Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib
Robenacoxib is a veterinary‐approved non‐steroidal anti‐inflammatory drug (NSAID) of the coxib group. It possesses anti‐hyperalgesic, anti‐inflammatory and anti‐pyretic properties. Robenacoxib inhibits the cyclooxygenase (COX)‐2 isoform of COX selectively (in vitro IC50 ratios COX‐1:COX‐2, 129:1 in...
Gespeichert in:
| Veröffentlicht in: | Journal of veterinary pharmacology and therapeutics 2022-07, Vol.45 (4), p.325-351 |
|---|---|
| Hauptverfasser: | , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 351 |
|---|---|
| container_issue | 4 |
| container_start_page | 325 |
| container_title | Journal of veterinary pharmacology and therapeutics |
| container_volume | 45 |
| creator | Lees, Peter Toutain, Pierre‐Louis Elliott, Jonathan Giraudel, Jerome M. Pelligand, Ludovic King, Jonathan N. |
| description | Robenacoxib is a veterinary‐approved non‐steroidal anti‐inflammatory drug (NSAID) of the coxib group. It possesses anti‐hyperalgesic, anti‐inflammatory and anti‐pyretic properties. Robenacoxib inhibits the cyclooxygenase (COX)‐2 isoform of COX selectively (in vitro IC50 ratios COX‐1:COX‐2, 129:1 in dogs, 32:1 in cats). At registered dosages (2 mg/kg subcutaneously in dogs and cats, 1–4 mg/kg orally in dogs and 1–2.4 mg/kg orally in cats), robenacoxib produces significant inhibition of COX‐2 whilst sparing COX‐1. The pharmacokinetic (PK) profile of robenacoxib is characterized by a high degree of binding to plasma proteins (>98%) and moderate volume of distribution (at steady state, 240 ml/kg in dogs and 190 ml/kg in cats). In consequence, the terminal half‐life in blood ( |
| doi_str_mv | 10.1111/jvp.13052 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_hal_p</sourceid><recordid>TN_cdi_hal_primary_oai_HAL_hal_03672721v1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2654297951</sourcerecordid><originalsourceid>FETCH-LOGICAL-c3942-38aaf6b53ac02e5bee6f611040907019494bfb771314180474c9f426c9cd50cb3</originalsourceid><addsrcrecordid>eNp1kM1OGzEQgC0EImnaAy9Q-Ugllsz4Z717RFELRZHgAFVvlu3YxGizTtcJbW59hD4jT8LSBDgxl9GMPn2Hj5AjhFPsZ3z_sDxFDpLtkSHyUhasquQ-GQIKKJSq-IB8yPkeAHiFeEgGXIoSoOJDcns9N93CuNSku80JzSb4Vb99CNEZt6GmnVHXxLa_GrrOPtMU6Gru6eTq5-Pff4zGdh5tXKWOdsn6tjf9ifYjOQimyf7Tbo_I7bevN5OLYnp1_n1yNi0crwUreGVMKK3kxgHz0npfhhIRBNSgAGtRCxusUshRYAVCCVcHwUpXu5kEZ_mIfNl656bRyy4uTLfRyUR9cTbVzz_gpWKK4QP27PGWXXbp19rnlV7E7HzTmNanddaslILVqpb4pnVdyrnz4dWNoJ-L6764_l-8Zz_vtGu78LNX8iVxD4y3wO_Y-M37Jn3543qrfAJcJ4jz</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2654297951</pqid></control><display><type>article</type><title>Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib</title><source>Wiley Online Library Journals Frontfile Complete</source><creator>Lees, Peter ; Toutain, Pierre‐Louis ; Elliott, Jonathan ; Giraudel, Jerome M. ; Pelligand, Ludovic ; King, Jonathan N.</creator><creatorcontrib>Lees, Peter ; Toutain, Pierre‐Louis ; Elliott, Jonathan ; Giraudel, Jerome M. ; Pelligand, Ludovic ; King, Jonathan N.</creatorcontrib><description>Robenacoxib is a veterinary‐approved non‐steroidal anti‐inflammatory drug (NSAID) of the coxib group. It possesses anti‐hyperalgesic, anti‐inflammatory and anti‐pyretic properties. Robenacoxib inhibits the cyclooxygenase (COX)‐2 isoform of COX selectively (in vitro IC50 ratios COX‐1:COX‐2, 129:1 in dogs, 32:1 in cats). At registered dosages (2 mg/kg subcutaneously in dogs and cats, 1–4 mg/kg orally in dogs and 1–2.4 mg/kg orally in cats), robenacoxib produces significant inhibition of COX‐2 whilst sparing COX‐1. The pharmacokinetic (PK) profile of robenacoxib is characterized by a high degree of binding to plasma proteins (>98%) and moderate volume of distribution (at steady state, 240 ml/kg in dogs and 190 ml/kg in cats). In consequence, the terminal half‐life in blood (<2 h) is short, despite moderate body clearance (0.81 L/kg/h) in dogs and low clearance (0.44 L/kg/h) in cats. Excretion is principally in the bile (65% in dogs and 72% in cats). Robenacoxib concentrates in inflamed tissues, and clinical efficacy is achieved with once‐daily dosing, despite the short blood terminal half‐life. In dogs, no relevant breed differences in robenacoxib PK have been detected. Robenacoxib has a wide safety margin; in healthy laboratory animals daily oral doses 20‐fold (dog, 1 month), eight‐fold (cat, 6 weeks) and five‐fold (dog, 6 months) higher than recommended clinical doses were well tolerated. Clinical efficacy and safety have been demonstrated in orthopaedic and soft tissue surgery, and in musculoskeletal disorders in dogs and cats.</description><identifier>ISSN: 0140-7783</identifier><identifier>EISSN: 1365-2885</identifier><identifier>DOI: 10.1111/jvp.13052</identifier><identifier>PMID: 35460083</identifier><language>eng</language><publisher>England: Wiley-Blackwell</publisher><subject>cat ; coxib ; dog ; Life Sciences ; NSAID ; Pharmaceutical sciences ; Pharmacology ; robenacoxib</subject><ispartof>Journal of veterinary pharmacology and therapeutics, 2022-07, Vol.45 (4), p.325-351</ispartof><rights>2022 The Authors. published by John Wiley & Sons Ltd.</rights><rights>2022 The Authors. Journal of Veterinary Pharmacology and Therapeutics published by John Wiley & Sons Ltd.</rights><rights>Attribution</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3942-38aaf6b53ac02e5bee6f611040907019494bfb771314180474c9f426c9cd50cb3</citedby><cites>FETCH-LOGICAL-c3942-38aaf6b53ac02e5bee6f611040907019494bfb771314180474c9f426c9cd50cb3</cites><orcidid>0000-0002-4194-9015 ; 0000-0002-8846-8892 ; 0000-0002-4517-6590 ; 0000-0001-6005-1975 ; 0000-0002-8966-3737</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fjvp.13052$$EPDF$$P50$$Gwiley$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fjvp.13052$$EHTML$$P50$$Gwiley$$Hfree_for_read</linktohtml><link.rule.ids>230,314,776,780,881,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/35460083$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://hal.inrae.fr/hal-03672721$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Lees, Peter</creatorcontrib><creatorcontrib>Toutain, Pierre‐Louis</creatorcontrib><creatorcontrib>Elliott, Jonathan</creatorcontrib><creatorcontrib>Giraudel, Jerome M.</creatorcontrib><creatorcontrib>Pelligand, Ludovic</creatorcontrib><creatorcontrib>King, Jonathan N.</creatorcontrib><title>Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib</title><title>Journal of veterinary pharmacology and therapeutics</title><addtitle>J Vet Pharmacol Ther</addtitle><description>Robenacoxib is a veterinary‐approved non‐steroidal anti‐inflammatory drug (NSAID) of the coxib group. It possesses anti‐hyperalgesic, anti‐inflammatory and anti‐pyretic properties. Robenacoxib inhibits the cyclooxygenase (COX)‐2 isoform of COX selectively (in vitro IC50 ratios COX‐1:COX‐2, 129:1 in dogs, 32:1 in cats). At registered dosages (2 mg/kg subcutaneously in dogs and cats, 1–4 mg/kg orally in dogs and 1–2.4 mg/kg orally in cats), robenacoxib produces significant inhibition of COX‐2 whilst sparing COX‐1. The pharmacokinetic (PK) profile of robenacoxib is characterized by a high degree of binding to plasma proteins (>98%) and moderate volume of distribution (at steady state, 240 ml/kg in dogs and 190 ml/kg in cats). In consequence, the terminal half‐life in blood (<2 h) is short, despite moderate body clearance (0.81 L/kg/h) in dogs and low clearance (0.44 L/kg/h) in cats. Excretion is principally in the bile (65% in dogs and 72% in cats). Robenacoxib concentrates in inflamed tissues, and clinical efficacy is achieved with once‐daily dosing, despite the short blood terminal half‐life. In dogs, no relevant breed differences in robenacoxib PK have been detected. Robenacoxib has a wide safety margin; in healthy laboratory animals daily oral doses 20‐fold (dog, 1 month), eight‐fold (cat, 6 weeks) and five‐fold (dog, 6 months) higher than recommended clinical doses were well tolerated. Clinical efficacy and safety have been demonstrated in orthopaedic and soft tissue surgery, and in musculoskeletal disorders in dogs and cats.</description><subject>cat</subject><subject>coxib</subject><subject>dog</subject><subject>Life Sciences</subject><subject>NSAID</subject><subject>Pharmaceutical sciences</subject><subject>Pharmacology</subject><subject>robenacoxib</subject><issn>0140-7783</issn><issn>1365-2885</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><sourceid>24P</sourceid><recordid>eNp1kM1OGzEQgC0EImnaAy9Q-Ugllsz4Z717RFELRZHgAFVvlu3YxGizTtcJbW59hD4jT8LSBDgxl9GMPn2Hj5AjhFPsZ3z_sDxFDpLtkSHyUhasquQ-GQIKKJSq-IB8yPkeAHiFeEgGXIoSoOJDcns9N93CuNSku80JzSb4Vb99CNEZt6GmnVHXxLa_GrrOPtMU6Gru6eTq5-Pff4zGdh5tXKWOdsn6tjf9ifYjOQimyf7Tbo_I7bevN5OLYnp1_n1yNi0crwUreGVMKK3kxgHz0npfhhIRBNSgAGtRCxusUshRYAVCCVcHwUpXu5kEZ_mIfNl656bRyy4uTLfRyUR9cTbVzz_gpWKK4QP27PGWXXbp19rnlV7E7HzTmNanddaslILVqpb4pnVdyrnz4dWNoJ-L6764_l-8Zz_vtGu78LNX8iVxD4y3wO_Y-M37Jn3543qrfAJcJ4jz</recordid><startdate>202207</startdate><enddate>202207</enddate><creator>Lees, Peter</creator><creator>Toutain, Pierre‐Louis</creator><creator>Elliott, Jonathan</creator><creator>Giraudel, Jerome M.</creator><creator>Pelligand, Ludovic</creator><creator>King, Jonathan N.</creator><general>Wiley-Blackwell</general><scope>24P</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>1XC</scope><orcidid>https://orcid.org/0000-0002-4194-9015</orcidid><orcidid>https://orcid.org/0000-0002-8846-8892</orcidid><orcidid>https://orcid.org/0000-0002-4517-6590</orcidid><orcidid>https://orcid.org/0000-0001-6005-1975</orcidid><orcidid>https://orcid.org/0000-0002-8966-3737</orcidid></search><sort><creationdate>202207</creationdate><title>Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib</title><author>Lees, Peter ; Toutain, Pierre‐Louis ; Elliott, Jonathan ; Giraudel, Jerome M. ; Pelligand, Ludovic ; King, Jonathan N.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3942-38aaf6b53ac02e5bee6f611040907019494bfb771314180474c9f426c9cd50cb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>cat</topic><topic>coxib</topic><topic>dog</topic><topic>Life Sciences</topic><topic>NSAID</topic><topic>Pharmaceutical sciences</topic><topic>Pharmacology</topic><topic>robenacoxib</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lees, Peter</creatorcontrib><creatorcontrib>Toutain, Pierre‐Louis</creatorcontrib><creatorcontrib>Elliott, Jonathan</creatorcontrib><creatorcontrib>Giraudel, Jerome M.</creatorcontrib><creatorcontrib>Pelligand, Ludovic</creatorcontrib><creatorcontrib>King, Jonathan N.</creatorcontrib><collection>Wiley Online Library Open Access</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><jtitle>Journal of veterinary pharmacology and therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lees, Peter</au><au>Toutain, Pierre‐Louis</au><au>Elliott, Jonathan</au><au>Giraudel, Jerome M.</au><au>Pelligand, Ludovic</au><au>King, Jonathan N.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib</atitle><jtitle>Journal of veterinary pharmacology and therapeutics</jtitle><addtitle>J Vet Pharmacol Ther</addtitle><date>2022-07</date><risdate>2022</risdate><volume>45</volume><issue>4</issue><spage>325</spage><epage>351</epage><pages>325-351</pages><issn>0140-7783</issn><eissn>1365-2885</eissn><abstract>Robenacoxib is a veterinary‐approved non‐steroidal anti‐inflammatory drug (NSAID) of the coxib group. It possesses anti‐hyperalgesic, anti‐inflammatory and anti‐pyretic properties. Robenacoxib inhibits the cyclooxygenase (COX)‐2 isoform of COX selectively (in vitro IC50 ratios COX‐1:COX‐2, 129:1 in dogs, 32:1 in cats). At registered dosages (2 mg/kg subcutaneously in dogs and cats, 1–4 mg/kg orally in dogs and 1–2.4 mg/kg orally in cats), robenacoxib produces significant inhibition of COX‐2 whilst sparing COX‐1. The pharmacokinetic (PK) profile of robenacoxib is characterized by a high degree of binding to plasma proteins (>98%) and moderate volume of distribution (at steady state, 240 ml/kg in dogs and 190 ml/kg in cats). In consequence, the terminal half‐life in blood (<2 h) is short, despite moderate body clearance (0.81 L/kg/h) in dogs and low clearance (0.44 L/kg/h) in cats. Excretion is principally in the bile (65% in dogs and 72% in cats). Robenacoxib concentrates in inflamed tissues, and clinical efficacy is achieved with once‐daily dosing, despite the short blood terminal half‐life. In dogs, no relevant breed differences in robenacoxib PK have been detected. Robenacoxib has a wide safety margin; in healthy laboratory animals daily oral doses 20‐fold (dog, 1 month), eight‐fold (cat, 6 weeks) and five‐fold (dog, 6 months) higher than recommended clinical doses were well tolerated. Clinical efficacy and safety have been demonstrated in orthopaedic and soft tissue surgery, and in musculoskeletal disorders in dogs and cats.</abstract><cop>England</cop><pub>Wiley-Blackwell</pub><pmid>35460083</pmid><doi>10.1111/jvp.13052</doi><tpages>27</tpages><orcidid>https://orcid.org/0000-0002-4194-9015</orcidid><orcidid>https://orcid.org/0000-0002-8846-8892</orcidid><orcidid>https://orcid.org/0000-0002-4517-6590</orcidid><orcidid>https://orcid.org/0000-0001-6005-1975</orcidid><orcidid>https://orcid.org/0000-0002-8966-3737</orcidid><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0140-7783 |
| ispartof | Journal of veterinary pharmacology and therapeutics, 2022-07, Vol.45 (4), p.325-351 |
| issn | 0140-7783 1365-2885 |
| language | eng |
| recordid | cdi_hal_primary_oai_HAL_hal_03672721v1 |
| source | Wiley Online Library Journals Frontfile Complete |
| subjects | cat coxib dog Life Sciences NSAID Pharmaceutical sciences Pharmacology robenacoxib |
| title | Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-01T16%3A07%3A15IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_hal_p&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Pharmacology,%20safety,%20efficacy%20and%20clinical%20uses%20of%20the%20COX%E2%80%902%20inhibitor%20robenacoxib&rft.jtitle=Journal%20of%20veterinary%20pharmacology%20and%20therapeutics&rft.au=Lees,%20Peter&rft.date=2022-07&rft.volume=45&rft.issue=4&rft.spage=325&rft.epage=351&rft.pages=325-351&rft.issn=0140-7783&rft.eissn=1365-2885&rft_id=info:doi/10.1111/jvp.13052&rft_dat=%3Cproquest_hal_p%3E2654297951%3C/proquest_hal_p%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=2654297951&rft_id=info:pmid/35460083&rfr_iscdi=true |