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Alirocumab

Medically reviewed by Drugs.com. Last updated on Jun 6, 2020.

Pronunciation

(al i ROK ue mab)

Index Terms

  • REGN727
  • SAR236553

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Auto-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.

  • Praluent

Pharmacologic Category

  • Antilipemic Agent, PCSK9 Inhibitor
  • Monoclonal Antibody

Pharmacology

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.

Distribution

IV: Vd: ~0.04 to 0.05 L/kg

Metabolism

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

Half-Life Elimination

SubQ: Steady-state: 17 to 20 days; reduced to 12 days when administered with a statin

Use: Labeled Indications

Hyperlipidemia, primary: Adjunct to diet, alone or in combination with other lipid-lowering therapies (eg, statins, ezetimibe) for the treatment of adults with primary hyperlipidemia (including heterozygous familial hypercholesterolemia [HeFH]) to reduce low-density lipoprotein cholesterol (LDL-C).

Secondary prevention of cardiovascular events: To reduce the risk of MI, stroke, and unstable angina requiring hospitalization in adults with established cardiovascular disease (Schwartz 2018).

Contraindications

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.

Dosing: Adult

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) (AHA/ACC [Grundy 2018]).

Hyperlipidemia, primary: 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 of 150 mg every 2 weeks. Note: In patients with heterozygous familial hypercholesterolemia undergoing LDL apheresis, the recommended initial dose is 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.

Dosing: Geriatric

Refer to adult dosing.

Administration

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 subcutaneous 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 areas of active skin disease or injury (eg, sunburns, skin rashes, inflammation, skin infections); do not inject into skin that is tender, 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.

Storage

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.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

>10%: Local: Injection site reaction (4% 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%)

Immunologic: Antibody development (6%; neutralizing: <1%)

Infection: Influenza (6%)

Neuromuscular & skeletal: Myalgia (4% to 6%), muscle spasm (3%)

Respiratory: Cough (3%)

Frequency not defined:

Cardiovascular: Hypersensitivity angiitis

Endocrine & metabolic: Decreased LDL cholesterol (<25 mg/dL)

<1%, postmarketing, and/or case reports: Angioedema, flu-like symptoms

Warnings/Precautions

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.

Monitoring Parameters

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.

Pregnancy Considerations

Alirocumab is a humanized monoclonal antibody (IgG1). Potential placental transfer of human IgG is dependent upon the IgG subclass and gestational age, generally increasing as pregnancy progresses. The lowest exposure would be expected during the period of organogenesis (Palmeira 2012; Pentsuk 2009).

Patient Education

What is this drug used for?

• It is used to lower cholesterol.

• It is used to lower the risk of heart attack, stroke, and a type of chest pain (unstable angina) in people with heart disease.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Stuffy nose

• Sore throat

• Injection site pain

• Itching or irritation

• Flu-like symptoms

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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