A Novel ω-3 Acid Ethyl Ester Formulation Incorporating Advanced Lipid TechnologiesTM (ALT® ) Improves Docosahexaenoic Acid and Eicosapentaenoic Acid Bioavailability Compared with Lovaza

• Published in: Clinical therapeutics Vol. 39; no. 3; pp. 581 - 591
• Main Authors: Lopez-Toledano, Miguel A., PhD, Thorsteinsson, Thorsteinn, PhD, Daak, Ahmed, MD, MSc, PhD, Maki, Kevin C., PhD, Johns, Colleen, BS, Rabinowicz, Adrian L., MD, Sancilio, Frederick D., PhD
• Format: Journal Article
• Language: English
• Published: Bridgewater Elsevier Inc 01.03.2017; Elsevier Limited
• Subjects: Advanced Lipid Technologies; Alcohol; Bioavailability; Blood & organ donations; Diet; Dietary supplements; Docosahexaenoic acid; Drug dosages; Drugs; Eicosapentaenoic acid; Esters; Ethyl esters; Family medical history; Fatty acids; FDA approval; Feeding; food effect; Hepatitis; Hormone replacement therapy; Hypertriglyceridemia; Internal Medicine; Lipids; Lipoproteins; Medical Education; Metabolism; Pharmacology; Prescription drugs; Triglycerides; ω-3 fatty acids; United States > US; eicosapentaenoic acid; ω-3 fatty acids; food effect; bioavailability; Advanced Lipid Technologies; docosahexaenoic acid
• ISSN: 0149-2918; 1879-114X
• DOI: 10.1016/j.clinthera.2017.01.020

Abstract Purpose The US Food and Drug Administration has approved several highly purified ω-3 fatty acid prescription drugs for the treatment of severe hypertriglyceridemia. These differ in the amounts and forms of docosahexaenoic acid (DHA) and/or eicosapentaenoic acid (EPA). This study compared the bioavailability of SC401 (1530 mg EPA-ethyl esters [EEs] and DHA-EEs plus Advanced Lipid Technologies [ALT ], a proprietary lipid-delivery platform to improve absorption), with. Lovaza (3600 mg ω-3, primarily EPA-EEs and DHA-EEs) under low-fat feeding conditions. Methods This was a Phase I, randomized, open-label, single-dose, 2-way crossover study in healthy participants housed from day –3 to day 2 in each treatment period. Blood samples for pharmacokinetic measurements were collected before and after dosing, and safety profile and tolerability were assessed. Findings In unadjusted analyses, SC401 had 5% lower Cmax and approximately the same AUC0–last of EPA + DHA total lipids compared with Lovaza. When adjusted for baseline, SC401 had ~6% higher Cmax and 18% higher AUC0–last for EPA + DHA total lipids, and dose- and baseline-adjusted analyses found that SC401 had ~149% higher Cmax and 178% higher AUC0–last than Lovaza for EPA + DHA total lipids. The Tmax was also substantially longer with Lovaza (~10 hours) than with SC401 (~6 hours). Implications These results indicate that SC401, an ω-3 acid EE formulation containing ALT achieved high bioavailability of EPA and DHA, at a lower dose (1530 mg) than Lovaza (3600 mg), under low-fat feeding conditions.