Pharmacokinetics and Pharmacodynamics of LCZ696, a Novel Dual‐Acting Angiotensin Receptor—Neprilysin Inhibitor (ARNi)
@article{Gu2010PharmacokineticsAP, title={Pharmacokinetics and Pharmacodynamics of LCZ696, a Novel Dual‐Acting Angiotensin Receptor—Neprilysin Inhibitor (ARNi)}, author={Jessie Gu and Adele No{\`e} and Priya Chandra and Suliman I. Al-Fayoumi and Monica Ligueros‐Saylan and Ramesh Sarangapani and Suzanne Maahs and Gary Michael Ksander and Dean F. Rigel and Arco Y. Jeng and Tsu-han Lin and Weiyi Zheng and William P. Dole}, journal={The Journal of Clinical Pharmacology}, year={2010}, volume={50} }
Angiotensin receptor blockade and neprilysin (NEP) inhibition together offer potential benefits for the treatment of hypertension and heart failure. LCZ696 is a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio). Oral administration of LCZ696 caused dose‐dependent increases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague‐Dawley rats and provided sustained, dose‐dependent blood pressure reductions in…
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While atorvastatin had no significant impact on the pharmacokinetics of LCZ696 analytes upon co-administration, the Cmax of atorVastatin and its metabolites increased twofold, with a marginal increase in AUC.
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All pharmacokinetic parameters ofLCZ696 analytes (LBQ657 and valsartan) were similar between male and female subjects, indicating no effect on the pharmacokinetics of LCZ696 analyzetes based on sex.
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