Lojuxta 5 mg hard capsules

Lojuxta 10 mg hard capsules

Lojuxta 20 mg hard capsules

Each 5 mg hard capsule contains lomitapide mesylate equivalent to 5 mg lomitapide.

Each 10 mg hard capsule contains lomitapide mesylate equivalent to 10 mg lomitapide.

Each 20 mg hard capsule contains lomitapide mesylate equivalent to 20 mg lomitapide.

Excipient with known effect

Each 5 mg hard capsule contains 70.12 mg of lactose (as monohydrate) (see section 4.4).

Each 10 mg hard capsule contains 140.23 mg of lactose (as monohydrate) (see section 4.4).

Each 20 mg hard capsule contains 129.89 mg of lactose (as monohydrate) (see section 4.4).

For the full list of excipients, see section 6.1.

Capsule, hard.

The 5 mg capsule is an orange cap/orange body hard capsule of 19.4 mm, printed with black ink imprinted with “5 mg” on body and “A733” on cap.

The 10 mg capsule is an orange cap/white body hard capsule of 19.4 mm, printed with black ink imprinted with “10 mg” on body and “A733” on cap.

The 20 mg capsule is a white cap/white body hard capsule of 19.4 mm, printed with black ink imprinted with “20 mg” on body and “A733” on cap.

Lojuxta 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.

Treatment with Lojuxta should be initiated and monitored by a physician experienced in the treatment of lipid disorders.

Posology

The recommended starting dose is 5 mg once daily. After 2 weeks the dose may be increased, 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 (see section 4.8).

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

Administration with food may increase exposure to Lojuxta. Lojuxta 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.

The occurrence and severity of gastrointestinal adverse reactions associated with the use of Lojuxta 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 Lojuxta treatment, and should continue this diet during treatment. Dietary counselling should be provided.

Patients should avoid consumption of grapefruit juice (see sections 4.4 and 4.5).

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

• Separate the dose of the medications by 12 hours

OR

• Decrease the dose of Lojuxta by half.

Patients on 5 mg should remain on 5 mg.

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

Upon discontinuation of atorvastatin the dose of Lojuxta should be up-titrated according to LDL-C response and safety/tolerability.

For patients on a stable maintenance dose of Lojuxta who receive any other weak CYP3A4 inhibitor, separate the dose of the medications (Lojuxta and the weak CYP3A4 inhibitor) by 12 hours.

Consider limiting the maximum dose of Lojuxta according to desired LDL-C response.

Exercise additional caution if administering more than 1 weak CYP3A4 inhibitor with Lojuxta.

Based on observations of decreased essential fatty acid and vitamin E levels in clinical trials, 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 Lojuxta.

Elderly population

There is limited experience with Lojuxta 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.

Hepatic impairment

Lojuxta is contraindicated in patients with moderate or severe hepatic impairment including patients with unexplained persistent abnormal liver function tests (see section 5.2).

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

Renal impairment

Patients with end-stage renal disease receiving dialysis should not exceed 40 mg daily (see section 5.2).

Paediatric population

The safety and efficacy of Lojuxta in children <18 years have not been established and the use of this medicinal product in children is therefore not recommended. No data are available.

Method of administration

Oral use.

• Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

• Patients with moderate or severe hepatic impairment and those with unexplained persistent abnormal liver function tests.

• Patients with a known significant or chronic bowel disease such as inflammatory bowel disease or malabsorption.

• Concomitant administration of >40 mg simvastatin (see section 4.5).

• Concomitant use of Lojuxta with strong or moderate cytochrome P450 (CYP) 3A4 inhibitors (e.g., antifungal azoles such as itraconazole, fluconazole,ketoconazole, voriconazole, posaconazole; macrolide antibiotics such as erythromycin or clarithromycin; ketolide antibiotics such as telithromycin; HIV protease inhibitors; the calcium channel blockers diltiazem and verapamil, and the anti-arrhythmic dronedarone [see section 4.5]).

• Pregnancy (see section 4.6).