What is Brinsupri?
Brinsupri (bempedoic acid/ezetimibe) is a once-daily, fixed-dose combination medication approved for the treatment of adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional lowering of LDL cholesterol when maximally tolerated statin therapy is not sufficient.
Mechanism of Action
Brinsupri combines two lipid-lowering agents with complementary mechanisms of action:
Bempedoic acid: An adenosine triphosphate-citrate lyase (ACL) inhibitor that reduces cholesterol synthesis in the liver by inhibiting an enzyme upstream from HMG-CoA reductase (the target of statins)
Ezetimibe: Inhibits absorption of cholesterol at the brush border of the small intestine, reducing delivery of intestinal cholesterol to the liver
Clinical Use
Brinsupri is indicated for:
- Adults with heterozygous familial hypercholesterolemia (HeFH)
- Adults with established atherosclerotic cardiovascular disease (ASCVD)
- Patients who require additional LDL-C lowering despite maximally tolerated statin therapy
Dosing
- Standard dose: One tablet daily (containing bempedoic acid 180 mg and ezetimibe 10 mg)
- Can be taken with or without food
- No dosage adjustment required for renal impairment
Efficacy
- Provides approximately 38% LDL-C reduction when added to maximally tolerated statin therapy
- Dual mechanism targets both cholesterol production and absorption
- More effective than either component alone
Safety and Adverse Effects
Common side effects include:
- Elevated liver enzymes
- Muscle-related symptoms (less frequent than with statins)
- Upper respiratory tract infections
- Back pain
- Abdominal pain
- Hyperuricemia
Important Considerations
- Not a replacement for statins - intended for use in addition to maximally tolerated statin therapy
- Contraindicated in pregnancy
- Should be used with caution in patients with significant hepatic impairment
- Drug interactions similar to those of ezetimibe component
Clinical Pearls
- Unlike statins, bempedoic acid is a prodrug that requires activation by an enzyme (very long-chain acyl-CoA synthetase-1) that is not present in skeletal muscle, potentially reducing muscle-related side effects
- Provides an additional option for patients who cannot tolerate high-intensity statin therapy
- Can be used as part of a comprehensive approach to cardiovascular risk reduction
Note: Brinsupri should be considered within the context of comprehensive cardiovascular risk management, including lifestyle modifications and other lipid-lowering therapies as appropriate.