- ACRONYMS AND DEFINITIONS
- CVD - Cardiovascular disease
- HeFH - Heterozygous familial hypercholesterolemia
- HoFH - Homozygous familial hypercholesterolemia
- PCSK9 - Proprotein convertase subtilisin kexin type 9
- PCSK9 INHIBITORS
Alirocumab (Praluent®)
Dosage forms
Single-dose prefilled pens
- 75 mg/ml
- 150 mg/ml
- Comes in pack of 1 or 2 pens
Single-dose prefilled syringes
- 75 mg/ml
- 150 mg/ml
- Comes in pack of 1 or 2 syringes
Dosing
Adults with established CVD or with primary hyperlipidemia including HeFH
- Starting: 75 mg every 2 weeks OR 300 mg every 4 weeks
- Maintenance: 75 - 150 mg every 2 weeks OR 300 mg every 4 weeks
- Max: 150 mg every 2 weeks OR 300 mg every 4 weeks
- May administer without regard to food
Adults with HeFH undergoing LDL apheresis or in adults with HoFH
- Dosing: 150 mg every 2 weeks
- May be administered without regard to the timing of LDL apheresis
Missed doses
- If an every-2-week dose is missed, administer the injection within 7 days from the missed dose and resume the original schedule. If the missed dose is not administered within 7 days, wait until the next dose on the original schedule.
- If an every-4-week dose is missed, administer the injection within 7 days from the missed dose and resume the original schedule. If the missed dose is not administered within 7 days, administer the dose, starting a new schedule based on this date.
Other
- Allow syringe to warm to room temperature for 30 - 40 minutes before injecting
- Inject subcutaneously into thigh, abdomen, or upper arm. Rotate injection sites.
- Recheck LDL 4 - 8 weeks after starting therapy and after dose changes. For patients receiving 300 mg every 4 weeks, check LDL just prior to the next scheduled dose since LDL levels can vary widely on this dosing regimen.
- To administer the 300 mg dose, give two 150 mg injections consecutively at two different injection sites
- Do not expose to direct sunlight
- Do not shake syringes or pens
Generic / Price
- NO/$$$$Storage
- Store unused pens in a refrigerator
- If needed, Praluent may be kept at room temperature up to 77°F (25°C) for a maximum of 30 days in original carton to protect from light
Evolocumab (Repatha®)
Dosage forms
Single-use prefilled syringe
- 140 mg/ml
- Comes in pack of one syringe
Single-use prefilled autoinjector
- 140 mg/ml
- Comes in packs of 1, 2, or 3 injectors
Single-use on-body infuser (Pushtronex® System)
- 420 mg/3.5 ml
- Infuses drug subcutaneously over 5 minutes
Dosing
Established CVD or primary hyperlipidemia (adults)
- Dosing: 140 mg every 2 weeks OR 420 mg once monthly
- If switching dosage regimens, administer the first dose of the new regimen on the next scheduled date of the prior regimen
- The LDL-lowering effect of evolocumab may be measured as early as 4 weeks after initiation. LDL can vary during the dosing interval in some patients; recommend measuring LDL just prior to the next scheduled dose.
HeFH in pediatric patients aged 10 years and older
- Dosing: 140 mg every 2 weeks OR 420 mg once monthly
- If switching dosage regimens, administer the first dose of the new regimen on the next scheduled date of the prior regimen
- The LDL-lowering effect of evolocumab may be measured as early as 4 weeks after initiation. LDL can vary during the dosing interval in some patients; recommend measuring LDL just prior to the next scheduled dose.
HoFH in pediatric patients aged 10 years and older and adults
- Starting: 420 mg once monthly
- The dosage can be increased to 420 mg every 2 weeks if a clinically meaningful response is not achieved in 12 weeks
- Patients on lipid apheresis may initiate treatment with 420 mg every 2 weeks to correspond with their apheresis schedule. Administer evolocumab after the apheresis session is complete.
- The LDL-lowering effect of evolocumab may be measured as early as 4 weeks after initiation. LDL can vary during the dosing interval in some patients; recommend measuring LDL just prior to the next scheduled dose.
Missed doses
- Still within 7 days of the missed dose
- Administer evolocumab and resume original schedule
- More than 7 days after missed dose
- Every 2-week dosing - wait until the next dose on the original schedule
- Once monthly dosing - administer the dose and start a new schedule based on this date
Other
- Dose is given by subcutaneous injection in the abdomen, thigh, or upper arm
- Dose may be given without regard to food
- To administer the 420 mg dose, give 3 injections consecutively within 30 minutes or use the on-body infuser. Choose a different injection site with each injection.
- Prior to use, allow to warm to room temperature for at least 30 minutes for the autoinjector or syringe and for at least 45 minutes for the on-body infusor
- Do not expose to direct sunlight
- Do not shake syringes or injectors
Generic / Price
- NO/$$$$Storage
- Store in refrigerator
- May be kept at room temperature for a maximum of 30 days
- Do not expose to temperatures above 25°C (77°F)
- Kidney disease dosing
- Alirocumab (Praluent®)
- CrCl ≥ 30 ml/min: no dose adjustment necessary
- CrCl < 30 ml/min: has not been studied
- Evolocumab (Repatha®)
- No dose adjustment necessary in renal impairment
- Liver disease dosing
- Alirocumab (Praluent®)
- Mild-moderate (Child-Pugh A and B): no dose adjustment necessary
- Severe (Child-Pugh C): has not been studied
- Evolocumab (Repatha®)
- Mild-moderate (Child-Pugh A and B): no dose adjustment necessary
- Severe (Child-Pugh C): has not been studied
- DRUG INTERACTIONS
- NOTE: Drug interactions presented here are NOT all-inclusive. Other interactions may exist. The interactions presented here are meant to encompass commonly prescribed medications and/or interactions that are well-documented. Always consult your physician or pharmacist before taking medications concurrently. CLICK HERE for more information on drug interactions.
- Alirocumab and Evolocumab
- No significant drug interactions are known
- Metabolism and elimination
- PCSK9 inhibitors are proteins, and they are metabolized through proteolytic pathways to smaller peptides and individual amino acids
- PCSK9 inhibitors do not undergo liver metabolism
- PRICE ($) INFO / ASSISTANCE
Pricing legend
- $ = 0 - $50
- $$ = $51 - $100
- $$$ = $101 - $150
- $$$$ = > $150
- Pricing based on one month of therapy at standard dosing in an adult
- Pricing based on information from GoodRX.com®
- Pricing may vary by region and availability
Patient Assistance Programs for PCSK9 inhibitors | ||||
---|---|---|---|---|
Drug | Manufacturer | Ships to | PAP info | Application |
Alirocumab (Praluent®) | Regeneron | Patient or pharmacy | Link | Link |
Evolocumab (Repatha®) | Amgen | Patient | Link | Link |
- BIBLIOGRAPHY
- Manufacturer's package insert