Bemvas

• Approved Indications:
• As an adjunct to diet and maximally tolerated statin therapy to reduce low-density lipoprotein cholesterol (LDL-C) in adults with:
• Established atherosclerotic cardiovascular disease (ASCVD).
• Heterozygous familial hypercholesterolemia (HeFH).
• For adults who require additional LDL-C lowering when statins are not tolerated or contraindicated.
• Off-label Uses:
• Occasionally used off-label as part of combination lipid-lowering therapy in patients with mixed dyslipidemia.

• Route: Oral.
• Adult Dose: 180 mg once daily, taken orally with or without food.
• Pediatrics: Safety and efficacy not established; not recommended.
• Elderly: No dose adjustment necessary; monitor for tolerability.
• Renal Impairment: No dose adjustment required for mild to moderate impairment; caution in severe impairment due to limited data.
• Hepatic Impairment: Not recommended in patients with severe hepatic impairment; use caution in mild to moderate cases.
• Administration Notes:
• Take at the same time daily.
• Continue adherence to diet and lifestyle modifications.

Bempedoic acid is a prodrug activated in the liver to its Coenzyme A (CoA) form. It selectively inhibits ATP citrate lyase (ACL), an enzyme upstream of HMG-CoA reductase in the cholesterol biosynthesis pathway. By inhibiting ACL, it reduces cholesterol synthesis in the liver, leading to upregulation of LDL receptors and increased clearance of LDL cholesterol from the bloodstream, resulting in lower plasma LDL-C levels. Because activation occurs primarily in the liver and not in skeletal muscle, bempedoic acid may have a lower risk of muscle-related side effects compared to statins.

• Absorption: Peak plasma concentration approximately 3.5 hours post-dose.
• Distribution: Highly protein bound (>99%).
• Metabolism: Converted in the liver to active CoA form; undergoes glucuronidation primarily via UGT2B7.
• Elimination: Excreted mainly via urine and feces as metabolites and unchanged drug.
• Half-life: Approximately 21 hours, supporting once-daily dosing.

• Pregnancy: No adequate controlled studies in pregnant women; animal studies showed no direct fetal harm. Use only if clearly needed after risk-benefit assessment.
• Lactation: It is unknown whether bempedoic acid is excreted in human milk. Breastfeeding is generally not recommended during treatment.

• Primary Therapeutic Class: Lipid-lowering agent
• Subclass: ATP citrate lyase inhibitor

• Known hypersensitivity to bempedoic acid or any excipients.
• Active liver disease or unexplained persistent elevations in hepatic transaminases.
• Pregnancy and lactation unless benefits clearly outweigh risks.

• Monitor liver function tests before initiation and periodically thereafter; discontinue if significant transaminase elevations occur.
• Use caution in patients with a history of tendon disorders; rare cases of tendon rupture reported.
• May increase serum uric acid levels; monitor in patients with gout or hyperuricemia.
• Use cautiously in severe renal impairment due to limited data.
• Assess for muscle-related symptoms, especially when used with statins.

• Common:
• Upper respiratory tract infections
• Muscle spasms
• Hyperuricemia
• Abdominal pain
• Constipation
• Bronchitis
• Serious but Rare:
• Tendon rupture
• Elevated liver enzymes
• Hypersensitivity reactions including rash and angioedema
• Myopathy

• May increase plasma concentrations of statins by inhibiting OATP1B1 and OATP1B3 transporters, increasing risk of myopathy.
• Avoid concomitant use with strong inhibitors of OATP1B1 (e.g., cyclosporine).
• No significant interactions via CYP450 enzymes.
• No known significant interactions with food or alcohol.

• Bempedoic acid is recognized in lipid management guidelines as an add-on therapy for patients inadequately controlled on maximally tolerated statins or statin-intolerant patients.
• FDA has approved fixed-dose combination tablets with ezetimibe for enhanced LDL-C reduction.
• Ongoing studies are assessing cardiovascular outcomes and long-term safety.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep the container tightly closed.
• Do not freeze.
• Keep out of reach of children.