Active Ingredient: Lomitapide
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 hyperlipoproteinemia and secondary causes of hypercholesterolaemia (e.g., nephrotic syndrome, hypothyroidism) must be excluded.
For this indication, competent medicine agencies globally authorize below treatments:
For:
Oral, 5 milligrams lomitapide, once daily 120 minutes after dinner, over the duration of 2 weeks. Afterwards, oral, 10 milligrams lomitapide, once daily 120 minutes after dinner, over the duration of 4 weeks. Afterwards, oral, 20 milligrams lomitapide, once daily at evening, over the duration of 4 weeks. Afterwards, oral, 40 milligrams lomitapide, once daily 120 minutes after dinner, over the duration of 4 weeks. Afterwards, oral, 60 milligrams lomitapide, once daily 120 minutes after dinner.
The recommended starting dose is 5 mg once daily. After 2 weeks the dose may be increased, according to LDL-C response and based on acceptable safety and tolerability, to 10 mg and then, at a minimum of 4-week intervals, to 20 mg, 40 mg, and to the maximum recommended dose of 60 mg.
The dose should be escalated gradually to minimise the incidence and severity of gastrointestinal adverse reactions and aminotransferase elevations.
The occurrence and severity of gastrointestinal adverse reactions associated with the use of lomitapide decreases in the presence of a low fat diet. Patients should follow a diet supplying less than 20% of energy from fat prior to initiating treatment, and should continue this diet during treatment. Dietary counselling should be provided.
Patients should avoid consumption of grapefruit juice and alcohol.
For patients on a stable maintenance dose of lomitapide who receive atorvastatin either:
OR
Careful titration may then be considered according to LDL-C response and safety/tolerability. Upon discontinuation of atorvastatin the dose of lomitapide should be up-titrated according to LDL-C response and safety/tolerability.
For patients on a stable maintenance dose of lomitapide who receive any other weak cytochrome P450 (CYP) 3A4 inhibitor, separate the dose of the medicinal products (lomitapide and the weak CYP3A4 inhibitor) by 12 hours. Exercise additional caution if administering more than 1 weak CYP3A4 inhibitor with lomitapide. Consider limiting the maximum dose of lomitapide according to desired LDL-C response.
Based on observations of decreased essential fatty acid and vitamin E levels in clinical studies, patients should take daily dietary supplements that provide 400 IU vitamin E and approximately 200 mg linoleic acid, 110 mg eicosapentaenoic acid (EPA), 210 mg alpha linolenic acid (ALA) and 80 mg docosahexaenoic acid (DHA) per day, throughout treatment with lomitapide.
There is limited experience with lomitapide in patients aged 65 years or older. Therefore, particular caution should be exercised in these patients.
Since the recommended dose regimen involves starting at the low end of the dosing range and escalating cautiously according to individual patient tolerability, no adjustment to the dosing regimen is recommended for the elderly.
Administration with food may increase exposure to lomitapide. It 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.
Grapefruit juice must be omitted from the diet while patients are treated with lomitapide.
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