Pharmacokinetics of MAT9001, an Omega‐3 Fatty Acid Medication, Compared with Eicosapentaenoic Acid Ethyl Esters in Hypertriglyceridemic Subjects

Abstract

Synopsis MAT9001 (Matinas BioPharma Inc., Bedminster, NJ) is a novel investigational omega‐3 fatty acid (OM3) medication containing predominantly eicosapentaenoic (EPA) and docosapentaenoic (DPA) acids under development as an adjunct to diet for the treatment of severe hypertriglyceridemia (≥500 mg/dL). Purpose This randomized, crossover trial compared the bioavailability of MAT9001 and an OM3 EPA ethyl ester (EPA‐EE) agent (Vascepa; Amarin Pharmaceuticals, Bedminster, NJ) after single‐ and multiple‐dosing under fed (low‐fat) conditions in men and women with fasting triglycerides (TG) 200–400 mg/dL at screening without lipid‐altering therapy, or TG 200–350 mg/dL if on stable‐dose statin monotherapy. Methods Forty‐two subjects received 4 g/day MAT9001 and EPA‐EE in random order, while housed in a clinical research unit for 14‐day treatment periods, separated by ≥35 days of wash‐out. Baseline values were averaged from pre‐dose samples drawn on days −1 and 0. On‐treatment values were determined from plasma samples drawn on days 0 (single‐dose) and 13 (multiple‐dose). Total EPA, DPA, docosahexaenoic (DHA) and heneicosapentaenoic (HPA) acids were measured in plasma by a liquid chromatography–tandem mass spectrometry method using isotopically substituted OM3 compounds as internal standards. Total OM3 was calculated as the sum of molar concentrations of total EPA, DPA, DHA, and HPA for each time point. Systemic exposure (area under the curve [AUC]) and peak exposure (C max ) were ca…