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Food Does Not Affect the Pharmacokinetics of Tesaglitazar, a Novel Dual Peroxisome Proliferator‐Activated Receptor α/γ Agonist
Author(s) -
Samuelsson S.,
Johansson S.,
Halldórsdóttir S.,
Stenhoff H.,
Öhman K. P.
Publication year - 2006
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270006290335
Subject(s) - pharmacokinetics , crossover study , agonist , medicine , confidence interval , endocrinology , calorie , bioavailability , chemistry , receptor , pharmacology , placebo , alternative medicine , pathology
Tesaglitazar is a dual peroxisome proliferator‐activated receptor (PPAR) α/γ 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 (C max ). Mean C max 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 C max was increased (2.00 vs 0.75 h) in fed versus fasted state. The median difference of t max 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.