Lomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor primarily used as an adjuvant therapy in adult patients with homozygous familial hypercholesterolemia (HoFH), requiring a combination of low-fat diet and other lipid-lowering treatments. This drug is not marketed in China and requires close monitoring of liver function and fat metabolism.

1. Basic Information

Common name: Lometapai Lomitapide; Product Name: Juxtapid. Approved for market by the FDA in December 2012 and by the European Commission in July 2013. The specifications produced in Japan include 5mg, 10mg, and 20mg (14 capsules), which are relatively expensive and currently have no generic drugs.

2 Indications and Mechanisms of Action

The indication is adjuvant therapy for adult patients with HoFH, which requires the combination of other lipid-lowering measures. Its target is MTP, which reduces lipoprotein synthesis by inhibiting this protein, thereby lowering cholesterol levels.

3 Usage and Dosage

The initial dose is 5mg orally per day, the maintenance dose is 5-60mg/day (individualized adjustment), and the maximum dose is 60mg/day. Missing server does not require replacement, excessive data processing is insufficient. The dosage needs to be adjusted based on factors such as liver function and drug interactions.

4 Precautions

(1) Prohibited during pregnancy, there is a risk to the fetus; (2) May cause deficiency of fat soluble vitamins and require supplementation; (3) Common gastrointestinal reactions; (4) INR needs to be monitored when combined with warfarin.

Medication for 5 special populations

Prohibited during lactation period; The safety of children has not been established; Elderly patients do not need to adjust the dosage; Use with caution in patients with moderate to severe liver damage; People with renal insufficiency usually do not need to adjust the dosage.

6 pharmacokinetics

The peak is reached about 6 hours after oral administration, with a plasma protein binding rate of 99.8%, mainly metabolized by the liver, and a half-life of about 39.7 hours. Excretion through urine and feces, storage should be kept away from moisture and high temperatures, with a shelf life of 24 months.