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一酸化窒素供与型COX阻害薬（英: COX-inhibiting nitric ox … 一酸化窒素供与型COX阻害薬（英: COX-inhibiting nitric oxide donators、CINODs）はNO-NSAIDsとも呼ばれる非ステロイド性抗炎症薬（NSAIDs）の一群で、NSAIDsの安全性向上を目標に開発されている医薬品である。 CINODは既存のNSAID分子に一酸化窒素（NO）供与基を結合した化合物であり、通常両者はエステル結合で結ばれる。CINODsはシクロオキシゲナーゼ（COX）阻害に基づくNSAIDsの抗炎症作用を維持する一方で、一酸化窒素に基づく血管拡張作用、白血球接着阻害作用、カスパーゼ阻害作用により消化器系および血管系の副作用を軽減している。 最初のCINODは1990年代に開発され始めたが、上市された化合物はない。であるロフェコキシブやが2000年代中盤に血管系の副作用で市場から撤退した事でCINODsの重要性は高まっている。さらに、既存のNSAIDsは血圧を上昇させ、高血圧治療薬の作用に拮抗する。CINODsのいくつかは治験の段階にある。その内では（NO-ナプロキセン）が最も先行していたが、2010年に米国FDAがさらなる臨床試験の必要性を指摘し不承認を決定した。他のCINODsも炎症関連疾患の治療薬として開発中である。を指摘し不承認を決定した。他のCINODsも炎症関連疾患の治療薬として開発中である。
, Les inhibiteurs de cyclooxygénase à libéra … Les inhibiteurs de cyclooxygénase à libération de monoxyde d'azote ou NO-AINS (en anglais COX-inhibiting nitric oxide donator, CINOD ou NO-NSAID), sont une nouvelle classe d’anti-inflammatoires. Ces composés organiques sont des nitroesters d'anti-inflammatoires non stéroïdiens qui peuvent être utilisés en remplacement des AINS d'ancienne génération. Ces composés ont été décrits pour la première fois par (en) et ses collègues de l'Université de Calgary. Ils sont dérivés d'un AINS existant auquel est ajouté, généralement par liaison ester, un radical libérant du monoxyde d'azote (NO). Les NO-AINS conservent ainsi l'efficacité anti-inflammatoire des AINS via l'inhibition des cyclooxygénases (COX) tout en améliorant la sécurité gastrique et vasculaire, vraisemblablement via la vasodilatation, l'inhibition de l'adhésion des leucocytes et l'inhibition des caspases, autant d'effets connus du NO. En plus d'être actifs sur la COX-2, les inhibiteurs de cyclooxygénase non sélectifs agissent également sur la COX-1, avec tous les effets secondaires que cela entraine (principalement une élevée). L'introduction de nitrate dans la structure moléculaire a permis d'éviter ou d'atténuer ces effets secondaires : les NO-AINS libèrent in vivo du monoxyde d'azote, un puissant vasodilatateur endogène aux effets cytoprotecteurs similaires à ceux des prostaglandines. Le naproxcinod est le composé le plus avancé de cette nouvelle génération, qui potentiellement peut changer les habitudes des prescripteurs et augmenter la sécurité des patients sous traitement long et en particulier les personnes âgées.ong et en particulier les personnes âgées.
, COX-inhibiting nitric oxide donators (CINO … COX-inhibiting nitric oxide donators (CINODs), also known as NO-NSAIDs, are a new class of nonsteroidal anti-inflammatory drug (NSAID) developed with the intention of providing greater safety than existing NSAIDs. These compounds were first described by John Wallace and colleagues. CINODs are compounds generated by the fusion of an existing NSAID with a nitric oxide (NO)-donating moiety by chemical means, usually by ester linkage. CINODs retain the anti-inflammatory efficacy of NSAIDs via inhibition of cyclooxygenase (COX) while arguably improving upon gastric and vascular safety, most likely via vasorelaxation, inhibition of leukocyte adhesion and inhibition of caspases, all known effects of NO. The first CINODs were developed in the 1990s, and as yet none have been approved for use by the general public. The importance of developing such drugs was increased when COX-2-specific NSAIDs rofecoxib (Vioxx) and lumiracoxib (Prexige) were removed from major pharmaceutical markets in the mid-2000s due to vascular safety concerns. In addition, traditional NSAIDs increase blood pressure and interfere with the actions of antihypertensive drugs. Several CINODs are currently being tested in clinical trials, the most advanced of which are being conducted by the French pharmaceutical company NicOx, whose flagship compound naproxcinod (NO-naproxen, nitronaproxen) is in phase III trials for the treatment of osteoarthritis. Naproxcinod is a fusion of naproxen and a NO-donating group. Other CINODs are also being tested by NicOx for the treatment of diseases in which inflammation plays a role.seases in which inflammation plays a role.
, Per COX-inibitori a rilascio di monossido … Per COX-inibitori a rilascio di monossido di azoto o FANS a rilascio di monossido di azoto o più semplicemente NO-FANS si intende una classe di composti organici ottenuti da derivati nitro-esteri dei farmaci antinfiammatori non steroidei che possono essere impiegati in ambito terapeutico in sostituzione ai FANS di vecchia generazione. Furono descritti per la prima volta dal professor John Wallace dell'università di Calgary. I COX-inibitori non selettivi delle cicloossigenasi oltre ad essere attivi sulla COX-2 hanno anche affinità per la COX-1, con tutti gli effetti collaterali che ciò comporta (in primis l'elevata gastrolesività). L'introduzione del nitrato nella struttura molecolare è stata studiata al fine di scongiurare ed attenuare gli effetti collaterali che derivano dall'inibizione non selettiva delle COX; infatti in vivo gli NO-FANS rilasciano monossido d'azoto, potente vasodilatatore endogeno con effetti citoprotettivi simili a quelli delle prostaglandine.tivi simili a quelli delle prostaglandine.
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Per COX-inibitori a rilascio di monossido … Per COX-inibitori a rilascio di monossido di azoto o FANS a rilascio di monossido di azoto o più semplicemente NO-FANS si intende una classe di composti organici ottenuti da derivati nitro-esteri dei farmaci antinfiammatori non steroidei che possono essere impiegati in ambito terapeutico in sostituzione ai FANS di vecchia generazione. Furono descritti per la prima volta dal professor John Wallace dell'università di Calgary. I COX-inibitori non selettivi delle cicloossigenasi oltre ad essere attivi sulla COX-2 hanno anche affinità per la COX-1, con tutti gli effetti collaterali che ciò comporta (in primis l'elevata gastrolesività). L'introduzione del nitrato nella struttura molecolare è stata studiata al fine di scongiurare ed attenuare gli effetti collaterali che derivano dall'inibizione ncollaterali che derivano dall'inibizione n
, 一酸化窒素供与型COX阻害薬（英: COX-inhibiting nitric ox … 一酸化窒素供与型COX阻害薬（英: COX-inhibiting nitric oxide donators、CINODs）はNO-NSAIDsとも呼ばれる非ステロイド性抗炎症薬（NSAIDs）の一群で、NSAIDsの安全性向上を目標に開発されている医薬品である。 CINODは既存のNSAID分子に一酸化窒素（NO）供与基を結合した化合物であり、通常両者はエステル結合で結ばれる。CINODsはシクロオキシゲナーゼ（COX）阻害に基づくNSAIDsの抗炎症作用を維持する一方で、一酸化窒素に基づく血管拡張作用、白血球接着阻害作用、カスパーゼ阻害作用により消化器系および血管系の副作用を軽減している。 最初のCINODは1990年代に開発され始めたが、上市された化合物はない。であるロフェコキシブやが2000年代中盤に血管系の副作用で市場から撤退した事でCINODsの重要性は高まっている。さらに、既存のNSAIDsは血圧を上昇させ、高血圧治療薬の作用に拮抗する。CINODsのいくつかは治験の段階にある。その内では（NO-ナプロキセン）が最も先行していたが、2010年に米国FDAがさらなる臨床試験の必要性を指摘し不承認を決定した。他のCINODsも炎症関連疾患の治療薬として開発中である。を指摘し不承認を決定した。他のCINODsも炎症関連疾患の治療薬として開発中である。
, COX-inhibiting nitric oxide donators (CINODs), also known as NO-NSAIDs, are a new class of nonsteroidal anti-inflammatory drug (NSAID) developed with the intention of providing greater safety than existing NSAIDs.
, Les inhibiteurs de cyclooxygénase à libéra … Les inhibiteurs de cyclooxygénase à libération de monoxyde d'azote ou NO-AINS (en anglais COX-inhibiting nitric oxide donator, CINOD ou NO-NSAID), sont une nouvelle classe d’anti-inflammatoires. Ces composés organiques sont des nitroesters d'anti-inflammatoires non stéroïdiens qui peuvent être utilisés en remplacement des AINS d'ancienne génération. Le naproxcinod est le composé le plus avancé de cette nouvelle génération, qui potentiellement peut changer les habitudes des prescripteurs et augmenter la sécurité des patients sous traitement long et en particulier les personnes âgées.ong et en particulier les personnes âgées.
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COX-inhibiting nitric oxide donator
, Inhibiteur de cyclooxygénase à libération de monoxyde d'azote
, COX-inibitori a rilascio di monossido di azoto
, 一酸化窒素供与型COX阻害薬
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