ETC-1002 (Bempedoic acid) for the management of hyperlipidemia: from preclinical studies to phase 3 trials

Expert Opinion on Pharmacotherapy
M RuscicaC R Sirtori

Abstract

Tolerability problems in treating hypercholesterolemic patients undergoing statin treatment are of growing concern to physicians and patients, thus underlining the need for an agent with a similar mechanism but minimal side effects. A drug with a somewhat similar mechanism to statins but free of muscular side effects is ETC-1002 (bempedoic acid). It inhibits cholesterol biosynthesis at a step preceding HMG-CoA reductase, i.e. ATP citrate lyase (ACLY). A prodrug, ETC-1002 is converted to the active agent only in liver, not in skeletal muscle, and this may prevent any myotoxic activity. Area covered: The mechanism of ETC-1002 activity is described in detail, considering that ACLY inhibition markedly attenuated atherosclerosis in animal models. Clinical studies are also reported. Expert opinion: Present day LDL-C lowering treatments lead to significant reductions of cardiovascular (CV) events but, at times, the need to interrupt statin treatment appears to be dangerous due to a rapid rise in CV risk. The excellent tolerability of ETC-1002 makes it a useful alternative, either alone or as an adjunct to ezetimibe, for patients with statin intolerance needing to achieve significant CV risk reduction. ETC-1002 is also associated with ...Continue Reading

References

Dec 1, 1969·Archives of Biochemistry and Biophysics·J A WatsonJ M Lowenstein
May 1, 1995·Arteriosclerosis, Thrombosis, and Vascular Biology·K J Williams, I Tabas
May 23, 2000·Annals of Medicine·S BellostaA Corsini
Dec 10, 2003·The Journal of Biological Chemistry·Anne P BeigneuxStephen G Young
Feb 3, 2006·Cardiovascular Drugs and Therapy·Eric BruckertBernard Bégaud
Mar 24, 2006·The New England Journal of Medicine·Jonathan C CohenHelen H Hobbs
Feb 12, 2009·American Journal of Physiology. Endocrinology and Metabolism·Hyun Woo JeongJae Bum Kim
Mar 25, 2014·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Cesare R Sirtori
Dec 3, 2014·Atherosclerosis·Dragana NikolicMaciej Banach
Feb 3, 2015·European Journal of Internal Medicine·Paolo MagniMassimiliano Ruscica
Feb 20, 2015·European Heart Journal·Erik S StroesUNKNOWN European Atherosclerosis Society Consensus Panel
Apr 11, 2015·Archives of Medical Science : AMS·Maciej BanachDimitri P Mikhailidis
Apr 26, 2015·Journal of Clinical Lipidology·Terry A JacobsonW Virgil Brown
Apr 26, 2015·Journal of Clinical Lipidology·Giuliana MombelliCesare R Sirtori
Jun 4, 2015·The New England Journal of Medicine·Christopher P CannonUNKNOWN IMPROVE-IT Investigators
Jun 16, 2015·Journal of Clinical Lipidology·Paul D ThompsonRoger S Newton
Jan 23, 2016·Nature Reviews. Molecular Cell Biology·Mei Wang, Patrick J Casey
May 4, 2016·The American Journal of Cardiology·Christie M BallantyneNarendra D Lalwani
Sep 17, 2016·Journal of the American College of Cardiology·Yashashwi PokharelSalim S Virani
Sep 25, 2016·Current Atherosclerosis Reports·Ozlem Bilen, Christie M Ballantyne
Sep 28, 2016·JAMA : the Journal of the American Medical Association·Michael G SilvermanMarc S Sabatine
Nov 29, 2016·Nature Communications·Stephen L PinkoskyNarendra D Lalwani
Jan 7, 2017·Current Opinion in Lipidology·Amy C Burke, Murray W Huff
Jan 10, 2017·Expert Opinion on Investigational Drugs·Peter PensonMaciej Banach
Jan 26, 2017·European Journal of Preventive Cardiology·Stephen J NichollsDiederick E Grobbee
Mar 18, 2017·Journal of the American College of Cardiology·Maria-Corina SerbanRobert S Rosenson
Mar 18, 2017·The New England Journal of Medicine·Marc S SabatineUNKNOWN FOURIER Steering Committee and Investigators
Aug 29, 2017·The New England Journal of Medicine·Paul M RidkerUNKNOWN CANTOS Trial Group
Sep 2, 2017·Journal of the American College of Cardiology·Robert S RosensonPaul D Thompson

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Citations

May 8, 2019·European Journal of Preventive Cardiology·Cesare R SirtoriMassimiliano Ruscica
May 18, 2019·Expert Opinion on Drug Discovery·Massimiliano RuscicaCesare R Sirtori
Jul 26, 2019·Expert Opinion on Pharmacotherapy·Niki KatsikiMaciej Banach
Apr 1, 2020·Expert Opinion on Drug Metabolism & Toxicology·Brian TomlinsonChristopher Wai Kei Lam
Jul 17, 2020·PLoS Medicine·Arrigo F G CiceroUNKNOWN Lipid and Blood Pressure Meta-Analysis Collaboration (LBPMC) Group and the International Lipid Expert Panel (ILEP)
Jul 22, 2020·Journal of the American Heart Association·Alessandro Di MinnoMatteo Nicola Dario Di Minno
Sep 27, 2019·Pharmacological Reviews·Dongdong WangAtanas G Atanasov
Sep 20, 2020·International Journal of Molecular Sciences·Yoshiaki Sunami
Mar 30, 2020·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Li GuYoujun Li
Sep 10, 2019·Progress in Lipid Research·Xiaojun FengAi-Zong Shen
Dec 20, 2020·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Tongxin SongMiaomiao Jiang
Jan 28, 2021·Cardiovascular Drugs and Therapy·Andrey V SusekovGerald F Watts
Aug 26, 2020·Journal of Cardiovascular Medicine·Furio ColivicchiDomenico Gabrielli
Mar 7, 2021·International Journal of Molecular Sciences·Giulia Maria CamerinoSabata Pierno
Nov 25, 2020·Coronary Artery Disease·Chiara SchimmentiFabio Venturella
May 11, 2021·Clínica e investigación en arteriosclerosis : publicación oficial de la Sociedad Española de Arteriosclerosis·José López-Miranda, Juan Pedro-Botet
Jul 2, 2021·Expert Opinion on Drug Metabolism & Toxicology·Arrigo F G CiceroIvan Cincione
Jul 27, 2021·Seminars in Liver Disease·Yi ZhouXin Chen
Jun 17, 2021·Cardiology in Review·William SmithJames Nawarskas

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