No influence of moderate hepatic impairment on the pharmacokinetics of lumiracoxib, an oral COX-2 selective inhibitor.

The aim of this study was to evaluate the influence of hepatic impairment on the pharmacokinetics (PK) of the novel cyclooxygenase-2 (COX-2) selective inhibitor lumiracoxib (Prexige), so that dose recommendations for clinical use can be provided. This was an open-label, single dose, case-controlled study in which eight subjects with liver cirrhosis classed as moderate hepatic impairment (Child-Pugh score: 7-9) and eight demographically-matched healthy subjects received a single oral 400 mg dose of lumiracoxib. Routine safety assessments were made and blood samples were taken for determination of lumiracoxib concentrations for 96 h post dose.

Concomitant administration of lumiracoxib and a triphasic oral contraceptive does not affect contraceptive activity or pharmacokinetic profile.

This study evaluated the effect of lumiracoxib on the pharmacokinetics and pharmacodynamics of ethinyl estradiol (EE) and levonorgestrel (LN) in Triphasil-28 (a triphasic oral contraceptive). Females stabilized on Triphasil-28 continued on Triphasil-28 alone for another month (Treatment Period 1), then also received lumiracoxib (400 mg daily) or placebo for 28 days each (Periods 2 and 3) in a double-blind crossover design. Plasma pharmacokinetic profiles were assessed on Day 21 of Periods 2 and 3.

Pharmacokinetics of lumiracoxib in plasma and synovial fluid.

Background: Lumiracoxib is a new cyclo-oxygenase-2 (COX-2) selective inhibitor in development for the treatment of rheumatoid arthritis, osteoarthritis and acute pain.

Objective: To investigate the pharmacokinetics of lumiracoxib in plasma and knee joint synovial fluid from patients with rheumatoid arthritis.

Design: Open-label multiple-dose study evaluating the steady-state pharmacokinetics of lumiracoxib in plasma and synovial fluid after 7 days of treatment with lumiracoxib 400 mg once daily.

Differential influence of two cyclosporine formulations on everolimus pharmacokinetics: a clinically relevant pharmacokinetic interaction.

Everolimus is an immunosuppressant intended for use with cyclosporine in acute-rejection prophylaxis following organ transplantation. The possibility of a drug interaction of cyclosporine on everolimus was assessed. In this randomized, two-period, crossover study, 24 healthy subjects received a single oral dose of 2 mg everolimus alone and with one of two cyclosporine formulations: either 175 mg Neoral or 300 mg Sandimmune.

Mealtime glucose regulation with nateglinide in healthy volunteers: comparison with repaglinide and placebo.

Objective: This study was designed to compare the pharmacodynamic effects of single doses of nateglinide (A-4166), repaglinide, and placebo on mealtime insulin secretion and glycemic control in healthy subjects.

Research Design And Methods: Fifteen healthy volunteers participated in this open-label five-period crossover study. They received single 10-min preprandial doses of 120 mg nateglinide, 0.