alirocumab (Rx)

Brand and Other Names:Praluent
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

SC injection

  • 75mg/mL
  • 150mg/mL

Hyperlipidemia Treatment and/or CV Risk Reduction

Indications

  • Primary hyperlipidemia (including heterozygous familial hypercholesterolemia)
    • Indicated as an adjunct to diet, alone or in combination with other lipid-lowering therapies (eg, statins, ezetimibe), for treatment of adults with primary hyperlipidemia to reduce low-density lipoprotein cholesterol (LDL-C
  • Prevention of cardiovascular events
    • Indicated to reduce the risk of MI, stroke, and unstable angina requiring hospitalization in adults with established cardiovascular disease

Every 2 week schedule

  • Recommended starting dose: 75 mg SC q2Weeks
  • Measure CLC-C levels within 4-8 week of initiating; if inadequate response, may increase to 150 mg SC q2Weeks; reassess LDL-C within 4-8 weeks
  • Not to exceed 150 mg SC q2Weeks

Every 4 week schedule

  • Recommended starting dose: 300 mg SC q4Weeks (ie, two 150-mg injections consecutively at 2 different injection sites)
  • Measure LDL-C just prior to the next scheduled dose; if inadequate response, may adjust dose to 150 mg q2Weeks, starting the new dose on the next scheduled dosing date; reassess LDL-C within 4-8 weeks

Patients with HeFH undergoing apheresis

  • 150 mg SC q2Weeks
  • May be administered without regard to timing of apheresis

Dosage Modifications

Renal impairment

  • Mild or moderate: No dose adjustment required
  • Severe: Not studied

Hepatic impairment

  • Mild or moderate: No dose adjustment required
  • Severe: Not studied

Dosing Considerations

Limitation of use: Effect on cardiovascular morbidity and mortality not determined

Homozygous Familial Hypercholesterolemia (Orphan)

Orphan designation for treatment of homozygous familial hypercholesterolemia

Sponsor

  • Sanofi-Aventis US, LLC; 55 Corporate Drive; Bridgewater, New Jersey 08807

Safety and efficacy not established

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Adverse Effects

1-10%

Allergic reactions (8.6%)

Injection site reactions (7.2%)

Influenza (5.7%)

Antidrug antibodies (4.8%)

Myalgia (4.2%)

Muscle spasms (3.1%)

Contusion (2.1%)

Musculoskeletal pain (2.1%)

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Warnings

Contraindications

History of serious hypersensitivity reaction to alirocumab; reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization

Cautions

Hypersensitivity reactions (eg, pruritus, rash, urticaria), including some serious events (eg, hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization), have been reported; discontinue and treat if signs or symptoms of serious allergic reactions occur

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Pregnancy

Pregnancy

No available data on use in pregnant women; pregnancy exposure registry (1-877-311-8972 or https://mothertobaby.org/ongoing-study/praluent/) monitors pregnancy outcomes in women exposed to drug during pregnancy

Animal studies

  • Studies in rats have not shown effects on embryo-fetal development when given during organogenesis up to 12-fold the human exposure
  • In monkeys, suppression of the humoral immune response was observed in infant monkeys when alirocumab was dosed during organogenesis to parturition at dose exposures 13-fold the exposure at the maximum recommended human dose of 150 mg q2wk

Lactation

Unknown if distributed in human breast milk

The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed infant

Human IgG is present in human milk, but published data suggest that breastmilk IgG antibodies do not enter the neonatal and infant circulation in substantial amounts

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

more...
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Pharmacology

Mechanism of Action

Monoclonal antibody that binds to PCSK9 (proprotein convertase subtilisin/kexin type 9)

LDL-C is cleared from the circulation preferentially through the LDL receptor (LDLR) pathway

PCSK9 is a serine protease that destroys LDLR in the liver, resulting in decreased LDL-C clearance and increased plasma LDL-C

PCSK9 inhibitors decrease LDLR degradation by PCSK9, and thereby improve LDL-C clearance and lower plasma LDL-C

Absorption

Absolute bioavailability: 85%

Peak plasma time: 3-7 days

Distribution

Vd: 0.04-0.05 L/kg

Distributed primarily in circulatory system

Metabolism

Specific metabolism studies were not conducted because alirocumab is a protein and is expected to degrade to small peptides and individual amino acids

Does not affect P450 enzymes, P-gp, and OATP

Elimination

Half-life: 17-20 days

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Administration

SC Preparation

Provide proper training to patients and/or caregivers on preparation and administration prior to use

Allow prefilled syringe or pen to warm to room temperature for 30-40 minutes prior injection; administer as soon as possible after it has warmed up

Do not use if it has been at room temperature [77°F (25°C)] for ≥24 hr

Visually inspect for particulate matter and discoloration before administration; discard if the solution is discolored or contains visible particulate matter

Follow aseptic injection technique for every administration time

SC Administration

Administer by SC injection into the thigh, abdomen, or upper arm using a single-dose prefilled pen or syringe

Rotate the injection site with each injection

Do not inject into areas of active skin disease or injury (eg, sunburns, rashes, inflammation, infections)

Do not coadminister with other injectable drugs at the same injection site

Missed dose

  • Every 2 week dose
    • Administer the injection within 7 days from the missed dose and then resume the original schedule
    • If the missed dose is not administered within 7 days, instruct the patient to wait until the next dose on the original schedule
  • Every 4 week dose
    • Administer the injection within 7 days from the missed dose and then resume the original schedule
    • If the missed dose is not administered within 7 days, instruct the patient to administer the dose, starting a new 4-week schedule based on this date

Storage

Refrigerate at 36-46°F (2-8°C) in the outer carton in order to protect from light

If needed, may store up to 30 days at room temperature not exceeding 77°F (25°C) in original container

Do not freeze

Do not expose to extreme heat

Do not shake

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.