Table 1.
Currently available nonstatin therapy for lowering low-density lipoprotein cholesterol (LDL-C). * PCSK9: proprotein convertase subtilisin/kexin type 9; VLDL: very low-density lipoprotein; GI: gastrointestinal
| DRUG NAME | DOSAGE | MECHANISM | ROUTE | COMMON ADVERSE EFFECTS |
|---|---|---|---|---|
| Ezetimibe | 10 mg once daily | Inhibits gut absorption of cholesterol | Oral | Diarrhea, arthralgia, upper respiratory tract symptoms |
| Evolocumab Alirocumab | 140 mg every 2 weeks or 420 mg every month 75–150 mg every 2 weeks or 300 mg every month | Monoclonal antibody against PCSK9 | Subcutaneous | Nasopharyngitis, injection site reaction, flu-like symptoms |
| Colesevelam Cholestyramine Colestipol | 3.750 g once daily or 1.875 g twice daily 8–16 g per day divided into 2 doses 2–16 g per day in one or multiple doses | Binds bile acids and increases bile acid excretion | Oral | Constipation, dyspepsia, nausea |
| Niacin | 500–2000 mg once daily (extended release) | Inhibits release of free fatty acids from adipose tissue, decreases hepatic VLDL synthesis | Oral | Flushing, headache, hyperuricemia, gastritis, GI bleed, other bleeding, rhinitis |
Table 2.
Future therapies in development. ANGPTL3: angiopoietin-like 3; apo: apolipoprotein; Lp(a): lipoprotein(a); siRNA: small interfering RNA
| AGENT | MECHANISM OF ACTION | PRIMARY LIPID COMPONENT TARGET |
|---|---|---|
| Inclisiran (ALN-PCSsc) | siRNA to PCSK9 | LDL-C |
| Bempedoic acid (ETC-1002) | Inhibition of ATP citrate lyase | LDL-C |
| AKCEA-APO(a)-LRX | Antisense to apo(a) | Lp(a) |
| AKCEA-APOCIII-LRX | Antisense to apoCIII | Triglycerides |
| Evinacumab | Human monoclonal antibody to ANGPTL3 | Triglycerides and cholesterol |