dbo:abstract |
إيفاسيترابيب Evacetrapib هو من زمرة لا يزال قيد الدراسة، يعمل على زيادة مستويات البروتين دهني مرتفع الكثافة وخفض مستويات البروتين شحمي. لايسبب زيادة في ولا كما يفعل مركب (المركب الأول المصمم من هذه المجموعة، وقد تم إيقاف استخدامه بسبب زيادة احتمال حدوث أمراض القلب والشرايين عند استخدامه). (ar) Evacetrapib was a drug under development by Eli Lilly & Company (investigational name LY2484595) that inhibits cholesterylester transfer protein (CETP inhibitor). CETP collects triglycerides from very low-density lipoproteins (VLDL) or low-density lipoproteins (LDL) and exchanges them for cholesteryl esters from high-density lipoproteins (HDL), and vice versa, but primarily increasing high-density lipoprotein and lowering low-density lipoprotein. It is thought that modifying lipoprotein levels modifies the risk of cardiovascular disease. The first CETP inhibitor, torcetrapib, was unsuccessful because it increased levels of the hormone aldosterone and increased blood pressure, which led to excess cardiac events when it was studied. Evacetrapib does not have the same effect. When studied in a small clinical trial in people with elevated LDL and low HDL, significant improvements were noted in their lipid profile. Evacetrapib evaluation for treatment of high-risk vascular disease was discontinued due to lack of efficacy, as had already happened in the past with two other CETP inhibitors (torcetrapib and dalcetrapib) due to increased deaths and little identifiable cardiovascular benefit (despite substantial increases in HDL). Some hypothesize that CETP inhibitors may still be useful in the treatment of dyslipidemia, though significant caution is warranted. Anacetrapib is the fourth CETP inhibitor being tried for cardiovascular benefit (en) |
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LY2484595 (en) |
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Trans-4-({(5S)-5-[{[3,5-bis(trifluoromethyl)phenyl]methyl}(2-methyl-2H-tetrazol-5- yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1H-benzazepin-1-yl}methyl) cyclohexanecarboxylic acid (en) |
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Trans-4- cyclohexanecarboxylic acid (en) |
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rdfs:comment |
إيفاسيترابيب Evacetrapib هو من زمرة لا يزال قيد الدراسة، يعمل على زيادة مستويات البروتين دهني مرتفع الكثافة وخفض مستويات البروتين شحمي. لايسبب زيادة في ولا كما يفعل مركب (المركب الأول المصمم من هذه المجموعة، وقد تم إيقاف استخدامه بسبب زيادة احتمال حدوث أمراض القلب والشرايين عند استخدامه). (ar) Evacetrapib was a drug under development by Eli Lilly & Company (investigational name LY2484595) that inhibits cholesterylester transfer protein (CETP inhibitor). CETP collects triglycerides from very low-density lipoproteins (VLDL) or low-density lipoproteins (LDL) and exchanges them for cholesteryl esters from high-density lipoproteins (HDL), and vice versa, but primarily increasing high-density lipoprotein and lowering low-density lipoprotein. It is thought that modifying lipoprotein levels modifies the risk of cardiovascular disease. The first CETP inhibitor, torcetrapib, was unsuccessful because it increased levels of the hormone aldosterone and increased blood pressure, which led to excess cardiac events when it was studied. Evacetrapib does not have the same effect. When studied in (en) |
rdfs:label |
إيفاسيترابيب (ar) Evacetrapib (en) |
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