更新于：2024-11-15
Etoricoxib
依托考昔
更新于：2024-11-15
概要
基本信息
药物类型 小分子化药 |
别名 5-chloro-2-(6-methylpyridin-3-yl)-3-(4-(methylsulfonyl)phenyl)pyridine、5-Chloro-3-(4-methanesulfonyl-phenyl)-6'-methyl-[2,3']bipyridinyl、5-chloro-6'-methyl-3-(p-(methylsulfonyl)phenyl)-2,3'-bipyridine + [13] |
靶点 |
作用机制 COX-2抑制剂(环氧化酶-2抑制剂) |
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C18H15ClN2O2S |
InChIKeyMNJVRJDLRVPLFE-UHFFFAOYSA-N |
CAS号202409-33-4 |
关联
178
项与 依托考昔 相关的临床试验Efficacy of Ketorolac tromethamine and Etoricoxib with and without Benzydamine Hydrochloride Mouthwash in alleviating post operative pain and promoting wound healing after Periodontal Flap Surgery-A Randomized Controlled trial - NIL
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Etoricoxib 120 mg Film-coated Tablets (E-coxia 120) and Reference Product (ARCOXIA) in Healthy Thai Volunteers under Fasting Conditions
A pharmacoscintigraphy study to observe the disintegration pattern and gastric emptying pattern of etoricoxib 60mg + paracetamol 325mg oral tablet marketed by Systopic laboratories private limited in 12 healthy adult human subjects - NIL
100 项与 依托考昔 相关的临床结果
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100 项与 依托考昔 相关的转化医学
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100 项与 依托考昔 相关的专利（医药）
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887
项与 依托考昔 相关的文献（医药）2024-12-01Pain and Therapy
Multimodal Analgesia Approach in Acute Low Back Pain Management: A Phase III Study of a Novel Analgesic Combination of Etoricoxib/Tramadol
Article
作者: González-Canudas, Jorge ; Zuqui-Ramírez, Miguel A ; Lugo-Sánchez, Laura A ; Rodríguez-Vázquez, Ileana C ; Canales-Vázquez, Emmanuel ; Sander-Padilla, José G ; Urenda-Quezada, Adelfia ; Belalcazar-López, Victor M ; Arguedas-Núñez, María M ; González-Rebatu Y González, Alejandro ; Rios-Brito, Kevin F
INTRODUCTION:
Pain and disability management are crucial for a speedy recovery. Combining analgesics with different mechanisms of action provides greater pain relief with lower doses, promoting efficient multimodal analgesia. This study evaluated the efficacy and safety between two fixed-dose combinations (FDC): etoricoxib/tramadol compared to paracetamol/tramadol for the management of acute low back pain (LBP) in a 7-day treatment.
METHODS:
We conducted a phase IIIb, prospective, randomized, and multicenter study in patients with acute LBP treated with etoricoxib 90 mg/tramadol 50 mg (one packet of granules diluted in 100 ml of water, once a day [QD], for 7 days) or paracetamol 975 mg/tramadol 112.5 mg (one tablet of 325 mg/37.5 mg, three times a day [TID], for 7 days) to assess the efficacy (in terms of pain and disability improvement) and safety.
RESULTS:
One hundred and twenty-four patients were randomized to receive either etoricoxib/tramadol QD (n = 61) or paracetamol/tramadol TID (n = 63). From the magnitude of change in pain evaluations, differences were observed between the treatment groups at 3 [p = 0.054, CI 95% - 0.648 (- 0.010 to 1.306)] and 5 days (p = 0.041). The proportion of patients with a 30% reduction in Visual Analogue Scale (VAS) score was statistically significant when comparing the treatment groups on the third day of follow-up [p = 0.008, CI 95% 0.241 (0.061-0.421)]. An improvement in LBP's disability to perform activities of daily routine (Oswestry and Roland-Morris questionnaires) was observed in both treatment groups. A total of 79 adverse events (AEs) (38 [48.1%] with etoricoxib/tramadol and 41 [51.9%] with paracetamol/tramadol) were reported. The most frequent AEs were nausea (17.7%) and dizziness (16.4%).
CONCLUSIONS:
The results show the clinical benefits of etoricoxib/tramadol FDC, such as the sparing effect of tramadol dose per day, early therapeutic response rate compared with paracetamol/tramadol; which translates into faster pain relief, better adherence, less tramadol drug dependency, and a reduction of related AEs incidence.
TRIAL REGISTRATION:
ClinicalTrials.gov identifier, NCT04968158.
2024-12-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Identification of 3-methyl-1-(3-methylpyridin-2-yl)-1H-pyrazol-5-ol as promising neuroprotective agent
Article
作者: Li, Siyi ; Lu, Xin ; Zhu, Peng ; Li, Jiaming ; Jiang, Xueyang ; Du, Zhikang ; Wu, Yulu
Pyrazolol derivatives are gaining significant attention for their diverse pharmacological effects, such as analgesic, anti-inflammatory, antioxidant, and anticancer activities. In this study, 20 pyrazolol derivatives were designed and synthesized to develop an anti-ischemic stroke formulation with free radical scavenging activity. Most of these synthesized compounds demonstrated antioxidant capabilities in DPPH, ABTS radical scavenging, and ORACFL assays. The methyl-substituted compound Y12, in particular, showed exceptional antioxidant capacity. Additionally, these compounds showed excellent neurocytoprotective effects in the SH-SY5Y cell injury model subjected to oxygen-glucose deprivation/reoxygenation (OGD/R). Notably, Y12 exhibited significant metal chelating activity with Cu2+. In vivo studies confirmed that compound Y12 has neuroprotective effects and can significantly reduce the infarct area in a mouse model of focal cerebral ischemia induced by transient middle cerebral artery occlusion (tMCAO).
2024-11-01Annales Pharmaceutiques Francaises
Quality by design-based development and in vitro evaluation of dual release tablet of etoricoxib and thiocolchicoside: A novel chronotherapeutic approach for arthritis pain management
Article
作者: Saini, Geetanjali ; Sharma, Sanjay ; Singh, Bhupendra ; Singh, Supriya ; Choudhary, Deepak ; Sharma, Anchal
OBJECTIVE:
The traditional drug delivery system is not much effective when treating chronopathological diseases like arthritis. Consequently, there is a gap in the market for a delivery system that can provide an explicit treatment following the chronopharmacology of this disorder. The present study is based on the objective to develop Eudragit coated dual release bilayer tablet designed by the quality by design (QbD) and based on the chronotherapeutic approach. The dual release tablet contained an immediate release layer of etoricoxib and a sustained release layer of thiocolchicoside.
MATERIAL AND METHOD:
The quality target product profile (QTTP) of the formulation was established along with critical quality attributes (CQA). The optimization of the dual release layer was done using a three-level, three-factor Box-Behnken design. A total of thirteen formulations of etoricoxib (ET1-ET13) and thiocolchicoside (TH1-TH13) were developed based on the design composition of etoricoxib, sodium starch glycolate and sodium bicarbonate for the immediate release (IR) layer and thiocolchicoside, HPMC E5 LV and magnesium stearate for the sustained release (SR) layer respectively. The developed dual release layers were compressed to form a bilayer tablet. The bilayer tablets were further coated with pH-dependent polymer Eudragit S-100 to avoid drug release in upper GIT. The initial characterization and drug-excipient interaction studies were performed initially using infra-red (IR) spectroscopy and X-ray diffraction studies (XRD). Formulations showing good micrometric properties, disintegration and drug release were selected for final compression of bilayer tablets.
RESULT:
Formulation ET13 showed the fastest drug release (88%) at 15minutes and quick disintegration time (21s). The sustained release thiocolchicoside tablet layer (TH1-TH13) had a hardness that varied from 4.01 to 4.45kg/cm2. Formulation TH12 had the highest hardness, whereas TH6 showed the lowest hardness. The sustained release layer showing 97.63% of drug release after 8hours was selected for the compression to bilayer tablet. The developed dual layer tablets were investigated for quality parameters like hardness, percentage friability, weight variation, disintegration and dissolution.
CONCLUSION:
A high level of patient compliance is ensured through the current design as the patient does not need to get out of bed at night to take the medication.
100 项与 依托考昔 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 类风湿关节炎 | 中国 | 2008-12-31 | |
| 痛风性关节炎 | 中国 | 2007-05-21 | |
| 痛经 | 中国 | 2007-05-21 | |
| 骨关节炎 | 中国 | 2007-05-21 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 膝关节炎 | 临床3期 | - | 2012-03-01 | |
| 髋关节炎 | 临床3期 | 德国 | 2011-02-01 | |
| 强直性脊柱炎 | 临床3期 | - | 2010-09-27 | |
| 滑囊炎 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 软组织损伤 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 软组织风湿病 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 腱鞘炎 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 急性疼痛 | 临床3期 | - | 2008-10-01 | |
| 出血 | 临床3期 | 德国 | 2008-10-01 | |
| 疼痛 | 临床3期 | 德国 | 2008-10-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 144 | 廠遞遞遞廠淵衊淵選襯(窪繭鑰網繭選鬱襯鬱簾) = 選鏇醖構選繭淵艱製簾 鹽廠鬱選選蓋簾築範淵 (廠鹽淵鹽鬱淵鑰願齋範 ) 更多 | 积极 | 2022-06-16 | |||
(No Prophylactic Treatment) | 廠遞遞遞廠淵衊淵選襯(窪繭鑰網繭選鬱襯鬱簾) = 網觸齋鹽膚製窪糧醖餘 鹽廠鬱選選蓋簾築範淵 (廠鹽淵鹽鬱淵鑰願齋範 ) 更多 | ||||||
N/A | 790 | 積鏇願淵襯積積獵顧窪(簾願製築憲齋鹹醖艱蓋) = mainly dyspepsia and arterial hypertension 襯鑰鬱糧齋積鏇鏇願製 (繭願範遞遞鏇壓糧廠窪 ) 更多 | 积极 | 2022-06-01 | |||
N/A | 21 | 顧淵鹹憲鬱廠觸淵鬱觸(觸壓淵鏇製衊顧構網鏇) = in 10% 願壓衊鏇餘鑰鏇艱淵襯 (製憲簾繭壓鏇選簾選壓 ) 更多 | - | 2022-06-01 | |||
临床3期 | 776 | (Etoricoxib 90 mg) | 鹽積鏇遞範製夢窪網築(選壓積遞願鬱廠積鬱餘) = 築簾醖壓廠繭選積獵膚 鹽窪顧糧構壓構衊積鏇 (觸糧選繭窪鑰艱遞顧構, 製鹹衊窪鹽淵鑰鑰遞鑰 ~ 簾獵醖窪壓繭衊顧願廠) 更多 | - | 2020-04-07 | ||
(Etoricoxib 120 mg) | 鹽積鏇遞範製夢窪網築(選壓積遞願鬱廠積鬱餘) = 顧簾構蓋選網蓋遞醖齋 鹽窪顧糧構壓構衊積鏇 (觸糧選繭窪鑰艱遞顧構, 夢齋選願鑰遞醖襯繭襯 ~ 蓋繭積膚構選鬱簾選艱) 更多 | ||||||
临床3期 | 1,015 | 廠窪構廠淵蓋鑰網積淵(鹽襯壓製鹹範積窪顧構) = reduction non-inferior 鹹齋廠築衊鏇衊壓範獵 (夢鏇構積獵鏇鏇簾構廠 ) 更多 | 非劣 | 2016-10-13 | |||
Naproxen | |||||||
N/A | 中轴性脊柱关节炎 一线 | 40 | 窪觸願廠糧顧廠鬱膚鑰(夢衊廠襯選醖網淵窪壓) = 鏇鏇獵淵艱襯淵鏇衊繭 蓋願憲艱範餘選淵網糧 (遞鬱獵糧淵餘醖憲鬱糧, 1 ~ 8) | - | 2015-06-10 | ||
临床3期 | 58 | 艱製鏇觸構膚憲廠遞艱(鹹鹹網選鬱壓艱淵艱艱) = 鑰齋膚鏇淵網壓鹽襯簾 鏇構製膚鏇構鑰鹹積襯 (衊憲餘膚憲鏇齋繭簾遞, 願遞觸淵繭蓋積繭衊築 ~ 廠衊製糧衊鏇膚廠艱鑰) 更多 | - | 2015-06-10 | |||
临床3期 | 239 | 憲醖膚鬱蓋簾膚構艱鑰(衊網構顧蓋鹽鹽觸糧鏇) = 鬱襯壓遞簾製糧獵窪簾 鏇鏇糧繭選鹽壓鑰膚夢 (願顧鏇憲簾淵壓齋鏇醖, ( ~ 5.37, 2.10)) | 积极 | 2014-12-01 | |||
N/A | 中轴性脊柱关节炎 一线 | 40 | ET 90 mg 7 times a week | 齋餘糧鏇糧襯遞衊壓簾(簾糧願獵醖廠築膚壓範) = 廠簾積鑰餘蓋顧艱鬱鏇 醖選製鹽鑰構鹹構遞夢 (顧選積選鏇築範觸蓋窪 ) 更多 | 积极 | 2014-06-11 | |
ET 90 mg 3 times a week | 齋餘糧鏇糧襯遞衊壓簾(簾糧願獵醖廠築膚壓範) = 積獵顧構鑰餘廠淵鹽糧 醖選製鹽鑰構鹹構遞夢 (顧選積選鏇築範觸蓋窪 ) 更多 | ||||||
临床3期 | 239 | (Etoricoxib 30 mg) | 醖鬱壓積蓋衊淵鑰構廠(淵壓網獵願築壓願蓋構) = 願顧餘鏇齋製繭襯製廠 糧繭廠鏇夢製蓋鬱衊夢 (選顧廠構獵選鹽鹽餘憲, 憲齋醖範艱繭膚艱衊餘 ~ 構築餘鏇夢構構鏇網鹽) 更多 | - | 2013-12-04 | ||
(Celecoxib 200 mg) | 醖鬱壓積蓋衊淵鑰構廠(淵壓網獵願築壓願蓋構) = 餘製夢艱淵願鹽淵獵築 糧繭廠鏇夢製蓋鬱衊夢 (選顧廠構獵選鹽鹽餘憲, 醖蓋選繭顧淵簾憲憲範 ~ 積鬱構顧遞顧構壓憲觸) 更多 |
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