PRODUCTS

PRODUCTS

AMR101 for Hypertriglyceridemia

INTRODUCTION

AMR101 is a prescription grade Omega-3 fatty acid. It is a semi-synthetic, ultra pure (~97%) ethyl ester of eicosapentaenoic acid (Ethyl-EPA), a long chain highly unsaturated fatty acid (often written in short as 20:5n-3 or 20:5ω3).

Amarin’s cardiovascular strategy was initiated in November 2007 to leverage its extensive know-how and experience in lipid science and the potential therapeutic benefits of unsaturated fatty acids in cardiovascular disease. AMR101 is believed to impact on a number of biological factors in the body such as anti-inflammatory mechanisms, cell membrane composition and plasticity, triglyceride levels and regulation of glucose metabolism.

AMR101 is being progressed to Phase III clinical development for hypertriglyceridemia. Hypertriglyceridemia refers to a condition in which patients have high blood levels of triglycerides and is associated with increased levels of heart disease. It is one component of a range of lipid disorders collectively referred to as dyslipidemia. The overall dyslipidemia population in the U.S. is believed to be in excess of 100 million, with over 10 million of those diagnosed with hypertriglyceridemia. The value of the dyslipidemia market, excluding statins, was estimated at approximately $2.2 billion in 2006, representing a compound annual growth rate of 31% since 2002. The major driver of this growth is believed to be an overall broadening of dyslipidemia treatment beyond reduction in low density lipoprotein (LDL) cholesterol.

DEVELOPMENT STATUS

Amarin has met with officials at the U.S. Food and Drug Administration to discuss the Company’s plans to develop AMR101 for the treatment of hypertriglyceridemia. Following these discussions, the Company is proceeding to Phase III with AMR101 in hypertriglyceridemia, with commencement in 2009.

Amarin has previously investigated AMR101 in central nervous system disorders in several double-blind, placebo controlled studies, including Phase III trials in Huntington’s disease. Over 900 patients have received AMR101 in these studies, with over 100 receiving continuous treatment for a year or more. In all studies performed to date, AMR101 has shown a very good safety profile.

Numerous studies have demonstrated the safety and efficacy of ethyl-EPA in lowering plasma triglycerides in patients with high triglyceride levels of varying degrees of severity. In Japan, an ethyl-EPA prescription product has been approved for the treatment of high triglycerides and has been on the market for seventeen years. In Amarin’s most recent trials with AMR101 in Huntington’s disease, AMR101 was shown to lower triglycerides in patients with elevated baseline levels.

REFERENCES

  • Yokoyama et al – Lancet 2007;369;1090-1098 - “Effects of Eicosapentaenoic Acid on Major Coronary Events in Hypercholesterolaemic patients (Jelis): A Randomised Open-Label, Blinded Endpoint Analysis” 
  • Matsumoto et al - Abstract from ISSFAL meeting in Cairns Australia, 2006 – “Oral Administration of Eicosapentaenoic Acid Reduces and Stabilizes Atherosclerotic Lesions Through Lipid Lowering Independent Mechanism in APO E-Deficient Mice” 
  • Mori et al – Am J Clin Nutr 2000;71:1085-1094 – “Purified Eicosapentaenoic and Docosahexaenoic Acids Have Different Effects on Serum lipids and Lipoproteins, LDL Particle Size, Glucose and Insulin in Mildly Hyperlipidemic Men”