Version October 2024
Heterozygous familial hypercholesterolemia (HeFH) : Note: Should be used as adjunct to diet and other low-density lipoprotein cholesterol (LDL-C) lowering therapy.
Children ≥8 years and Adolescents:
Weight <50 kg: Initial: SUBQ: 150 mg every 4 weeks; if response inadequate, adjust dose to 75 mg every 2 weeks; in clinical trials, LDL-C was assessed after 2 doses (week 8) and dose adjusted to biweekly regimen if LDL-C ≥110 mg/dL beginning on week 12 (Ref).
Weight ≥50 kg: Initial: SUBQ: 300 mg every 4 weeks; if response inadequate, adjust dose to 150 mg every 2 weeks; in clinical trials, LDL-C was assessed after 2 doses (week 8) and dose adjusted to biweekly regimen if LDL-C ≥110 mg/dL beginning on week 12 (Ref).
Homozygous familial hypercholesterolemia (HoFH): Limited data available: Note: Should be used as adjunct to diet and other low-density lipoprotein cholesterol (LDL-C) lowering therapy.
Children ≥8 years and Adolescents: Note: In the trial, doses were not titrated to response; however, after week 12, doses could be adjusted based on changes in weight (50 kg cut-off) (Ref).
Weight <50 kg: Initial: SUBQ: 75 mg every 2 weeks.
Weight ≥50 kg: Initial: SUBQ: 150 mg every 2 weeks.
Dosing based on a multinational, phase 3, open-label trial including 18 patients (age range: 8 to 17 years) who had inadequate response to optimal doses of statin therapy with or without other lipid-modifying therapies (if statin intolerant). Results showed a decrease in LDL-C compared to baseline; an LDL-C reduction ≥15% was observed in approximately 50% of subjects (Ref).
Children ≥8 years and Adolescents: SUBQ:
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, dosage adjustment is unlikely to be required as monoclonal antibodies are not known to be renally eliminated.
Children ≥8 years and Adolescents: SUBQ:
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
(For additional information see "Alirocumab: Drug information")
Note: Use may be considered in patients who do not meet cholesterol treatment goals with dietary modification and other lipid-lowering therapies (ie, maximally tolerated statin plus ezetimibe) (Ref).
Homozygous familial hypercholesterolemia: SUBQ: 150 mg once every 2 weeks.
Hyperlipidemia, primary: SUBQ: Initial: 75 mg once every 2 weeks or 300 mg once every 4 weeks; for both regimens, if an adequate low-density lipoprotein cholesterol (LDL-C) response is not achieved, may increase or modify dosing regimen to a maximum of 150 mg every 2 weeks.
Heterozygous familial hypercholesterolemia undergoing LDL apheresis: SUBQ: 150 mg once every 2 weeks.
Secondary prevention of cardiovascular events: SUBQ: Initial: 75 mg once every 2 weeks or 300 mg once every 4 weeks; for both regimens, if an adequate LDL-C response is not achieved, may increase or modify dosing regimen to a maximum dose of 150 mg every 2 weeks.
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.
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, dosage adjustment is unlikely to be required as monoclonal antibodies are not known to be renally eliminated.
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults unless otherwise indicated.
>10%: Local: Injection-site reaction (children, adolescents, and adults: 4% to 17%; including erythema at injection site, injection-site pruritus, pain at injection site, swelling at injection site, tenderness at injection site)
1% to 10%:
Gastrointestinal: Diarrhea (5%)
Hepatic: Increased serum transaminases (>3 × ULN: 2%), liver enzyme disorder (3%)
Hypersensitivity: Hypersensitivity reaction (9%; including hypersensitivity angiitis, nummular eczema)
Immunologic: Antibody development (children and adolescents: 3%; adults: 6%; neutralizing: <1%)
Infection: Influenza (6%)
Neuromuscular & skeletal: Muscle spasm (3%), myalgia (4% to 6%)
Postmarketing:
Hypersensitivity: Angioedema
Respiratory: Flu-like symptoms
Serious hypersensitivity to alirocumab or any component of the formulation.
Concerns related to adverse effects:
• Hypersensitivity reactions: Hypersensitivity reactions, including some severe reactions requiring hospitalization (eg, hypersensitivity vasculitis, angioedema), 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.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution Auto-injector, Subcutaneous:
Praluent: 75 mg/mL (1 mL); 150 mg/mL (1 mL) [contains mouse (murine) and/or hamster protein]
Solution Auto-injector, Subcutaneous [preservative free]:
Praluent: 75 mg/mL (1 mL [DSC]); 150 mg/mL (1 mL [DSC]) [contains mouse (murine) and/or hamster protein]
No
Solution Auto-injector (Praluent Subcutaneous)
75 mg/mL (per mL): $303.89
150 mg/mL (per mL): $303.89
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution Auto-injector, Subcutaneous:
Praluent: 75 mg/mL (1 mL); 150 mg/mL (1 mL) [contains mouse (murine) and/or hamster protein]
Solution Prefilled Syringe, Subcutaneous:
Praluent: 75 mg/mL ([DSC]); 150 mg/mL ([DSC]) [contains mouse (murine) and/or hamster protein]
Only available via specialty pharmacies. Call 844-772-5836 or visit https://www.praluenthcp.com for additional information.
Note: In patients 8 to 11 years of age, doses should be administered by the caregiver; pediatric patients ≥12 years of age may self-administer doses after adequate training under adult supervision.
Parenteral: SUBQ: Allow pen/autoinjector to come to room temperature (30 to 40 minutes); do not warm in any other way. Do not shake.
Administer by SUBQ injection into the thigh, abdomen (avoiding the 2-inch area around the navel), or upper arm. Do not inject into skin that is tender, bruised, hard, red hot or damaged, or has visible veins, scars, or stretch marks. Do not coadminister with other injectable drugs at the same injection site. Pinch the skin to make the injection site firm in children <12 years; pinching of the skin may also be necessary in older pediatric patients to make the injection site firm. Injection may take up to 20 seconds for full dose to be injected.
Rotate injection site with each injection; for the 300 mg dose, administer two 150 mg injections consecutively at 2 different injection sites. Do not reuse prefilled pens/syringes. Do not administer if window on pen/syringe is solid yellow (indicates pen/syringe has been used). Do not use prefilled syringe if blue cap is missing or loose, if it has been dropped, or if damaged; avoid touching yellow safety cover. Based on experience in adults undergoing low-density lipoprotein apheresis, alirocumab may be administered without regard to the timing of apheresis.
Missed doses:
Every-2-week dosing: If the dose is within 7 days from the patient's original schedule, administer the dose and resume the original schedule. If it has been >7 days, wait until the next dose on the original schedule.
Every-4-week dosing: If the dose is within 7 days from the patient's original schedule, administer the dose and resume the original schedule. If it has been >7 days, administer the dose and start a new 4-week schedule based on the new dose.
SUBQ: Allow solution to come to room temperature for 30 to 40 minutes prior to administration; do not warm in any other way. Do not shake. Administer by SUBQ injection into the thigh, abdomen (avoiding the 2-inch area around the navel), or upper arm; rotate injection site with each injection; may take up to 20 seconds for full dose to be injected. For the 300 mg dose, administer two 150 mg injections consecutively at 2 different injection sites. Do not inject into skin that is tender, bruised, hard, red hot or damaged, or has visible veins, scars, or stretch marks. Do not coadminister with other injectable drugs at the same injection site. Do not reuse prefilled pens/syringes; single use only. Do not administer if window on pen/syringe is solid yellow (indicates pen/syringe has been used). Do not use prefilled syringe if blue cap is missing or loose, if it has been dropped, or if damaged; avoid touching yellow safety cover. 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.
Adjunct to diet and other low-density lipoprotein cholesterol (LDL-C) lowering therapies in pediatric patients with heterozygous familial hypercholesterolemia (HeFH) to reduce LDL-C (FDA approved in pediatric patients ≥8 years); adjunct to other LDL-C lowering therapies in patients with homozygous familial hypercholesterolemia (HoFH) to reduce LDL-C (FDA approved in adults); adjunct to diet, alone or in combination with other LDL-C lowering therapies, in patients with primary hyperlipidemia (including HeFH) to reduce LDL-C (FDA approved in adults); reduce the risk of myocardial infarction, stroke, and unstable angina requiring hospitalization in patients with established cardiovascular disease (FDA approved in adults).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program
Efgartigimod Alfa: May diminish the therapeutic effect of Fc Receptor-Binding Agents. Risk C: Monitor therapy
Rozanolixizumab: May diminish the therapeutic effect of Fc Receptor-Binding Agents. Risk C: Monitor therapy
Alirocumab is a humanized monoclonal antibody (IgG1). Human IgG crosses the placenta. Fetal exposure is dependent upon the IgG subclass, maternal serum concentrations, placental integrity, newborn birth weight, and GA, generally increasing as pregnancy progresses. The lowest exposure would be expected during the period of organogenesis and the highest during the third trimester (Clements 2020; Palmeira 2012; Pentsuk 2009).
Outcome data following maternal use of alirocumab during pregnancy are limited (Vuignier 2021).
Data collection to monitor pregnancy and infant outcomes following exposure to alirocumab is ongoing. Health care providers are encouraged to report exposures of alirocumab during pregnancy (1-844-734-6643).
Lipid profile (baseline [fasting or nonfasting]; 4 to 12 weeks after initiation, every 3 to 12 months). Monitor for hypersensitivity reactions.
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.
Note: Pharmacokinetics in pediatric patients (age range: 8 to 17 years) were similar to adults.
Onset: Peak effect: Proprotein convertase subtilisin kexin type 9 (PCSK9) suppression: 4 to 8 hours.
Distribution: IV: Vd: ~0.04 to 0.05 L/kg.
Metabolism: Expected to undergo proteolysis and be degraded to small peptides and amino acids.
Bioavailability: SUBQ: ~85%.
Half-life elimination: SUBQ: Steady-state: 17 to 20 days; reduced to 12 days when administered with a statin.
Time to peak: SUBQ: 3 to 7 days.
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