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:
1.1 Primary Hyperlipidemia
REPATHA™ is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease (CVD), who require additional lowering of low density lipoprotein cholesterol (LDL-C).

1.2 Homozygous Familial Hypercholesterolemia
REPATHA is indicated as an adjunct to diet and other LDL-lowering therapies (e.g., statins, ezetimibe, LDL apheresis) for the treatment of patients with homozygous familial hypercholesterolemia (HoFH) who require additional lowering of LDL-C.

1.3 Limitations of Use
The effect of REPATHA on cardiovascular morbidity and mortality has not been determined.

HOW SUPPLIED:
REPATHA is a sterile, clear to opalescent, colorless to pale yellow solution available as follows:
Injection: 140 mg/mL solution in a single-use prefilled syringe
Injection: 140 mg/mL solution in a single-use prefilled SureClick® autoinjector

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates. A local search option of this data can be found here.