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LCZ-696

机译:LCZ-696

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摘要

LCZ-696 is an investigational, dual-acting molecule consisting of the angiotensin II (Ang II) type 7 (AT_1) receptor blocker (ARB) valsartan and the neprilysin (neutral endopeptidase, NEP) inhibitor AHU-377. The rationale for the development of LCZ-696 is based on the concept of additive effects for the ARB valsartan and the NEP inhibitor AHU-377 for the treatment of hypertension and heart failure (HF). Valsartan, by blocking the AT_1 receptor, interferes with the vasoconstrictive and cardiovascular remodeling of Ang II and has been shown to be effective for the treatment of hypertension and HF. The other component of LCZ-696, AHU-377, is an NEP inhibitor that interferes with the catabolism of natriuretic peptides (NPs), leading to increased blood levels of NPs and promoting salt and water diuresis. This combined action of LCZ-696 can be very effective for the treatment of hypertension and HF. So far, clinical trials have shown that LCZ-696 is effective and safe for the treatment of hypertension. Large clinical trials for the treatment of HF are under way and results will be reported soon. Based on the current information, approval of LCZ-696 will be a useful addition to our armamentarium for the treatment of hypertension and HF.
机译:LCZ-696是一种研究性双分子,由血管紧张素II(Ang II)7型(AT_1)受体阻断剂(ARB)缬沙坦和中性溶酶(中性内肽酶,NEP)抑制剂AHU-377组成。开发LCZ-696的基本原理是基于ARB缬沙坦和NEP抑制剂AHU-377对高血压和心力衰竭(HF)的加和作用。缬沙坦可通过阻断AT_1受体来干扰Ang II的血管收缩和心血管重塑,已被证明可有效治疗高血压和心衰。 LCZ-696的另一个组件AHU-377是NEP抑制剂,可干扰利钠肽(NP)的分解代谢,导致NPs的血中浓度升高,并促进盐和水利尿作用。 LCZ-696的这种联合作用对于高血压和HF的治疗非常有效。到目前为止,临床试验表明,LCZ-696治疗高血压是安全有效的。治疗HF的大型临床试验正在进行中,并将很快报告结果。根据当前信息,LCZ-696的批准将成为我们用于治疗高血压和心衰的军备库的有用补充。

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