Praluent Pen (alirocumab)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Alirocumab, a fully human IgG1 monoclonal antibody that binds to proprotein convertase subtilisin kexin type 9 (PCSK9), is an antilipemic agent.
Alirocumab, a fully human IgG1 monoclonal antibody produced by recombinant DNA technology in Chinese hamster ovary cells, is an inhibitor of human proprotein convertase subtilisin kexin type 9 (PCSK9). PCSK9 is a serine protease that is produced principally in the liver. The major function of PCSK9 is to regulate the metabolism of low-density lipoprotein (LDL) cholesterol by promoting the degradation of LDL receptors, the primary receptors responsible for clearing circulating LDL cholesterol.
PCSK9 binds to the LDL receptor on the surface of hepatocytes and directs it towards lysosomal degradation; this causes a reduction in the amount of LDL receptors available to bind and remove LDL particles from circulation, and consequently, increases plasma LDL-cholesterol concentrations. Alirocumab binds specifically and with high affinity to PCSK9, preventing the binding of PCSK9 to the LDL-cholesterol receptor and thereby increasing the number of receptors available to clear LDL cholesterol. Reductions in lipoprotein (a), apolipoprotein B, and other lipid fractions also have been demonstrated with alirocumab therapy.
Familial hypercholesterolemia is a group of inherited disorders characterized by excessive elevations in LDL-cholesterol concentrations and early atherosclerotic disease. In most cases, the condition is caused by mutations in the LDL-receptor gene, but mutations in other genes, including the gene encoding apolipoprotein B and PCSK9, also can cause the condition.
Alirocumab reduces circulating PCSK9 in a concentration-dependent manner. Following a single subcutaneous injection of the drug (75 or 150 mg), maximal suppression of free PCSK9 occurs within 4-8 hours and returns to baseline once drug concentrations fall below the limit of quantification. In healthy individuals who received a single subcutaneous injection of alirocumab 75 mg, maximal reduction of LDL-cholesterol concentration occurred 15 days after the dose.
Alirocumab exhibits nonlinear pharmacokinetics with slightly greater than dose-proportional increases in plasma concentrations with increasing doses. Following subcutaneous administration, absolute bioavailability of alirocumab is approximately 85% and peak plasma concentrations are attained within 3-7 days. Monthly dose-normalized exposure of alirocumab was similar between patients receiving a dosage of 300 mg every 4 weeks and a dosage of 150 mg every 2 weeks.
Steady-state concentrations are achieved after 2-3 doses with an accumulation ratio up to a maximum of approximately twofold in adults. In pediatric patients, steady state concentrations were reached in <=8 weeks with the recommended dosage regimen. Although specific drug metabolism studies have not been conducted, alirocumab is expected to be degraded into small peptides and individual amino acids.
Elimination of alirocumab is concentration-dependent; at low concentrations, elimination occurs principally through saturable binding to the PCSK9 target, while at higher concentrations, elimination occurs principally through a non-saturable proteolytic pathway. The median apparent half-life of alirocumab is 17-20 days.
USES: Alirocumab is used by people who have blockage in the heart blood vessels to reduce the risk of heart attack, stroke, and certain types of chest pain that require treatment in a hospital. It is also used by people who have an inherited condition that causes high levels of LDL. Treatment with alirocumab, a proper diet, and cholesterol-lowering drugs can help lower "bad" cholesterol (LDL) in the blood.
Alirocumab belongs to a class of drugs known as monoclonal antibodies. It works by improving how well your body gets rid of LDL cholesterol. In addition to eating a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking.
Consult your doctor for more details.
Generic name: alirocumab
Pronunciation: (AL-i-ROK-ue-mab)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Praluent Pen:
- Atherosclerotic Cardiovascular Disease
- Heterozygous Familial Hypercholesterolemia
- Homozygous Familial Hypercholesterolemia
- Hypercholesterolemia
Also known as: Atherosclerosis, Atherosclerotic Vascular Disease, Cardiovascular Disease Related To Atherosclerosis, Elevated Blood Cholesterol Level, Familial Heterozygous Hypercholesterolemia, Familial Homozygous Hypercholesterolemia, Heterozygous Familial Elevated Blood Cholesterol.
Dosing
No dosing information is available for this tab.
Administer alirocumab by subcutaneous injection.
Train patients and/or their caregivers on how to prepare and administer alirocumab using the prefilled injection pen provided by the manufacturer. Alirocumab should be administered by or under the supervision of an adult in children 12 to 17 years of age; it should be administered by a caregiver in children 8 to 11 years of age.
Prior to use, the prefilled pens should be stored at 2-8degreesC in their original carton to protect from light; the drug should not be frozen, shaken, or exposed to extreme heat or direct sunlight. Prior to administration, alirocumab should be allowed to warm to room temperature for 30-40 minutes; the drug should not be returned to the refrigerator after removal and should be used within 30 days or discarded.
Alirocumab injection is a clear, colorless to pale yellow solution. The solution should be inspected visually prior to administration and should not be used if discolored, cloudy, or contains any particles. Commercially available alirocumab injection contains no preservatives and is intended for single use only.
Subcutaneous injections of alirocumab should be administered into areas of the thigh, abdomen (except for the 2-inch area around the navel), or upper arm that are not tender, bruised, red, or indurated; injection sites should be rotated. Injection of alirocumab may take up to 20 seconds to complete.
To administer a 300-mg dose of alirocumab, administer 2 consecutive doses of 150 mg at 2 different injection sites.
If a dose of alirocumab is missed, the dose should be administered as soon as possible within 7 days. If a missed dose is not administered within 7 days in a patient receiving the every-2-week regimen, the dose should be withheld and the next dose should be administered at the regularly scheduled time. If a missed dose is not administered within 7 days in a patient receiving the once-monthly regimen, the dose should be administered and a new dosing schedule should be initiated starting on that date.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*History of serious hypersensitivity reaction to alirocumab or any of its excipients.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in >5% of patients receiving alirocumab and more frequently than placebo in primary hyperlipidemia studies include injection site reactions and influenza.
Adverse effects reported in >5% of patients receiving alirocumab and more frequently than placebo in patients with established cardiovascular disease include myalgia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of alirocumab as an adjunct to diet and other LDL-lowering therapies for the treatment of HeFH were established in pediatric patients >=8 years of age based on data from a 24-week, randomized, placebo-controlled, double-blind trial involving 153 pediatric patients with HeFH and evidence from controlled trials in adults.
Available data from clinical trials and post-marketing reports are insufficient to determine the drug-related risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes of alirocumab use during pregnancy. Monoclonal antibodies cross the placenta in increasing amounts closer to term; therefore, placental transfer of alirocumab can occur from the mother to the developing fetus.
In animal reproductive studies, no adverse embryofetal effects were observed in rats exposed to alirocumab during the period of organogenesis; however, in utero exposure to the drug appeared to suppress the humoral immune response in infant monkeys. Alirocumab was administered at dose exposures of 12-13 times the maximum recommended human dosage in these animal studies.
To monitor pregnancy outcomes in pregnant women exposed to alirocumab, a pregnancy safety study is being conducted. Clinicians and patients should call 1-844-734-6643 to report alirocumab exposure during pregnancy.
It is not known whether alirocumab is distributed into human milk; the effects of alirocumab on the breastfed infant or on milk production are also unknown. Human IgG is distributed into human milk; however, published data suggest that IgG antibodies present in human milk are not substantially distributed into the circulation of neonates and infants. The potential adverse effects of alirocumab on the infant should be weighed against the known benefits of breastfeeding, taking into account the importance of the drug to the woman.
No specific dosage recommendations in geriatric patients.
Controlled studies involving alirocumab included 3663 patients >=65 years of age and 734 patients >=75 years of age. Although no overall differences in safety or efficacy have been observed between geriatric patients and younger adults in controlled studies or in other clinical experience, the possibility of increased sensitivity to alirocumab in some geriatric patients cannot be ruled out.
ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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