New cholesterol lowering medicines In 2025 .
Bempedoic acid (Nexletol)
Mechanism: Inhibits ATP citrate lyase, reducing cholesterol synthesis. – Dose: 180 mg once daily. – Use: Heterozygous familial hypercholesterolemia (HeFH) or established atherosclerotic cardiovascular disease (ASCVD) with statin intolerance. – Side effects: Hyperuricemia, gout, elevated liver enzymes.
What it is: An oral medication that is part of the class of drugs called ACLY inhibitors.
How it works: Inhibits the ACLY enzyme in the liver, which reduces the production of cholesterol. It also has other metabolic and anti-inflammatory effects.
Primary use: To lower LDL cholesterol in adults with heterozygous familial hypercholesterolemia, or other high-risk patients who require additional LDL reduction.
Administration: Oral tablet.
Key considerations: Can increase uric acid levels, potentially leading to gout. It also increases the blood concentration of some statins, so caution and dose adjustments are needed when co-administered with certain statins.
Inclisiran (Leqvio)
Mechanism: Small interfering RNA (siRNA) that reduces PCSK9 production, increasing LDL receptor activity. – Dose: 300 mg subcutaneously every 6 months. – Use: HeFH or ASCVD with elevated LDL-C despite maximally tolerated statin therapy. – Side effects: Injection-site reactions, flu-like symptoms.
Evolocumab (Repatha)
Mechanism: Monoclonal antibody that inhibits PCSK9, increasing LDL receptor activity. – Dose: 140 mg every 2 weeks or 420 mg monthly. – Use: HeFH or ASCVD with elevated LDL-C despite statin therapy. – Side effects: Injection-site reactions, flu-like symptoms, diabetes.
Alirocumab (Praluent)
Mechanism: Monoclonal antibody that inhibits PCSK9, increasing LDL receptor activity. – Dose: 75–300 mg every 2 weeks. – Side effects: Injection-site reactions, flu-like symptoms, myalgia.
Ezetimibe (Zetia)
Mechanism: Inhibits cholesterol absorption in the small intestine. – Dose: 10 mg once daily. – Use: Primary hyperlipidemia, HeFH, or ASCVD with elevated LDL-C. – Side effects: Diarrhea, abdominal pain, headache. –
Bococizumab
Bococizumab is a monoclonal antibody (mAb) that targets proprotein convertase subtilisin/kexin type 9 (PCSK9), a protein involved in low-density lipoprotein (LDL) receptor degradation. – Mechanism: Binds to PCSK9, preventing it from binding to LDL receptors, thereby increasing LDL receptor availability on the liver surface and enhancing LDL clearance from the bloodstream. – Indication: Used for the treatment of heterozygous familial hypercholesterolemia (HeFH) and clinical atherosclerotic cardiovascular disease (ASCVD) to reduce LDL cholesterol (LDL-C) levels. – Administration: Subcutaneous injection, typically administered every 2 weeks or monthly, depending on the dosing regimen. – Efficacy: Demonstrated significant reductions in LDL-C levels (up to 50–70% from baseline) in clinical trials, but its use has been limited due to concerns about immunogenicity and injection-site reactions. – Rationale: PCSK9 inhibitors like bococizumab are crucial for managing patients with refractory hypercholesterolemia or high ASCVD risk who do not achieve adequate LDL-C reduction with statins and ezetimibe.
What it is: A humanized monoclonal antibody that targets the PCSK9 protein.
How it works: By binding to and inhibiting PCSK9, it prevents the degradation of LDL receptors on liver cells, leading to more LDL being cleared from the blood.
Primary use: In clinical trials to lower LDL cholesterol and reduce the risk of major cardiovascular events in high-risk patients.
Administration: Subcutaneous injection, typically every two to four weeks.
Key considerations: Although it has shown efficacy, long-term responsiveness may be affected by the development of anti-drug antibodies
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