Lomitapide and mipomersen are antihyperlipidemic agents indicated for treating homozygous familial hypercholesterolemia (HoFH). Lomitapide is approved by the US Food and Drug Administration (FDA) for use alongside other antilipidemic drugs and a low-fat diet to lower serum lipids, decrease low-density lipoprotein (LDL) cholesterol (LDL-C), total cholesterol, apolipoprotein B (apo-B), and non–high-density lipoprotein cholesterol in patients with HoFH. Patients with HoFH might present with arcus corneae, tendinous xanthomas, xanthelasma, and planar or tuberous xanthomas. Lomitapide could be beneficial for HoFH patients exhibiting insufficient response to PCSK9 inhibitor treatment, those with atherosclerotic cardiovascular disease and a baseline LDL-C of 190 mg/dL or higher, and those who demonstrate insufficient responses to statins, whether used alone or in combination with PCSK9 inhibitors or ezetimibe. Lomitapide rapidly binds to and inhibits microsomal triglyceride transfer protein (MTP) within the endoplasmic reticulum lumen, which impedes the synthesis of lipoproteins containing apo-B in both hepatocytes and enterocytes. This process reduces the production of very low-density lipoprotein and chylomicrons, thereby lowering plasma LDL-C levels. The safety and efficacy of lomitapide have not been established for heterozygous familial hypercholesterolemia. This activity elucidates the indications, mechanism of action, pharmacokinetics, adverse event profile, and other relevant interactions essential for interprofessional healthcare team members in treating patients with HoFH and related conditions.
- Provider:StatPearls, LLC
- Activity Link: https://www.statpearls.com/ArticleLibrary/viewarticle/111460
- Start Date: 2023-09-01 05:00:00
- End Date: 2023-09-01 05:00:00
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- Specialty: Adolescent Medicine, Adult Cardiac, Adult Congenital Heart Disease, Cardiothoracic, Cardiovascular, Cardiovascular Disease, Chemical Pathology, Endocrinology, Diabetes, and Metabolism, General Pediatrics, General Surgery, Geriatric Medicine, Hospital Medicine, Internal Medicine, Interventional Cardiology, Molecular Genetic Pathology, Pediatric Cardiology