Generic Name

Bempedoic

Precaution

Hyperuricemia Inhibits renal tubular OAT2 and may increase blood uric acid levels Elevated uric acid levels usually occurred within the first 4 weeks of treatment initiation and persisted throughout treatment; elevated blood uric acid may lead to gout Tendon rupture Associated with increased risk of tendon rupture or injury Tendon rupture occurred within weeks to months of initiating May occur more frequently in patients aged ≥60 yr Discontinue immediately if tendon rupture occurs Consider discontinuing with joint pain, swelling, or inflammation

Indication

Hypercholesterolemia

Contra Indication

N/A

Dose

N/A

Side Effect

1-10% Upper respiratory tract infection (4.5%) Muscle spasms (3.6%) Hyperuricemia (3.5%) Back pain (3.3%) Abdominal pain or discomfort (3.1%) Bronchitis (3%) Pain in extremity (3%) Anemia (2.8%) Elevated liver enzymes (2.1%) Gout (1.5%) Benign prostatic hyperplasia (1.3%) Atrial fibrillation (1.7%) <1% Tendon rupture (0.5%) Next:

Pregnancy Category

Mode of Action

Adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers LDL-C by inhibiting cholesterol synthesis in the liver ACL is an enzyme upstream of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase in the cholesterol biosynthesis pathway Bempedoic acid and its active metabolite, ESP15228, require coenzyme A (CoA) activation by very long-chain acyl-CoA synthetase 1 (ACSVL1) to ETC-1002-CoA and ESP15228-CoA, respectively ACSVL1 is expressed primarily in the liver, but absent in most peripheral tissues

Interaction

Simvastatin or pravastatin Coadministration increases simvastatin or pravastatin serum concentrations and may increase simvastatin/pravastatin-related myopathy Avoid use with simvastatin doses >20 mg Avoid use with pravastatin doses >40 mg Atorvastatin and rosuvastatin: Elevations of 1.7-fold in AUC of atorvastatin, rosuvastatin, and/or their major metabolites were observed with bempedoic acid coadministration, suggesting a weak interaction; these elevations were generally within the individual statin exposures and do not affect dosing recommendations

Pregnancy Category Note

Pregnancy Discontinue bempedoic acid when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus No available data regarding use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes Note: Statins are contraindicated in pregnant women Clinical considerations Treatment of hyperlipidemia is not generally necessary during pregnancy Cholesterol and cholesterol derivatives are needed for normal fetal development Animal studies Bempedoic acid was not teratogenic in rats and rabbits when administered at doses resulting in exposures up to 11 and 12 times, respectively, the human exposures at the maximum clinical dose, based on AUC Lactation Data are not available regarding drug presence in human or animal milk, effects on breastfed infants, or effects on milk production Since bempedoic acid decreases cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, these actions may cause harm to the breastfed infant Based on the mechanism of action, advise patients that breastfeeding is not recommended during treatment

Adult Dose

Hypercholesterolemia Indicated as an adjunct to diet and maximally tolerated statin therapy for adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional lowering of low-density lipoprotein cholesterol (LDL-C) 180 mg PO qDay in combination with maximally tolerated statin therapy Hepatic impairment Mild or moderate (Child-Pugh A or B): No dosage adjustment required Severe (Child-Pugh C): Not studied

Child Dose

N/A

Renal Dose

Renal impairment Mild or moderate (eGFR ?30 mL/min/1.73 m2): No dosage adjustment required Severe (eGFR <30 mL/min/1.73 m2): Data are limited End-stage renal disease with dialysis: Not studied

Administration

May take with or without food