What is alirocumab, and how does it work (mechanism of action)?
Alirocumab is a man-made injectable drug that
reduces cholesterol levels in the blood. It is the first member of a new class
of drugs called proprotein convertase subtilisin kexin type 9 (PCSK9)
inhibitors. Cholesterol is carried in the blood to a large extent by particles
of low density lipoproteins that are removed from the blood by liver cells.
The particles are removed from the blood by low-density lipoprotein receptors
(LDLR) on liver cells. PCSK9 is a protein on liver cells that promotes the
destruction of LDLR. Therefore, a decrease in LDLR levels by PCSK9 results in
higher blood levels of LDL cholesterol.
Alirocumab is an antibody, which means that it is a protein that binds to
another protein and inactivates it. Alirocumab binds to the PCSK9 protein and
prevents it from destroying LDLR. By inhibiting PCSK9, Alirocumab increases the
number of LDLRs available to remove LDL cholesterol and consequently reduces LDL
cholesterol levels in blood. The FDA approved alirocumab in July 2015.
What brand names are available for alirocumab?
Is alirocumab available as a generic drug?
Do I need a prescription for alirocumab?
What are the side effects of alirocumab?
The most common side effects associated with alirocumab
Other side effects include
Liver problems were reported in 2.5% of patients
treated with alirocumab compared to 1.8% in patients treated with placebo.
What is the dosage for alirocumab?
The recommended starting dose of alirocumab is 75 mg via subcutaneous
injection (into the fat layer underneath the skin) every 2 weeks. If the LDL
cholesterol lowering response is not adequate with this starting dose, the
dosage may be increased to a maximum dosage of 150 mg every 2 weeks. LDL
cholesterol levels should be measured within 4 to 8 weeks of starting therapy to
assess response to treatment, and a decision should be made whether or not to
adjust the dose.
Alirocumab should only be injected by subcutaneous injection into the thigh,
abdomen, or upper arm. Injection sites should be rotated with each injection to
prevent or reduce injection site reactions and irritation. Alirocumab should not
be co-administered with other injectable drugs at the same injection site.
Which drugs or supplements interact with alirocumab?
No clinically significant drug-drug interactions are listed for alirocumab.
Is alirocumab safe to take if I’m pregnant or breastfeeding?
There is no data on the use of alirocumab in pregnant women.
It is not known if alirocumab can enter human milk or cause
harm to the nursing infant.
What else should I know about alirocumab?
What preparations of alirocumab are available?
Single dose pre-filled pens and single-dose pre-filled glass
syringes, each designed to deliver 1 ml of 75 mg/ml or 150 mg/ml.
How should I keep alirocumab stored?
Alirocumab should be stored in the refrigerator at 2 C to 8 C (36 F
to 46 F) and protected from light and extreme heat. It should not be frozen.
Medically Reviewed on 9/3/2019
FDA Prescribing Information