Dalcetrapib
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چکیده
Roche and Japan Tobacco are in a licensing agreement to develop and commercialize dalcetrapib, a cholesteryl ester transfer protein (CETP) inhibitor to slow or prevent atherosclerosis. This drug is currently in phase III development. This review discusses the development history and scientific profile of this new compound.
منابع مشابه
Safety and tolerability of dalcetrapib (RO4607381/JTT-705): results from a 48-week trial
AIMS Co-primary objectives were to evaluate dalcetrapib (JTT-705/RO4607381), which targets cholesteryl ester transfer protein (CETP), effects on high-density lipoprotein cholesterol (HDL-C) in participants with coronary heart disease or risk equivalents and to evaluate potential changes in mesenteric lymph nodes. METHODS AND RESULTS Double-blind trial with participants randomized (2:1) to dal...
متن کاملDalcetrapib and anacetrapib differently impact HDL structure and function in rabbits and monkeys[S]
Inhibition of cholesteryl ester transfer protein (CETP) increases HDL cholesterol (HDL-C) levels. However, the circulating CETP level varies and the impact of its inhibition in species with high CETP levels on HDL structure and function remains poorly characterized. This study investigated the effects of dalcetrapib and anacetrapib, the two CETP inhibitors (CETPis) currently being tested in lar...
متن کاملBiochemical characterization of cholesteryl ester transfer protein inhibitors.
Cholesteryl ester transfer protein (CETP) has been identified as a novel target for increasing HDL cholesterol levels. In this report, we describe the biochemical characterization of anacetrapib, a potent inhibitor of CETP. To better understand the mechanism by which anacetrapib inhibits CETP activity, its biochemical properties were compared with CETP inhibitors from distinct structural classe...
متن کاملImproved Synthesis and Crystal Structure of Dalcetrapib
An improved synthesis of the Cholesteryl Ester Transfer Protein inhibitor dalcetrapib is reported. The precursor disulfide was reduced (a) by Mg/MeOH or (b) by EtSH/DBU/THF. The resulting thiol was acylated (a) by a known procedure or (b) in a one-pot process. Impurities were removed (a) by dithiothreitol (DTT) or (b) by oxidation using H2O2. Dalcetrapib crystallized in space group P21/c.
متن کاملVascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial.
AIMS High-density lipoprotein cholesterol (HDL-C) is inversely associated with cardiovascular (CV) events and thus an attractive therapeutic target. However, in spite of marked elevations in HDL-C, the first cholesterol transport protein (CETP) inhibitor torcetrapib raised blood pressure (BP), impaired endothelial function, and increased CV mortality and morbidity. Dalcetrapib is a novel molecu...
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عنوان ژورنال:
دوره 10 شماره
صفحات -
تاریخ انتشار 2010