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• W1586702946 abstract "The correlation between high-density lipoprotein cholesterol (HDL-C) levels and cardiovascular risk is well established. Cholesteryl ester transfer protein (CETP) has been investigated as a target for HDL-raising intervention. Torcetrapib and dalcetrapib are compounds from two different chemical classes that differ in lipophilicity and affect CETP activity by different mechanisms. The development of the CETP inhibitor torcetrapib was prematurely halted due to increased mortality in torcetrapib-treated patients during the phase III ILLUMINATE trial. More recently, the dal-HEART phase III clinical trial program with the CETP modulator dalcetrapib was halted due to lack of efficacy, although no significant safety signals were observed. Torcetrapib and most torcetrapib derivatives share the properties of directly increasing aldosterone secretion in vitro and blood pressure in many animal species. Thorough investigation of both dalcetrapib and anacetrapib (another CETP inhibitor) in preclinical and clinical studies with regard to effect on plasma aldosterone level and blood pressure showed no evidence of clinically relevant changes in either parameter. Off-target effects on two important regulators of low-density lipoprotein (LDL) metabolism (LDL receptor and PCSK9 expression) have also been observed with the CETP inhibitors torcetrapib, anacetrapib, and evacetrapib, but not with the CETP modulator dalcetrapib, suggesting a range of nontarget activities of highly lipophilic derivatives of torcetrapib. Preclinical studies suggested an effect of dalcetrapib on lymph node macrophages, but the underlying molecular mechanisms support a lack of relevance to the clinical setting. In conclusion, understanding the mechanism of off-target activities of torcetrapib has allowed other compounds that affect CETP activity, including dalcetrapib, anacetrapib, and evacetrapib, to be derisked, and for development of this class to continue despite the phase III safety findings of torcetrapib." @default.
• W1586702946 created "2016-06-24" @default.
• W1586702946 creator A5064835358 @default.
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• W1586702946 date "2015-04-22" @default.
• W1586702946 modified "2023-10-14" @default.
• W1586702946 title "Torcetrapib and Dalcetrapib Safety: Relevance of Preclinical <i>In Vitro</i> and <i>In Vivo</i> Models" @default.
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• W1586702946 doi "https://doi.org/10.1002/9783527673643.ch19" @default.
• W1586702946 hasPublicationYear "2015" @default.
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