rheumatoid arthritis, osteoarthritis, and gout. However, due to concerns about its potential for serious adverse effects, such as gastrointestinal bleeding, liver damage, and bone marrow suppression, its use has declined significantly. Mofebutazone remains an important subject of research, particularly in the context of veterinary medicine, where it continues to be used to treat inflammatory conditions in animals. Further research aims to understand its potential for safer and more targeted applications, perhaps in combination with other drugs or in different delivery methods. Mofebutazone's importance lies in its historical significance as a pioneering NSAID and its continued use in veterinary medicine, while its study focuses on exploring safer and more effective applications.'
mofebutazone: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
mofebutazone : A pyrazolidine that is phenylbutazone lacking one of the phenyl substituents. It is used for treatment of joint and muscular pain. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 16639 |
| CHEMBL ID | 1892201 |
| CHEBI ID | 76252 |
| SCHEMBL ID | 23506 |
| MeSH ID | M0042918 |
| Synonym |
|---|
| butazone |
| 4-butyl-1-phenylpyrazolidine-3,5-dione |
| mofebutazonum [inn-latin] |
| brn 0213056 |
| nsc 73725 |
| mofebutazona [inn-spanish] |
| einecs 218-641-1 |
| 2 fdbp |
| 3,5-pyrazolidinedione, 4-butyl-1-phenyl- |
| 2-phenyl-3,5-dihydroxy-4-butylpyrazolidine |
| mofebutazone (inn) |
| monazone (tn) |
| D07262 |
| mofebutazone |
| 2210-63-1 |
| mls002693879 , |
| corbuton |
| nsc-73725 |
| mobuzon |
| monozon |
| arcomonol tablets |
| mobutazon |
| reumatox |
| 4-butyl-1-phenyl-3,5-dioxopyrazolidine |
| 4-butyl-1-phenyl-3,5-pyrazolidinedione |
| mobutazone |
| monorheumetten |
| monobutyl |
| nsc73725 |
| arcobutine |
| mozol |
| monophenylbutazone |
| 3, 4-butyl-1-phenyl- |
| monofen |
| mophebutazone |
| monomil |
| monazan |
| smr001559820 |
| HMS3094E11 |
| spw36wui5z , |
| mofebutazonum |
| unii-spw36wui5z |
| mofebutazone [inn:dcf] |
| mofebutazona |
| CHEMBL1892201 |
| chebi:76252 , |
| monazone |
| AKOS015962258 |
| mofebutazone [mi] |
| mofebutazone [mart.] |
| mofebutazone [inn] |
| mofebutazone [who-dd] |
| SCHEMBL23506 |
| 1-phenyl-4-butyl-3,5-pyrazolidinedione |
| mofesal |
| monazon |
| 4-butyl-3,5-diketo-1-phenylpyrazolidine |
| REOJLIXKJWXUGB-UHFFFAOYSA-N |
| W-107503 |
| monophenyl butazone |
| DTXSID4023331 |
| mofebutazon |
| DB13629 |
| Q6890329 |
| AS-56394 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The difference between mofebutazone and phenylbutazone is shown by means of toxicological, pharmacological and pharmacokinetic studies as well as by the protein binding." | ( [Pharmacology, toxicology and pharmacokinetics of mofebutazone]. Graul, EH; Knoell, HE; Loew, D; Schuster, O, ) | 0.7 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The almost complete recovery of mofebutazone in the urine indicates that after oral administration, this drug has a very high bioavailability via the oral route." | ( Pharmacokinetics of [4-14C] mofebutazone after oral administration in man. Kassem, MA; Schulte, KE, ) | 0.71 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " On the basis of this study we regard it once again as essential that the kinetics in the synovial fluid should without doubt be preferred to the kinetics in the plasma for the calculation of a dosage schedule for non-steroidal antiphlogistics." | ( [Kinetics of mofebutazone in plasma and synovial fluid]. Barkow, D; Deister, J; Kamp, J; Knoell, HE; Loew, D; Schuster, O, ) | 0.5 |
| Role | Description |
|---|---|
| non-steroidal anti-inflammatory drug | An anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. |
| non-narcotic analgesic | A drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| pyrazolidines | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 1.7783 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 7.0795 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
| IDH1 | Homo sapiens (human) | Potency | 1.8356 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| Vpr | Human immunodeficiency virus 1 | Potency | 3.9811 | 1.5849 | 19.6264 | 63.0957 | AID651644 |
| Glycoprotein hormones alpha chain | Homo sapiens (human) | Potency | 5.6234 | 4.4668 | 8.3448 | 10.0000 | AID624291 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 12.5893 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 11 (47.83) | 18.7374 |
| 1990's | 8 (34.78) | 18.2507 |
| 2000's | 1 (4.35) | 29.6817 |
| 2010's | 2 (8.70) | 24.3611 |
| 2020's | 1 (4.35) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (3.33%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 1 (3.33%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 28 (93.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||