Romanian Society of Pharmaceutical Sciences

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PERSPECTIVES IN LIPID LOWERING THERAPY. NEW THERAPIES TARGETING LDL – CHOLESTEROL

ADRIANA MIHAELA ILIEŞIU 1,2*, IRINA PÂRVU 2, ANDREEA SIMONA HODOROGEA 1,2, IOAN TIBERIU NANEA 1,2, ANDREEA CATARINA POPESCU 1

1.“Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
2.“Prof. Dr. Th. Burghele” Clinical Hospital, Department of Internal Medicine and Cardiology, 20 Panduri Road, District 5, Bucharest, Romania
*corresponding author: [email protected]

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New lipid-lowering drugs are needed, because current treatment options, in which statins play a central role, are limited by suboptimal control of low-density lipoprotein cholesterol (LDL-C), the ineffectiveness of treatment in some forms of dyslipidaemia, and residual cardiovascular risks. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, among which human monoclonal antibodies are currently recommended by guidelines, increase the number of LDL receptors, lowering serum LDL-C levels. Monoclonal antibodies are indicated, in addition to diet and statins in highest tolerated doses, in heterozygous familial hypercholesterolemia, or in patients with high cardiovascular risk, when a lower level of LDL-C is required. Bempedoic acid (ETC 1002) is an inhibitor of adenosine triphosphate citrate lyase, reducing cholesterol synthesis in hepatocytes, with hypocholesterolemic and anti-inflammatory effects. In familial hypercholesterolemia, apoB-100 inhibitors (the antisense oligonucleotide mipomersen) or microsomal triglyceride transfer protein inhibitors (lopitamid) are niche drugs because of adverse reactions, being only indicated in homozygous forms. LDL-C apheresis is an alternative in forms of familial hypercholesterolemia unresponsive to pharmacological treatment.