This site is intended for UK healthcare professionals
Medscape UK Univadis Logo
Medscape UK Univadis Logo

Lomitapide oral

Updated 2 Feb 2023 | Other lipid-regulating drugs


Oral formulations of lomitapide.

Drugs List

  • LOJUXTA 10mg capsules
  • LOJUXTA 20mg capsules
  • LOJUXTA 5mg capsules
  • lomitapide 10mg capsules
  • lomitapide 20mg capsules
  • lomitapide 5mg capsules
  • Therapeutic Indications


    Homozygous familial hypercholesterolaemia: Adjunct to diet

    Lomitapide is indicated as an adjunct to a low-fat diet and other lipid-lowering medicinal products with or without low density lipoprotein (LDL) apheresis in adult patients with homozygous familial hypercholesterolaemia (HoFH).


    Genetic confirmation of HoFH should be obtained whenever possible. Other forms of primary hyperlipoproteinaemia and secondary causes of hypercholesterolaemia (e.g. nephrotic syndrome, hypothyroidism) must be excluded.


    Initial dose: 5mg once daily. After 2 weeks the dose may be increased, based on acceptable safety and tolerability, to 10mg and then, at a minimum of 4 week intervals, to 20mg, 40mg, and to the maximum recommended dose of 60mg once daily.

    The dose should be escalated gradually to minimise the incidence and severity of gastrointestinal side effects and aminotransferase elevations.

    Patients with Renal Impairment

    Patients with end stage renal disease receiving dialysis should not exceed 40mg daily.

    Patients with Hepatic Impairment

    Patients with mild hepatic impairment (Child-Pugh A) should not exceed 40mg daily.

    Additional Dosage Information

    Lomitapide should be taken on an empty stomach, at least 2 hours after the evening meal because the fat content of a recent meal may adversely impact gastrointestinal tolerability.
    Patients should follow a diet supplying less than 20% of energy from fat prior to initiating lomitapide treatment. A low-fat diet should continue during treatment. Dietary counselling should be provided.
    The manufacturer states that concurrent use with a moderate or strong CYP3A4 inhibitor is contraindicated. Patients receiving any other weak CYP3A4 inhibitor and a stable maintenance dose of lomitapide should space the dose of the medications by 12 hours.

    For patients on a stable dose of lomitapide who receive atorvastatin either:

    Separate the dose of the medications by 12 hours.
    Decrease the dose of lomitapide by half.
    Patients on 5mg should remain on 5mg.

    Careful titration may then be considered according to LDL-C response and safety/tolerability.

    Dose adjustment and monitoring for patients with elevated aminotransferases

    ALT or AST of 3 to less than 5 times ULN
    Confirm elevation with a repeat measurement within one week.
    If confirmed, reduce the dose and obtain additional liver-related tests if not already measured.
    Repeat tests weekly and withhold dosing if there are signs of abnormal liver function, if aminotransferase levels rise above 5x ULN, or if aminotransferase levels do not fall below 3x ULN within approximately 4 weeks. Refer patients with persistent elevations in aminotransferase greater than 3x ULN to a hepatologist for further investigation.
    If resuming lomitapide after aminotransferase levels resolve to less than less than 3x ULN, consider reducing the dose and monitor liver-related tests more frequently.

    ALT or AST of 5 or more times ULN
    Withhold dosing and obtain additional liver-related tests if not already measured. If aminotransferase levels do not fall below 3x ULN within approximately 4 weeks refer the patient to a hepatologist for further investigation.
    If resuming lomitapide after aminotransferase levels resolve to less than 3x ULN, reduce the dose and monitor liver-related tests more frequently.

    Clinical symptoms of hepatic injury
    If aminotransferase elevations are accompanied by clinical symptoms of liver injury, increases in bilirubin greater than 2x ULN, or active liver disease, discontinue treatment with lomitapide and refer the patient to a hepatologist for further investigation.
    Reintroduction of treatment may be considered if the benefits outweigh the risks associated with potential liver disease.


    Children under 18 years
    Elevated serum transaminases - greater than 5 times upper limit of normal
    Abnormal liver function test
    Chronic inflammatory bowel disease
    Moderate hepatic impairment
    Severe inflammatory bowel disease

    Precautions and Warnings

    Females of childbearing potential
    Patients over 65 years
    Glucose-galactose malabsorption syndrome
    Lactose intolerance
    Mild hepatic impairment
    Severe renal impairment

    Advise ability to drive/operate machinery may be affected by side effects
    Exclude other causes of hyperlipoproteinaemia
    Treatment to be initiated and supervised by a specialist
    Contains lactose
    Reduce dose if ALT or AST 3-5 x ULN, on repeat test
    Exclude pregnancy prior to initiation of treatment
    Perform liver function tests before commencing therapy
    After 1st year of therapy monitor LFTs 3 monthly or before dose increase
    During 1st year of therapy perform LFTs monthly or before dose increase
    Monitor for steatohepatitis/fibrosis at baseline and annually
    Advise patient of potential risk of dehydration
    Advise patient to seek advice at first indications of pregnancy
    Discontinue if bilirubin > 2 x ULN and refer to hepatologist
    Interrupt treatment if ALT or AST > 5 x ULN
    Pregnancy confirmed: Advise patient to discontinue and consult doctor
    Discontinue if active liver disease occurs and refer to hepatologist
    Careful dose titration may minimise incidence of side effects
    Advise patient not to take St John's wort concurrently
    Advise patient peppermint oil products may increase plasma level
    Advise patient to avoid alcohol during treatment
    Advise patient Seville (sour) orange products may increase plasma level
    Advise patient that blueberry products may increase plasma level
    Advise patient that cranberry products may increase plasma level
    Advise patient to avoid grapefruit products
    Dietary restrictions should be maintained
    Female: Ensure adequate contraception during treatment
    Advise patient how to prevent dehydration
    Advise patient to take vitamin E and saturated fatty acid supplements
    Take once daily at least 2 hours after last meal of the day

    Perform liver function tests prior to commencing treatment. If the baseline liver-related tests are abnormal, consider initiating the medicinal product after appropriate investigation by a hepatologist and the baseline abnormalities are explained or resolved.

    Regular screening for steatohepatitis/fibrosis should be performed at baseline and on an annual basis using the following imaging and biomarker evaluations:
    Imaging for tissue elasticity (e.g. fibroscan, acoustic radiation force impulse or magnetic resonance elastography).
    Gamma-GT and serum albumin to detect possible liver injury.

    At least one marker from each of the following categories:
    High sensitivity C-reactive protein (hs-CRP), erythrocyte sedimentation rate, CK-18 fragment, NASH test.
    Enhanced liver fibrosis (ELF) panel, fibrometer, AST/ALT ratio, Fib-4 score, Fibrotest.

    The performance of these tests and their interpretation should involve collaboration between the treating physician and the hepatologist. Patients with results suggesting the presence of steatohepatitis or fibrosis should be considered for liver biopsy.

    If a patient has biopsy-proven steatohepatitis or fibrosis, the risk/benefit ratio should be reassessed and treatment stopped if necessary.

    Caution should be exercised when lomitapide is used with other medicinal products known to have potential for hepatotoxicity.

    Prescribe daily supplements that contain 400 units of vitamin E and at least 200mg linoleic acid, 210mg alpha linolenic acid, 110mg eicosapentaenoic acid, and 80mg docosahexaenoic acid.

    Pregnancy and Lactation


    Lomitapide is contraindicated during pregnancy.
    The manufacturer contraindicates use of lomitapide during pregnancy. Animal studies have shown developmental toxicity (teratogenicity, embryotoxicity). As there is limited published information regarding use in human pregnancy the risks are unknown.


    Lomitapide is contraindicated during breastfeeding.
    The manufacturer advises that the patient either discontinues lomitapide or discontinues breastfeeding. The presence of lomitapide in human breast milk is unknown and therefore the effects on exposed infants are also unknown.

    Side Effects

    Abdominal discomfort
    Abdominal distension
    Abdominal pain
    Abnormal INR
    Abnormal liver function tests
    Alanine aminotransferase increased
    Aspartate aminotransferase increased
    Carotene decreased
    Chest pain
    Decreased appetite
    Disturbances of appetite
    Dry mouth
    Dry skin
    Early satiety
    Epigastric discomfort
    Erythematous rash
    Eye swelling
    Faecal urgency
    Gait abnormality
    Gamma glutamyl transferase (GGT) increased
    Gastric dilatation
    Gastric disorders
    Gastro-intestinal haemorrhage
    Gastro-intestinal infection
    Gastroesophageal reflux disease
    Haemorrhoidal haemorrhage
    Hard faeces
    Hepatic steatosis
    Increase in alkaline phosphatase
    Increase in serum transaminases
    Increased bowel action
    Joint swelling
    Muscle spasm
    Muscle twitch
    Neutrophil percentage increased
    Painful extremities
    Pharyngeal lesion
    Prothrombin time increased
    Pulmonary function test abnormal
    Reduced neutrophil count
    Reduced plasma potassium levels
    Serum bilirubin increased
    Upper-airway cough syndrome
    Vitamin E decreased
    Vitamin K decreased
    Weight loss
    White blood cell count decreased
    White blood cell count raised


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: May 2019.

    Reference Sources

    Summary of Product Characteristics: Lojuxta hard capsules. Aegerion Pharmaceuticals Ltd. Revised August 2019.

    The Renal Drug Handbook. Fourth Edition (2014) ed. Ashley, C and Dunleavy, A, Radcliffe Publishing Ltd, London.

    NICE Evidence Services Available at: Last accessed: 22 May 2019.

    US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
    Available at:
    Lomitapide Last revised: 03 December 2018
    Last accessed: 22 May 2019.

    Access the full UK drug database with a FREE Medscape UK Account
    It takes just a few minutes, and you’ll get unlimited access to information on over 11,000 UK drugs.
    Register for Free

    Already a member? Log in

    Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content

    FDB Logo

    FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.