Drug Overview
Juxtapid (lomitapide mesylate) is a novel, first-in-class microsomal triglyceride transfer protein (MTP) inhibitor marketed by Aegerion. MTP is responsible for the transfer of triglycerides (TGs) onto apolipoprotein B, affecting production of both very low-density lipoprotein (VLDL) cholesterol in the liver and chylomicrons in the intestine. Low-density lipoprotein (LDL) particles are formed through the action of lipoprotein lipase, which removes TGs from VLDL particles. Inhibition of VLDL production therefore leads to a reduction in plasma levels of LDL cholesterol.
Despite strong initial uptake, Juxtapid sales have been lower than expected over the past few years due to high patient dropout rates. Aegerion has attributed these high discontinuation rates to Juxtapid’s unfavorable side-effect profile and recent competition from the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors Repatha (evolocumab; Amgen/Astellas) and Praluent (alirocumab; Sanofi/Regeneron). Unlike Juxtapid, which has a black box warning for severe liver toxicity, Repatha and Praluent have demonstrated impressive safety and tolerability profiles throughout clinical trials. Additionally, the enormous $235,000–$295,000 annual cost of Juxtapid further disadvantages the product as compared to PCSK9 products, which can be acquired for less than $10,000 per year. The author expects the number of US patients using Juxtapid to continue to decline as more and more patients switch to the cheaper and more tolerable PCSK9 inhibitors.
Juxtapid (lomitapide mesylate) is a novel, first-in-class microsomal triglyceride transfer protein (MTP) inhibitor marketed by Aegerion. MTP is responsible for the transfer of triglycerides (TGs) onto apolipoprotein B, affecting production of both very low-density lipoprotein (VLDL) cholesterol in the liver and chylomicrons in the intestine. Low-density lipoprotein (LDL) particles are formed through the action of lipoprotein lipase, which removes TGs from VLDL particles. Inhibition of VLDL production therefore leads to a reduction in plasma levels of LDL cholesterol.
Despite strong initial uptake, Juxtapid sales have been lower than expected over the past few years due to high patient dropout rates. Aegerion has attributed these high discontinuation rates to Juxtapid’s unfavorable side-effect profile and recent competition from the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors Repatha (evolocumab; Amgen/Astellas) and Praluent (alirocumab; Sanofi/Regeneron). Unlike Juxtapid, which has a black box warning for severe liver toxicity, Repatha and Praluent have demonstrated impressive safety and tolerability profiles throughout clinical trials. Additionally, the enormous $235,000–$295,000 annual cost of Juxtapid further disadvantages the product as compared to PCSK9 products, which can be acquired for less than $10,000 per year. The author expects the number of US patients using Juxtapid to continue to decline as more and more patients switch to the cheaper and more tolerable PCSK9 inhibitors.
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