New Drug Introduction: Praluent®/ alirocumab
Pharmacology
Manufacturer
Approval Date
Indications
Contraindications
Black Box Warnings
Warnings &
Precautions
Pregnancy/Lactation
Pharmacokinetics
Drug Interactions –
Precipitant drugs
Adverse Effects
(Treatment%) [Placebo%]
Monitoring Efficacy
Dosing - Initial
Dosing - Max
Renal Adjustment
Hepatic Adjustment
Praluent is a human monoclonal antibody (IgG1 isotype) that inhibits
proprotein convertase subtilisin kexin type 9 (PCSK9).
Sanofi and Regeneron Pharmaceuticals
July 24, 2015
Indicated as an adjunct to diet and maximally tolerated statin therapy for
the treatment of adults with heterozygous familial hypercholesterolemia or
clinical atherosclerotic cardiovascular disease, who require additional
lowering of LDL-C
History of serious hypersensitivity reaction to alirocumab, including
vasculitis and hypersensitivity reactions requiring hospitalization
None
 Hypersensitivity reactions (pruritus, rash, urticarial), including some
serious events, have been reported. If signs or symptoms of serious
allergic reactions occur, discontinue treatment.
 Potential for immunogenicity with alirocumab, which may lead to a higher
incidence of injection site reactions or loss of efficacy
Pregnancy Category: C
Lactation Recommendation: unknown
A – F = 85%, tmax 3-7 days. Steady state reached after 2 to 3 doses
D – Vd = 0.04-0.05 L/kg
M – Expected to degrade to small peptides and individual amino acids.
Does not affect CYP450 enzymes, PGP, or OATP.
E – T1/2: 17 to 20 days.
Statins reduce half-life of alirocumab to 12 days; not clinically meaningful
Allergic reactions (8.6%) [7.8%]
UTI (4.8%) [4.6%]
Injection site reactions (7.2%)
Diarrhea (4.7%) [4.4%]
[5.1%]
Bronchitis (4.3%) [3.8%]
Influenza (5.7%%) [4.6%]
Myalgia (4.2) [3.4%]
LDL-C levels within 4 to 8 weeks of initiating or titrating alirocumab
75 mg SC every 2 weeks
Administration:
 Warm to room temperature for 30 to 40 min prior to use. Do not keep at
room temperature for more than 24 hours.
 Inject subcutaneously into stomach, upper arm, or thighs. Injection may
take up to 20 seconds.
 Rotate injection sites.
150 mg SC every 2 weeks
No dose adjustment is needed for patients with mild or moderate renal
impairment. No data are available in patients with severe renal impairment.
No dose adjustment is needed for patients with mild or moderate hepatic
impairment. No data are available in patients with severe hepatic
impairment.
Cost: Source: NY Times – accessed 08/11/2015
Dose(s)
Brand – Generic
®
75 mg, 150 mg injection
Praluent - alirocumab
1 year
$14,600
Summary
 Praluent® (alirocumab) is the first-in-class PCSK9 inhibitor that reduces LDL-C.
 Alirocumab is indicated for the treatment of adults with heterozygous familial
hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require
additional LDL lowering despite diet and maximally tolerated statin therapy.
 Dosing of alirocumab is 75 mg or 150 mg every 2 weeks given as a subcutaneous
injection.
 The most common adverse effects observed include hypersensitivity reactions.
 LDL should be monitored at 4 to 8 weeks after initiating or titrating alirocumab.
References:
1. www.praluent.com
2. Praluent [package insert]. Bridgewater, NJ: Sanofi and Regeneron; 2015.
3. Robinson JG, Farnier M, Krempf M, et al. Efficacy and safety of alirocumab in reducing
lipids and cardiovascular events. N Engl J Med 2015; 372:1489-99.
4. Pollack A. The New York Times Website. New Drug Sharply Lowers Cholesterol, but
it’s Costly. http://www.nytimes.com/2015/07/25/business/us-approves-drug-that-cansharply-lower-cholesterol-levels.html. Published July 24, 2015. Accessed August 11,
2015.
Date Prepared: 8/11/2015
Editor: Peter G. Koval, Pharm.D., BCPS
Author: Megan Shah, Pharm.D. Candidate, UNC Eshelman School of Pharmacy