mipomersen (Discontinued)

Brand and Other Names:Kynamro
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and mipomersen

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

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            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (97)

                • 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.

                • 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)

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                  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

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                  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

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                  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.

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                  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

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                  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)

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                  Images

                  No images available for this drug.
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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.