Alirocumab

Alirocumab is a human monoclonal antibody that binds to proprotein convertase subtilisin kexin type 9 (PCSK9). PCSK9 binds to the low-density lipoprotein (LDL) receptors (LDLR) on the surface of hepatocytes to promote LDLR degradation within the liver.

• PRALUENT ® is indicated: To reduce the risk of major adverse cardiovascular (CV) events (coronary heart disease death, myocardial infarction, stroke, or unstable angina requiring hospitalization) in adults at increased risk for these events . As an adjunct to diet and exercise to reduce low- density lipoprotein cholesterol (LDL-C) in: adults with hypercholesterolemia.ICD-10: E78.00, I20.9, I21.9, I63.9

• PRALUENT is contraindicated in patients with a history of a serious hypersensitivity reaction to alirocumab or any of the excipients in PRALUENT. Hypersensitivity vasculitis, angioedema, and hypersensitivity reactions requiring hospitalization have occurred [see Warnings and Precautions (5.1) ].contraindicated

In adults with hypercholesterolemia, including HeFH ( 2.1 ): The recommended starting dosage of PRALUENT is either 75 mg once every 2 weeks or 300 mg once every 4 weeks administered subcutaneously. For patients receiving PRALUENT 300 mg every 4 weeks, measure LDL-C just prior to the next scheduled dosage, because LDL-C can vary between dosages in some patients. If the LDL-C response is inadequate, the dosage may be adjusted 150 mg subcutaneously every 2 weeks. In adults with HeFH undergoing LDL apheresis or in adults with HoFH ( 2.1 ): The recommended dosage of PRALUENT is 150 mg once every 2 weeks administered subcutaneously. PRALUENT can be administered without regard to the timing of LDL apheresis. In pediatric patients with HeFH ( 2.2 ): The recommended dosage of PRALUENT for patients with a body weight less than 50 kg is 150 mg once every 4 weeks administered subcutaneously. The recommended dosage of PRALUENT for patients with a body weight of 50 kg or more is 300 mg once every 4 weeks administered subcutaneously. If the LDL-C response is inadequate, the dosage may be adjusted for patients with a body weight less than 50 kg to 75 mg subcutaneously once every 2 weeks or for patients with a body weight of 50 kg or more to 150 mg subcutaneously once every 2 weeks. Assess LDL-C when clinically appropriate. The LDL-lowering effect of PRALUENT may be measured as early as 4 weeks after initiation. ( 2.1 ) Administer PRALUENT subcutaneously into areas of the thigh, abdomen, or upper arm that are not tender, bruised, red, or indurated.

Hypersensitivity reactions: hypersensitivity vasculitis, angioedema, and other hypersensitivity reactions requiring hospitalization, have been reported with PRALUENT treatment. If signs or symptoms of serious hypersensitivity reactions occur, discontinue treatment with PRALUENT, treat according to the standard of care, and monitor until signs and symptoms resolve. ( 5.1 ) 5.1 Hypersensitivity Reactions Hypersensitivity reactions, including hypersensitivity vasculitis, angioedema, and other hypersensitivity reactions requiring hospitalization, have been reported with PRALUENT treatment. If signs or symptoms of serious hypersensitivity reactions occur, discontinue treatment with PRALUENT, treat according to the standard of care, and monitor until signs and symptoms resolve. PRALUENT is contraindicated in patients with a history of a serious hypersensitivity reaction to alirocumab or any excipient in PRALUENT [see Contraindications (4) ] .

The following adverse reactions are also discussed in the other sections of the labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.1) ] Common (>5% of patients treated with PRALUENT and more frequently than placebo) adverse reactions in adults with: Primary hypercholesterolemia : injection site reactions, and influenza. ( 6 ) Established CV disease: myalgia. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Regeneron at 1-844-734-6643 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse Reactions in Adults with Hypercholesterolemia The data in Table 1 are derived from 9 primary hypercholesterolemia placebo-controlled trials that included 2,476 adult patients treated with PRALUENT 75 mg and/or 150 mg every 2 weeks, including 2,135 exposed for 6 months and 1,999 exposed for more than 1 year (median treatment duration of 65 weeks). The mean age of the population was 59 years, 40% of the population were female, 90% were White, 4% were Black or African American, 3% were Asian, and 3% other races; 6% identified as Hispanic or Latino ethnicity. Adverse reactions reported in at least 2% of PRALUENT-treated patients, and more frequently than in placebo-treated patients, are shown in Table 1.

8.1 Pregnancy Risk Summary Available data from clinical trials and postmarketing reports on PRALUENT use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes. In animal reproduction studies, there were no effects on embryo-fetal development when rats were subcutaneously administered alirocumab during organogenesis at dose exposures up to 12-fold the exposure at the maximum recommended human dose of 150 mg every two weeks. 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 every two weeks. No additional effects on pregnancy or neonatal/infant development were observed at dose exposures up to 81-fold the maximum recommended human dose of 150 mg every two weeks. Measurable alirocumab serum concentrations were observed in the infant monkeys at birth at comparable levels to maternal serum, indicating that alirocumab, like other IgG antibodies, crosses the placental barrier. Monoclonal antibodies are transported across the placenta in increasing amounts especially near term; therefore, alirocumab has the potential to be transmitted from the mother to the developing fetus.

Metabolism

Absorption After subcutaneous administration of 75 mg to 300 mg alirocumab, median times to maximum serum concentrations (t max ) were 3-7 days. The pharmacokinetics of alirocumab after single subcutaneous administration of 75 mg into the abdomen, upper arm, or thigh were similar.

• Jul 24, 2015BLABLA125559Regeneron Pharmaceuticals

1. 1Myalgia1,6676.8%
2. 2Product Dose Omission1,3645.5%
3. 3Injection Site Pain1,2865.2%
4. 4Muscle Spasms1,1684.7%
5. 5Arthralgia1,0624.3%
6. 6Fatigue1,0234.2%
7. 7Pain9523.9%
8. 8Pain In Extremity9393.8%
9. 9Product Dose Omission Issue9113.7%
10. 10Injection Site Bruising8483.4%
11. 11Headache8053.3%
12. 12Influenza Like Illness8033.3%
13. 13Diarrhoea8013.3%
14. 14Device Issue7883.2%
15. 15Cough7082.9%

The 10 most recently updated of 115 ClinicalTrials.gov registrations naming Alirocumab as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to See How Safe and Effective Alirocumab is When Given Weekly to Adult Participants Who Have Hypercholesterolemia
  Recruiting · Phase 2 · Interventional · 420 enrolled · Regeneron Pharmaceuticals
  NCT07477704updated 2026-06-10
• Dual PCSK9 Inhibition With Inclisiran and Alirocumab in Secondary Prevention
  Recruiting · Phase 4 · Interventional · 60 enrolled · University Medical Centre Ljubljana
  NCT07581808updated 2026-06-02
• Alirocumab and Ischemic Risk in Atherosclerotic Cardiovascular Disease (ASCVD)
  Active not recruiting · Observational · 2,214 enrolled · Sanofi
  NCT07615179updated 2026-05-29
• Low-Density Lipoprotein Cholesterol Reduction With Alirocumab 150 mg Versus Inclisiran in Individuals Initiating Therapy in Routine Clinical Practice
  Active not recruiting · Observational · 124 enrolled · Sanofi
  NCT07615166updated 2026-05-29
• Alirocumab for Stabilisation of Symptomatic Vulnerable Carotid Plaque
  Not yet recruiting · Phase 3 · Interventional · 280 enrolled · Middle East North Africa Stroke and Interventional Neurotherapies Organization
  NCT07586540updated 2026-05-14
• Safety, Tolerability, and Bioeffects of Alirocumab in Non-treatment Seeking Heavy Drinkers
  Recruiting · Phase 1 · Interventional · 100 enrolled · National Institute on Alcohol Abuse and Alcoholism (NIAAA)
  NCT04781322updated 2026-04-28
• A Real-World Study of Long-Term Adherence and Persistence to Inclisiran, Evolocumab, and Alirocumab
  Not yet recruiting · Observational · 5,995 enrolled · Novartis Pharmaceuticals
  NCT07543731updated 2026-04-22
• PCSK9 Inhibitor and PD-1 Inhibitor in Patients With Metastatic, Refractory To Prior Anti PD-1 Non-small Cell Lung
  Active not recruiting · Phase 2 · Interventional · 60 enrolled · Duke University
  NCT05553834updated 2026-04-13
• Cholesterol Disruption in Combination With the Standard of Care in Patients With Advanced Pancreatic Adenocarcinoma
  Active not recruiting · Early phase 1 · Interventional · 3 enrolled · CHU de Quebec-Universite Laval
  NCT04862260updated 2026-03-19
• Cardiac Allograft Vasculopathy Inhibition With Alirocumab
  Completed · Phase 2 · Interventional · 114 enrolled · Stanford University
  NCT03537742updated 2026-03-17

Frequently asked questions

How does Alirocumab work?

Alirocumab is a human monoclonal antibody that binds to proprotein convertase subtilisin kexin type 9 (PCSK9). PCSK9 binds to the low-density lipoprotein (LDL) receptors (LDLR) on the surface of hepatocytes to promote LDLR degradation within the liver.

What is Alirocumab used for?

According to FDA labeling, Alirocumab carries indications including: PRALUENT ® is indicated: To reduce the risk of major adverse cardiovascular (CV) events (coronary heart disease death, myocardial infarction, stroke, or unstable angina requiring hospitalization) in adults at increased risk for these events . As an adjunct to diet and exercise to reduce low- density lipoprotein cholesterol (LDL-C) in: adults with hypercholesterolemia.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Alirocumab?

Alirocumab is classified as Other lipid modifying agents, PCSK9 Inhibitor, PCSK9 Inhibitors, Increased Lipolysis.

What are the brand names for Alirocumab?

Alirocumab is marketed under brand names including Praluent.

What are the contraindications for Alirocumab?

Alirocumab labeling lists contraindications including: PRALUENT is contraindicated in patients with a history of a serious hypersensitivity reaction to alirocumab or any of the excipients in PRALUENT. Hypersensitivity vasculitis, angioedema, and hypersensitivity reactions requiring hospitalization have occurred [see Warnings and Precautions (5.1) ].. Always consult the full prescribing information and a clinician.