Medically reviewed by Drugs.com. Last updated on Apr 12, 2019.
(al i ROK ue mab)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution Pen-injector, Subcutaneous [preservative free]:
Praluent: 75 mg/mL (1 mL); 150 mg/mL (1 mL) [contains mouse (murine) and/or hamster protein]
Solution Prefilled Syringe, Subcutaneous [preservative free]:
Praluent: 75 mg/mL (1 mL [DSC]); 150 mg/mL (1 mL [DSC]) [contains mouse (murine) and/or hamster protein]
Brand Names: U.S.
- Antilipemic Agent, PCSK9 Inhibitor
- Monoclonal Antibody
Alirocumab is a human monoclonal antibody (IgG1isotype) that binds to proprotein convertase subtilisin kexin type 9 (PCSK9). PCSK9 binds to the low-density lipoprotein receptors (LDLR) on hepatocyte surfaces 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.
IV: Vd: ~0.04 to 0.05 L/kg
Expected to undergo proteolysis and be degraded to small peptides and amino acids
Onset of Action
Peak effect: Proprotein convertase subtilisin kexin type 9 (PCSK9) suppression: 4 to 8 hours
Time to Peak
SubQ: 3 to 7 days
SubQ: Steady-state: 17 to 20 days; reduced to 12 days when administered with a statin
Use: Labeled Indications
Hyperlipidemia, primary: Adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Off Label Uses
Secondary prevention of cardiovascular events after acute coronary syndrome
Data from a multicenter, randomized, double-blind, placebo-controlled trial of patients with a recent acute coronary syndrome (ACS) support the addition of alirocumab to high-intensity statin therapy to reduce subsequent cardiovascular events (death from coronary heart disease, nonfatal myocardial infarction, fatal or nonfatal stroke, or unstable angina requiring hospitalization). Patients were eligible for this trial if ACS events occurred within 1 to 12 months and LDL cholesterol was ≥70 mg/dL, non-HDL cholesterol was ≥100 mg/dL, or apolipoprotein B was ≥80 mg/dL despite maximum tolerated statin therapy prior to randomization [Schwartz 2018].
Serious hypersensitivity to alirocumab or any component of the formulation.
Documentation of allergenic cross-reactivity for PCSK9 inhibitors is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Note: Use may be considered in patients who do not meet cholesterol treatment goals with dietary modification and other lipid-lowering therapies (eg, maximally tolerated statin with or without ezetimibe) (AHA/ACC [Grundy 2018]).
Hyperlipidemia, primary: SubQ: Initial: 75 mg every 2 weeks or 300 mg every 4 weeks; for both regimens, if an adequate LDL-C response is not achieved, may increase or modify dosing regimen to a maximum of 150 mg every 2 weeks. Note: In patients with heterozygous familial hypercholesterolemia undergoing LDL apheresis, the recommended initial dose is 150 mg every 2 weeks.
Secondary prevention of cardiovascular events after acute coronary syndrome (off-label use) (alternative agent): SubQ: 75 mg every 2 weeks; may increase to a maximum dose of 150 mg every 2 weeks; titrate as needed to maintain a goal LDL cholesterol of 25 to 50 mg/dL (Schwartz 2014; Schwartz 2018).
Switching regimens: When switching from the monthly regimen to an every-2-week regimen, start the new dose on the next scheduled dosing date; reassess LDL-C 4 to 8 weeks after dosing change.
Missed dose: If a dose is missed ≤7 days from the usual day of administration, administer the dose as soon as possible and then resume the original schedule; otherwise, if beyond 7 days, skip the missed dose and resume the normal dosing schedule, or if dosage is monthly, start a new schedule based on this date.
Refer to adult dosing.
SubQ: Allow solution to come to room temperature for 30 to 40 minutes prior to administration. Do not shake. Administer by subcutaneous injection into the thigh, abdomen, or upper arm; rotate injection site with each injection. For the 300 mg dose, administer two 150 mg injections consecutively at two different injection sites. Do not inject into areas of active skin disease or injury (eg, sunburns, skin rashes, inflammation, skin infections). Do not coadminister with other injectable drugs at the same injection site. For patients undergoing LDL apheresis, may be administered without regard to the timing of apheresis.
Store at 2°C to 8°C (36°F to 46°F) in the outer carton to protect from light. If needed, solution may be kept at room temperature up to 25°C (77°F) for a maximum of 30 days in original carton to protect from light. Do not store >25°C (>77°F). After removal from the refrigerator, solution must be used within 30 days or discarded. Do not freeze. Do not expose to extreme heat. Do not shake.
Belimumab: Monoclonal Antibodies may enhance the adverse/toxic effect of Belimumab. Avoid combination
>10%: Local: Injection site reaction (7% to 17%)
1% to 10%:
Gastrointestinal: Diarrhea (5%)
Hematologic & oncologic: Bruise (2%)
Hepatic: Liver enzyme disorder (3%), increased serum transaminases (>3 x ULN: 2%)
Hypersensitivity: Hypersensitivity reaction (9%; including hypersensitivity angiitis, pruritus, severe hypersensitivity, skin rash, urticaria)
Immunologic: Antibody development (2% to 5%; neutralizing: 1% [loss of efficacy: <1%])
Infection: Influenza (6%)
Neuromuscular & skeletal: Myalgia (4%), muscle spasm (3%)
Respiratory: Cough (3%)
Frequency not defined: Endocrine & metabolic: Decreased LDL cholesterol (<25 mg/dL)
<1%, postmarketing, and/or case reports: Flu-like symptoms
Concerns related to adverse effects:
• Hypersensitivity reactions: Hypersensitivity reactions, including some severe reactions requiring hospitalization (eg, hypersensitivity vasculitis), have been reported. Discontinue treatment and initiate supportive treatment in patients who develop serious allergic reaction. Other hypersensitivity reactions, including pruritus, rash, and urticaria, have been reported.
Lipid profile (fasting or nonfasting) before initiating treatment. Fasting lipid profile should be rechecked 4 to 12 weeks after starting therapy and every 3 to 12 months thereafter (AHA/ACC [Grundy 2018]). For patients receiving 300 mg every 4 weeks, measure LDL-C just prior to the next scheduled dose (LDL-C varies considerably between doses with this regimen). Monitor for hypersensitivity reactions.
Adverse events were not observed in animal reproduction studies. Information specific to alirocumab in pregnancy is not available. However, IgG molecules are known to cross the placenta, with increasing amounts during the second and third trimesters of pregnancy. Health care providers are encouraged to enroll women exposed to alirocumab during pregnancy in the MotherToBaby Pregnancy Studies by contacting the Organization of Teratology Information Specialists (OTIS) (877-311-8972) or https://mothertobaby.org/ongoing-study/praluent/alirocumab/.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience rhinitis, pharyngitis, injection site pain, itching or irritation, or flu-like symptoms (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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More about alirocumab
Other brands: Praluent