Joy T R, Hegele R A
Department of Medicine, Robarts Research Institute and Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada.
Br J Pharmacol. 2008 Aug;154(7):1379-81. doi: 10.1038/bjp.2008.248. Epub 2008 Jun 9.
The failure of the cholesterol ester transfer protein (CETP) inhibitor, torcetrapib, has led to questions regarding whether the molecule itself or the mechanism of CETP inhibition was responsible for the adverse cardiovascular outcomes. Given the association with increases in blood pressure and plasma aldosterone levels, torcetrapib has been postulated to have adverse 'off-target' effects. In this issue of British Journal of Pharmacology, Forrest and co-workers have elegantly investigated these effects, demonstrating two salient points -- (1) the pressor effect of torcetrapib is independent of CETP inhibition and (2) although associated with hyperaldosteronism, the pressor effect is likely not mediated by hyperaldosteronism. Anacetrapib, by contrast, did not demonstrate any pressor or off-target effects. Despite these findings, it remains to be proven whether the adverse cardiovascular outcomes from torcetrapib were indeed related to the pressor effects and whether CETP inhibition by other agents will result in beneficial clinical outcomes. Yet, the studies of Forrest and co-workers do bring us closer to unravelling the reasons behind the failure of torcetrapib.
胆固醇酯转运蛋白(CETP)抑制剂托彻普(torcetrapib)的失败引发了关于是该分子本身还是CETP抑制机制导致不良心血管结局的疑问。鉴于其与血压升高和血浆醛固酮水平增加有关,有人推测托彻普具有不良的“脱靶”效应。在本期《英国药理学杂志》中,福雷斯特及其同事对这些效应进行了出色的研究,证明了两个要点——(1)托彻普的升压效应独立于CETP抑制;(2)尽管与醛固酮增多症相关,但升压效应可能不是由醛固酮增多症介导的。相比之下,阿那曲普(anacetrapib)未表现出任何升压或脱靶效应。尽管有这些发现,但托彻普的不良心血管结局是否确实与升压效应有关,以及其他药物抑制CETP是否会产生有益的临床结局仍有待证实。然而,福雷斯特及其同事的研究确实让我们更接近揭开托彻普失败背后的原因。