Dosing & Uses
Dosage Forms & Strengths
subcutaneous injection
- 200mg/mL
Homozygous Familial Hypercholesterolemia
Indicated as an adjunct to lipid-lowering medications and diet to reduce LDL-C, apoB, TC, and non-HDL-C in patients with homozygous familial hypercholesterolemia (HoFH)
200 mg SC once weekly
Dosage Modifications
Elevated transaminases
- ≥3x and <5x ULN: Confirm by repeating measurement within 1 week; if confirmed withhold dosing
- ≥5x ULN: Withhold dosing
- Obtain additional liver-related tests if not already measured (eg, total bilirubin, alkaline phosphatase, INR) and investigate to identify the probable cause
- Recommendations are based on ULN of ~ 30-40 IU/L
- If transaminase elevations accompanied by clinical symptoms of liver injury (eg, nausea, vomiting, abdominal pain, fever, jaundice, lethargy, flu-like symptoms), increases in bilirubin ≥2x ULN, or active liver disease, discontinue treatment and investigate to identify the probable cause
- If resuming mipomersen after transaminases resolve to <3x ULN consider monitoring liver-related tests more frequently
Dosing Considerations
Measure baseline transaminases (ALT, AST), alkaline phosphatase, and total bilirubin
Safety and effectiveness not been established in patients with hypercholesterolemia who do not have HoFH
Effect on cardiovascular morbidity and mortality undetermined
Safety and effectiveness of mipomersen as an adjunct to LDL apheresis have not been established; therefore, the use as an adjunct to LDL apheresis is not recommended
Monitor lipid levels at least q3months during the first year of treatment to determine if the LDL-C reduction achieved is sufficiently robust to warrant the potential risk of liver toxicity; maximal LDL-C reduction observed after ~6 months
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (98)
- acarbose
mipomersen, acarbose. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- acetaminophen
mipomersen, acetaminophen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- acetaminophen IV
mipomersen, acetaminophen IV. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- acetaminophen rectal
mipomersen, acetaminophen rectal. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- allopurinol
mipomersen, allopurinol. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- amiodarone
mipomersen, amiodarone. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- amitriptyline
mipomersen, amitriptyline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- atazanavir
mipomersen, atazanavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- atorvastatin
mipomersen increases toxicity of atorvastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- azathioprine
mipomersen, azathioprine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- baclofen
mipomersen, baclofen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- bupropion
mipomersen, bupropion. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- captopril
mipomersen, captopril. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- carbamazepine
mipomersen, carbamazepine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- celecoxib
mipomersen, celecoxib. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- chlorpromazine
mipomersen, chlorpromazine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- clavulanate
mipomersen, clavulanate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- clindamycin
mipomersen, clindamycin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- clopidogrel
mipomersen, clopidogrel. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- cyproheptadine
mipomersen, cyproheptadine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- darunavir
mipomersen, darunavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- demeclocycline
mipomersen, demeclocycline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- diclofenac
mipomersen, diclofenac. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- doxycycline
mipomersen, doxycycline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- enalapril
mipomersen, enalapril. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- erythromycin base
mipomersen, erythromycin base. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- erythromycin ethylsuccinate
mipomersen, erythromycin ethylsuccinate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- erythromycin lactobionate
mipomersen, erythromycin lactobionate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- erythromycin stearate
mipomersen, erythromycin stearate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- etodolac
mipomersen, etodolac. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- fenoprofen
mipomersen, fenoprofen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- fluconazole
mipomersen, fluconazole. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- fluoxetine
mipomersen, fluoxetine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- fluvastatin
mipomersen increases toxicity of fluvastatin by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs; OATP1B1 inhibitors may increase risk of myopathy.
- fosamprenavir
mipomersen, fosamprenavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- fosphenytoin
mipomersen, fosphenytoin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- glimepiride
mipomersen, glimepiride. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- glipizide
mipomersen, glipizide. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- glyburide
mipomersen, glyburide. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- heparin
mipomersen, heparin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- hydralazine
mipomersen, hydralazine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- ibuprofen
mipomersen, ibuprofen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- ibuprofen IV
mipomersen, ibuprofen IV. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- indinavir
mipomersen, indinavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- indomethacin
mipomersen, indomethacin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- isoniazid
mipomersen, isoniazid. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- isotretinoin
mipomersen, isotretinoin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- itraconazole
mipomersen, itraconazole. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- ketoconazole
mipomersen, ketoconazole. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- ketoprofen
mipomersen, ketoprofen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- ketorolac
mipomersen, ketorolac. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- labetalol
mipomersen, labetalol. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- levoketoconazole
mipomersen, levoketoconazole. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- lisinopril
mipomersen, lisinopril. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- lopinavir
mipomersen, lopinavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- losartan
mipomersen, losartan. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- lovastatin
mipomersen, lovastatin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- meclofenamate
mipomersen, meclofenamate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- meloxicam
mipomersen, meloxicam. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- methotrexate
mipomersen, methotrexate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- methyldopa
mipomersen, methyldopa. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- minocycline
mipomersen, minocycline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- mirtazapine
mipomersen, mirtazapine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- nabumetone
mipomersen, nabumetone. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- naproxen
mipomersen, naproxen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- nelfinavir
mipomersen, nelfinavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- niacin
mipomersen, niacin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- nitrofurantoin
mipomersen, nitrofurantoin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- paroxetine
mipomersen, paroxetine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- phenobarbital
mipomersen, phenobarbital. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- phenytoin
mipomersen, phenytoin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- pioglitazone
mipomersen, pioglitazone. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- piroxicam
mipomersen, piroxicam. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- pitavastatin
mipomersen increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs; OATP1B1 inhibitors may increase risk of myopathy.
- pravastatin
mipomersen increases toxicity of pravastatin by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs; OATP1B1 inhibitors may increase risk of myopathy.
- procainamide
mipomersen, procainamide. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- pyrazinamide
mipomersen, pyrazinamide. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- rifampin
mipomersen, rifampin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- risperidone
mipomersen, risperidone. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- ritonavir
mipomersen, ritonavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- rosuvastatin
mipomersen increases toxicity of rosuvastatin by Other (see comment). Use Caution/Monitor.
- salsalate
mipomersen, salsalate. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- saquinavir
mipomersen, saquinavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- sertraline
mipomersen, sertraline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- simvastatin
mipomersen, simvastatin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- sulfamethoxazole
mipomersen, sulfamethoxazole. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- sulindac
mipomersen, sulindac. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- tamoxifen
mipomersen, tamoxifen. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- testosterone
mipomersen, testosterone. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- testosterone buccal system
mipomersen, testosterone buccal system. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- testosterone topical
mipomersen, testosterone topical. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- tetracycline
mipomersen, tetracycline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- tigecycline
mipomersen, tigecycline. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- tipranavir
mipomersen, tipranavir. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- trazodone
mipomersen, trazodone. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- valproic acid
mipomersen, valproic acid. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- verapamil
mipomersen, verapamil. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- vitamin A
mipomersen, vitamin A. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
Minor (0)
Adverse Effects
>10%
Injection site reactions (84%)
Increased hepatic fat >5% (62%)
Fatigue (15%)
Nausea (14%)
Influenza-like illness (13%)
Headache (12%)
1-10%
ALT increased (10%)
Pyrexia (8%)
Hypertension (7%)
Hepatic steatosis (7%)
Extremity pain (7%)
AST increased (6%)
Chills (6%)
Abnormal LFTs (5%)
Edema (5%)
Musculoskeletal pain (4%)
Vomiting (4%)
Angina (4%)
Hepatic enzyme increased (3%)
Abdominal pain (3%)
Palpitations (3%)
Insomnia (3%)
Postmarketing Reports
Idiopathic thrombocytopenic purpura
Warnings
Black Box Warnings
In the clinical trial, 4 of 34 (12%) patients treated with mipomersen had at least 1 elevation in ALT ≥3x ULN compared with 0% of the 17 patients treated with placebo
Measure ALT, AST, alkaline phosphatase, and total bilirubin before initiating treatment and then ALT, AST regularly as recommended
During treatment, withhold dosing if ALT or AST are ≥3 x ULN
Discontinue clinically significant liver toxicity
Increases hepatic steatosis with or without concomitant increases in transaminases
Hepatic steatosis associated with therapy; may be a risk factor for progressive liver disease, including steatohepatitis and cirrhosis
Because of risk of hepatotoxicity, therapy is available only through a restricted REMS program; should only be prescribed to patients with a clinical or laboratory diagnosis consistent with HoFH; safety and efficacy in patients with hypercholesterolemia who do not have HoFH not established
Contraindications
Hypersensitivity
Moderate-to-severe hepatic impairment (Child-Pugh B or C) or active liver disease, including unexplained persistent increased serum transaminases
Cautions
May cause elevations in transaminases and hepatic steatosis (see Black Box Warnings, Dosage Modifications); concern exists that these increases could induce steatohepatitis, which can progress to cirrhosis over several years
Infection site reactions reported
Women of reproductive potential should use effective contraception during mipomersen therapy
Not recommended with severe renal impairment, clinically significant proteinuria, or on renal dialysis (lack of clinical data)
Site reactions, including erythema, pain, tenderness, pruritus and local swelling reported
Flu-like symptoms, occurring within 2 days after injection reported; symptoms may include influenza-like illness, pyrexia, chills, myalgia, arthralgia, malaise or fatigue
Generalized hypersensitivity (eg, angioedema, urticaria, generalized rash) reported; if hypersensitivity occurs, instruct patient to promptly seek medical advice regarding discontinuation
Pregnancy & Lactation
Pregnancy Category: B
Lactation: Unknown whether distributed in breast milk
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Antisense oligonucleotide inhibitor that targets messenger RNA for apolipoprotein B-100, the principal apolipoprotein of LDL and its metabolic precursor, VLDL
Absorption
Bioavailability: 54-78%
Peak plasma time: 3-4 hr
Distribution
Protein bound: ≥90%
Distribution half-life: 2-5 hr
Steady-state typically reached within 6 months
Metabolism
Metabolized in tissues by endonucleases to form shorter oligonucleotides that are then substrates for additional metabolism by exonucleases
Elimination
Half-life: 1-2 months
Excretion: <4% urine over 24 hr
Administration
SC Preparation
Allowed drug to reach room temperature for at least 30 minutes before administering
Do not use if solution is cloudy or contains visible particulate matter
SC Administration
For subcutaneous use only; do not administer IM or IV
Administer on the same day each week; if a dose is missed, the injection should be given at least 3 days from the next weekly dose
Inject SC into abdomen, thigh region, or outer area of the upper arm
Do not inject in areas of active skin disease or injury (eg, sunburns, skin rashes, inflammation, skin infections, active areas of psoriasis)
Avoid areas of tattooed skin and scarring
Storage
Vials or syringes: Store refrigerated between 2-8°C (36-46°F)
