J Clin Pharmacol
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PHARMACOKINETICS

Food Does Not Affect the Pharmacokinetics of Tesaglitazar, a Novel Dual Peroxisome Proliferator-Activated Receptor {alpha}/{gamma} Agonist

S. Samuelsson, MSc, S. Johansson, MSc, S. Halldórsdóttir, MSc, H. Stenhoff, MSc and K. P. Öhman, MD, PhD

From AstraZeneca R&D Mölndal, Mölndal, Sweden.

Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) {alpha}/{gamma} agonist in development to treat lipid and glucose abnormalities associated with type 2 diabetes. This study evaluated the effects of food on tesaglitazar pharmacokinetics. In an open, randomized, 2-way crossover study, 20 healthy men received tesaglitazar 1 mg during fasting and after a high-fat, high-calorie breakfast. Blood samples were taken to assess pharmacokinetic variables. Systemic exposure to tesaglitazar was unaffected by food intake. Estimated ratios were 0.99 (90% confidence interval [CI], 0.94-1.04) for fed/fasted area under plasma concentration-time curve and 0.82 (90% CI, 0.78-0.86) for fed/fasted maximum plasma concentration (Cmax). Mean Cmax was ~18% lower (0.41 [95% CI, 0.38-0.43] versus 0.50 [95% CI, 0.47-0.53] µmol/L), and median time to Cmax was increased (2.00 vs 0.75 h) in fed versus fasted state. The median difference of tmax was 1.25 h (P = .0001, signed-rank test). Tesaglitazar was well tolerated. Tesaglitazar pharmacokinetics is unaffected by food intake, allowing once-daily administration of tesaglitazar with or without food in clinical practice.

Key Words: Tesaglitazar • PPAR • type 2 diabetes • food • pharmacokinetics


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