Drug-drug interactions between pemafibrate and statins on pharmacokinetics in healthy male volunteers: Open-label, randomized, 6-sequence, 3-period crossover studies.

Elevated triglyceride levels are associated with an increased risk of cardiovascular events despite guideline-based statin treatment of low-density lipoprotein cholesterol. Peroxisome proliferator-activated receptor α (PPARα) agonists exert a significant triglyceride-lowering effect. However, combination therapy of PPARα agonists with statins poses an increased risk of rhabdomyolysis, which is rare but a major concern of the combination therapy.

Efficacy and Safety of K-877 (Pemafibrate), a Selective PPARα Modulator, in European Patients on Statin Therapy.

Objective: High plasma triglyceride (TG) is an independent risk factor for cardiovascular disease. Fibrates lower TG levels through peroxisome proliferator-activated receptor α (PPARα) agonism. Currently available fibrates, however, have relatively low selectivity for PPARα.

Statin action favors normalization of the plasma lipidome in the atherogenic mixed dyslipidemia of MetS: potential relevance to statin-associated dysglycemia.

The impact of statin treatment on the abnormal plasma lipidome of mixed dyslipidemic patients with metabolic syndrome (MetS), a group at increased risk of developing diabetes, was evaluated. Insulin-resistant hypertriglyceridemic hypertensive obese males (n = 12) displaying MetS were treated with pitavastatin (4 mg/day) for 180 days; healthy normolipidemic age-matched nonobese males (n = 12) acted as controls. Statin treatment substantially normalized triglyceride (-41%), remnant cholesterol (-55%), and LDL-cholesterol (-39%), with minor effect on HDL-cholesterol (+4%).

Pitavastatin therapy in polymedicated patients is associated with a low risk of drug-drug interactions: analysis of real-world and phase 3 clinical trial data.

Objectives: Medications that interact with the pathways responsible for statin metabolism may increase the risk of statin-associated myalgia. Pharmacokinetic studies show that pitavastatin is carried into the liver by a range of transporters and is minimally metabolized by cytochrome P450 in healthy volunteers, indicating a reduced potential for drug-drug interactions (DDIs). This post hoc analysis investigates the incidence of adverse events in patients receiving pitavastatin with concomitant medication in two large data sets.

Efficacy and Safety of Pitavastatin in Children and Adolescents at High Future Cardiovascular Risk.

Objectives: To assess the safety and efficacy of pitavastatin in children and adolescents with hyperlipidemia.

Study Design: A total of 106 children and adolescents with hyperlipidemia, ages 6 to 17 years, were enrolled in a 12-week randomized, double-blind, placebo-controlled study and randomly assigned to pitavastatin 1 mg, 2 mg, 4 mg, or placebo. During a 52-week extension period, subjects were up-titrated from 1 mg pitavastatin to a maximum dose of 4 mg in an effort to achieve an optimum low-density lipoprotein cholesterol (LDL-C) treatment target of <110 mg/dL (2.

Pitavastatin Concentrations Are Not Increased by CYP3A4 Inhibitor Itraconazole in Healthy Subjects.

Itraconazole is a synthetic triazole antifungal agent which is known to be a potent inhibitor of cytochrome P450 (CYP) 3A4, and may cause drug-drug interactions with the many drugs metabolized by this route, including some statins. In this study, the influence of concomitant administration of a single oral dose of pitavastatin with itraconazole at steady state was investigated to determine the potential for pharmacokinetic interaction and any effects on safety. Eighteen subjects were enrolled into the study.

Pitavastatin shows greater lipid-lowering efficacy over 12 weeks than pravastatin in elderly patients with primary hypercholesterolaemia or combined (mixed) dyslipidaemia.

Aim: To compare the safety and efficacy of once-daily pitavastatin (1, 2, and 4 mg) and pravastatin (10, 20, and 40 mg) in elderly patients (≥ 65 years of age) with primary hypercholesterolaemia or combined (mixed) dyslipidaemia.

Design: After a 6-8-week washout/dietary period, patients were randomized to six treatment groups (1, 2, or 4 mg pitavastatin vs. 10, 20, or 40 mg pravastatin) in a 12-week multicentre double-blind study.

Pitavastatin demonstrates long-term efficacy, safety and tolerability in elderly patients with primary hypercholesterolaemia or combined (mixed) dyslipidaemia.

Aims: To assess the long-term efficacy, safety and tolerability of pitavastatin (2 and 4 mg) in elderly patients (≥ 65 years of age) with primary hypercholesterolaemia or combined (mixed) dyslipidaemia.

Design: Patients (n = 545) who had completed a 12-week double-blind comparative study (core study) of pitavastatin and pravastatin entered a 60-week, open-label, multicentre extension study of pitavastatin. The initial daily dose was 2 mg, increasing to 4 mg after 8 weeks if necessary to achieve treatment targets.

Comparison of the pharmacokinetics of pitavastatin by formulation and ethnic group: an open-label, single-dose, two-way crossover pharmacokinetic study in healthy Caucasian and Japanese men.

Background And Objectives: Pitavastatin is a highly effective lipid-lowering drug (approved dose range 1-4 mg/day) with a distinctive metabolic pathway that has a low potential for drug interactions. The efficacy and safety of pitavastatin have been characterized in a broad clinical development programme conducted initially in Japanese patients. The objectives of the present study were to evaluate the pharmacokinetic bioequivalence of the European (EU) and Japanese (JP) formulations of pitavastatin 2 mg in healthy Japanese and Caucasian men, and to assess whether the bioavailability of each formulation was similar in the two ethnic groups.

Comparative efficacy of pitavastatin and simvastatin in high-risk patients: a randomized controlled trial.

Introduction: Despite the proven efficacy of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) in lowering total and low-density lipoprotein cholesterol (LDL-C), many patients do not reach recommended lipid targets. This study compared pitavastatin, a new and highly effective statin, and simvastatin in patients at high risk of coronary heart disease (CHD). The primary objective was to demonstrate noninferiority of pitavastatin to simvastatin.

Long-term efficacy of pitavastatin versus simvastatin.

Introduction: Pitavastatin is a novel, potent, 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. This study compared the long-term efficacy of pitavastatin and simvastatin in dyslipidemic patients at high risk of coronary heart disease.

Methods: A 44-week blinded extension study was conducted at 24 centers in five European countries for patients who had previously completed a 12-week randomized, double-blind core study in which they received pitavastatin 4 mg or simvastatin 40 mg once daily.

Long-term treatment with pitavastatin is effective and well tolerated by patients with primary hypercholesterolemia or combined dyslipidemia.

Objectives: The primary objective was to assess the safety and tolerability of pitavastatin 4mg once daily during 52 weeks treatment. The secondary objectives were to assess the effect on lipid and lipoprotein fractions and ratios, and LDL-C target attainment.

Methods: Patients with primary hypercholesterolemia or combined dyslipidemia who had previously received pitavastatin, atorvastatin or simvastatin for 12 weeks during double-blind phase III studies received open-label pitavastatin 4mg once daily for up to 52 weeks.

Comparison of pitavastatin with simvastatin in primary hypercholesterolaemia or combined dyslipidaemia.

Objectives: The primary objective of this study was to demonstrate equivalence of pitavastatin compared with simvastatin in the reduction of low-density lipoprotein cholesterol (LDL-C) levels in patients with primary hypercholesterolaemia or combined dyslipidaemia. Secondary objectives included achievement of National Cholesterol Education Program Adult Treatment Panel (NECP) and European Atherosclerosis Society (EAS) LDL-C goals, comparison of other lipid parameters, and assessment of safety and tolerability of the two statins.

Research Design And Methods: A prospective, randomised, active-controlled double-blind, double-dummy, 12-week therapy trial was conducted in 857 patients with either primary hypercholesterolaemia or combined dyslipidaemia.

Pregabalin drug interaction studies: lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and valproate in patients with partial epilepsy.

Purpose: Pregabalin (PGB) is an alpha2-delta ligand with demonstrated efficacy in epilepsy, neuropathic pain, and anxiety disorders. PGB is highly efficacious as adjunctive therapy in patients with refractory partial seizures.

Methods: Given its efficacy as adjunctive therapy, the potential for interaction of PGB with other antiepileptic drugs (AEDs) was assessed in patients with partial epilepsy in open-label, multiple-dose studies.