lomitapide mesylate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
lomitapide mesylate: clinical details
Prescribing considerations
- Initiate and monitor through a clinician experienced in lipid disorders.
- Confirm homozygous familial hypercholesterolaemia genetically where possible and exclude secondary causes of hypercholesterolaemia.
- Ensure a low-fat diet, dietary counselling and supplementation with vitamin E and essential fatty acids.
- Review alcohol intake, hepatotoxic medicines, CYP3A4 interactions and contraception before initiation.
- Clinical experience is limited in older adults; use in people under 18 is not recommended.
Contraindications and cautions
- Pregnancy
- Moderate or severe hepatic impairment or unexplained persistent abnormal liver tests
- Significant or chronic bowel disease, including inflammatory bowel disease or malabsorption
- Strong or moderate CYP3A4 inhibitors
- Simvastatin above the SmPC-permitted maximum
- Hypersensitivity to lomitapide or an excipient
Monitoring
- Check ALT, AST, alkaline phosphatase, bilirubin, gamma-GT and albumin before treatment.
- Monitor liver-related tests closely during the first year and regularly thereafter, with additional testing after clinically significant abnormalities.
- Screen for steatohepatitis or fibrosis at baseline and annually using appropriate imaging and biomarkers with hepatology input.
- Monitor LDL cholesterol, gastrointestinal tolerability, hydration, weight and adherence to dietary supplementation.
- Monitor INR closely when used with a coumarin anticoagulant.
Clinical pharmacology
Lomitapide selectively inhibits microsomal triglyceride transfer protein. It has low oral bioavailability, is highly protein-bound and is extensively metabolised, predominantly by CYP3A4; it also inhibits CYP3A4 and P-glycoprotein.
Formulation and product differences
- The selected UK product is an oral hard capsule.
- The capsule contains lactose monohydrate and gelatin and is essentially sodium-free.
- Keep the bottle tightly closed to protect the capsules from moisture.
lomitapide mesylate preparations and strengths
Capsule
Route: Oral
Strengths: 5 mg, 10 mg, 20 mg
lomitapide mesylate interactions
Lomitapide has important interactions. Check all prescriptions, over-the-counter products, supplements and herbal remedies with the specialist or pharmacist.
Strong or moderate CYP3A4 inhibitors
Azole antifungals, clarithromycin, erythromycin, HIV protease inhibitors, diltiazem, verapamil and dronedarone can markedly increase lomitapide exposure and are contraindicated.
Grapefruit juice
Can substantially increase lomitapide exposure and should be avoided.
Weak CYP3A4 inhibitors, including atorvastatin
May increase lomitapide exposure, requiring specialist review of administration timing or treatment.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.