Data di Pubblicazione:
2024
Citazione:
Low-Density Lipoprotein Cholesterol-Lowering Drugs: A Narrative Review / N. Ferri, M. Ruscica, S. Fazio, A. Corsini. - In: JOURNAL OF CLINICAL MEDICINE. - ISSN 2077-0383. - 13:4(2024), pp. 943.1-943.24. [10.3390/jcm13040943]
Abstract:
The modern history of cholesterol-lowering drugs started in 1972 when Dr. Akira Endo
identified an active compound (compactin) that inhibited cholesterol biosynthesis from the culture
broth of blue–green mold (Penicillium citrinum Pen-51). Since 1987, statins have represented the
milestone for the treatment of atherosclerotic cardiovascular disease. A new therapy for the treatment
of hypercholesterolemia since the discovery of statins is ezetimibe, the first and only agent inhibiting
intestinal cholesterol absorption. Ezetimibe was approved by the FDA in October 2002. A year later,
the association between gain-of-function PCSK9 genetic mutations and hypercholesterolemia was
reported, and this discovery opened a new era in lipid-lowering therapies. Monoclonal antibodies
and small-interfering RNA approaches to reduce PCSK9 were developed and approved for clinical
use in 2015 and 2022, respectively. Finally, the newly approved bempedoic acid, an oral adenosine
triphosphate citrate lyase inhibitor that lowers LDL-C, is able to reduce major adverse cardiovascular
events in both primary and secondary prevention. In the present narrative review, we summarize the
pharmacological properties and the clinical efficacy of all these agents currently used for a tailored
therapy of hypercholesterolemia in patients with atherosclerotic cardiovascular disease.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
LDL-cholesterol; PCSK9; statins; bempedoic acid; ezetimibe; inclisiran
Elenco autori:
N. Ferri, M. Ruscica, S. Fazio, A. Corsini
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