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Effect of pradigastat, a diacylglycerol acyltransferase 1 inhibitor, on the pharmacokinetics of a combination oral contraceptive in healthy female subjects

Chen, Jin and Bhansali, Suraj and Neelakantham, Srikanth Raju and Trusley, Craig and Majumdar, Tapan and Rebello, Sam and Sunkara, Gangadhar and Meyers, Charles (2015) Effect of pradigastat, a diacylglycerol acyltransferase 1 inhibitor, on the pharmacokinetics of a combination oral contraceptive in healthy female subjects. International Journal of Clinical Pharmacology and Therapeutics, 53 (4). pp. 317-324. ISSN 0946-1965

Abstract

Objective: We evaluated the potential pharmacokinetic interaction between pradigastat, a potent and selective dia-cylglycerol acyltransferase 1 inhibitor, and Levora-28®, a combination oral contraceptive (COC) containing 30 μg ethinylestra-diol (EE) and 150 μg levonorgestrel (LVG). Methods: An open-label, single-sequence, three-period (period 1, single dose of COC; period 2, pradigastat 100 mg × 3 days followed by 40 mg × 7 days; and period 3, both pradigastat 40 mg and a single dose of COC) study involving 24 healthy female subjects of childbearing potential was conducted. Results: The pharmacokinetic parameters of EE were similar when administered alone or in combination with pradigastat, as the 90% confidence interval (CI) of geometric mean ratios for EE exposure (AUC and C<inf>max</inf>) were all within the range of 0.80 - 1.25. The AUC<inf>∞</inf>, AUC<inf>last</inf>, and C<inf>max</inf> of LVG were slightly increased in the presence of pradi-gastat, the geometric mean ratios (90% CI) were 1.25 (1.16, 1.35), 1.24 (1.15, 1.34), and 1.16 (1.06, 1.27), respectively. Conclusions: Pradigastat did not elicit clinically relevant changes in the magnitude of Levora-28® exposure. Therefore, dose adjustment is not required for Levora-28® when co-administered with pradigastat.

Item Type: Article
Keywords: Drug-drug interaction Oral contraceptive Pharmaco-kinetics Pradigastat
Date Deposited: 14 Mar 2018 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/23674

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