PCSK9 inhibitors
Alirocumab injection - praluent ®
Drug UPDATES: PRALUENT ®- alirocumab injection, solution
[Drug information / PDF] Click link for the latest monograph
Dosing: Click (+) next to Dosage and Administration section (drug info link)
Initial U.S. Approval: 2015
Mechanism of Action: Alirocumab is a human monoclonal antibody that binds to proprotein convertase subtilisin kexin type 9 (PCSK9). PCSK9 binds to the low-density lipoprotein receptors (LDLR) on the surface of hepatocytes to promote LDLR degradation within the liver. LDLR is the primary receptor that clears circulating LDL, therefore the decrease in LDLR levels by PCSK9 results in higher blood levels of LDL-C. By inhibiting the binding of PCSK9 to LDLR, alirocumab increases the number of LDLRs available to clear LDL, thereby lowering LDL-C levels.
INDICATIONS AND USAGE: 1.1 Primary Hyperlipidemia
PRALUENT® is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
1.2 Limitations of Use
The effect of PRALUENT on cardiovascular morbidity and mortality has not been determined.
HOW SUPPLIED:
PRALUENT is a clear, colorless to pale yellow solution available as follows:
Injection: Single-dose pre-filled pen
75 mg/mL
150 mg/mL
Injection: Single-dose pre-filled syringe
75 mg/mL
150 mg/mL
Evolocumab - repatha™ injection
Drug UPDATES: REPATHA ™- evolocumab injection, solution [Drug information / PDF] Click link for the latest monograph Dosing: Click (+) next to Dosage and Administration section (drug info link) Initial U.S. Approval: 2015 Mechanism of Action: Evolocumab is a human monoclonal IgG2 directed against human proprotein convertase subtilisin kexin 9 (PCSK9). Evolocumab binds to PCSK9 and inhibits circulating PCSK9 from binding to the low density lipoprotein (LDL) receptor (LDLR), preventing PCSK9-mediated LDLR degradation and permitting LDLR to recycle back to the liver cell surface. By inhibiting the binding of PCSK9 to LDLR, evolocumab increases the number of LDLRs available to clear LDL from the blood, thereby lowering LDL-C levels. INDICATIONS AND USAGE: 1.2 Homozygous Familial Hypercholesterolemia 1.3 Limitations of Use HOW SUPPLIED: |
Reference(s)
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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