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Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: Results from two randomized, double‐blind, placebo‐controlled studies with single
TLDR
Sitagliptin is an orally active, potent, and selective inhibitor of dipeptidyl peptidase IV (DPP‐IV) currently in phase III development for the treatment of type 2 diabetes. Expand
Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.
TLDR
Ezetimibe does not have significant effects on plasma levels of HMG-CoA reductase inhibitors commonly known as statins, and coadministration with gemfibrozil and fenofibrate increased the bioavailability of ezetIMibe, but the clinical significance is thought to be minor. Expand
Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes.
TLDR
In patients with type 2 diabetes, near maximal glucose-lowering efficacy of sitagliptin after single oral doses was associated with inhibition of plasma DPP-4 activity of 80% or greater, corresponding to a plasma sitgliptin concentration of 100 nm or greater and an augmentation of active GLP-1 and GIP levels of 2-fold or higher after an OGTT. Expand
Transport of the Dipeptidyl Peptidase-4 Inhibitor Sitagliptin by Human Organic Anion Transporter 3, Organic Anion Transporting Polypeptide 4C1, and Multidrug Resistance P-glycoprotein
TLDR
The data indicate that sitagliptin is unlikely to be a perpetrator of drug-drug interactions with Pgp, hOAT1, or hOat3 substrates at clinically relevant concentrations, and the effects may not be clinically meaningful, due to the high safety margin of sitgliptin. Expand
Metabolism And Excretion of the Dipeptidyl Peptidase 4 Inhibitor [14C]Sitagliptin in Humans
TLDR
The metabolism and excretion of [14C]sitagliptin, an orally active, potent and selective dipeptidyl peptidase 4 inhibitor, were investigated in humans after a single oral dose of 83 mg/193 μCi, indicating that sitagli leptin was eliminated primarily by renal excretion. Expand
Effect of the cholesteryl ester transfer protein inhibitor, anacetrapib, on lipoproteins in patients with dyslipidaemia and on 24-h ambulatory blood pressure in healthy individuals: two double-blind,
TLDR
Anacetrapib seems to exhibit HDL-C increases greater than those seen with other investigational drugs in this class and LDL-C lowering effects similar to statins despite greater lipid-altering effects relative to other members of this class, suggesting that potent CETP inhibition by itself might not lead to increased blood pressure. Expand
Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male
TLDR
Assessment of the pharmacokinetic and pharmacodynamic properties and tolerability of multiple oral once-daily or twice-daily doses of sitagliptin found a finding consistent with near-maximal acute glucose lowering in preclinical studies. Expand
Tolerability of Fosaprepitant and Bioequivalency to Aprepitant in Healthy Subjects
TLDR
Fosaprepitant up to 150 mg (1 mg/mL) was generally well tolerated and AUC bioequivalent to aprepitant 125 mg; the 90% confidence interval for the geometric mean ratio of aprepant AUC fell within prespecified equivalence bounds of 0.80 to 1.25. Expand
Physiologically Based Modeling of Pravastatin Transporter-Mediated Hepatobiliary Disposition and Drug-Drug Interactions
TLDR
PBPK model of pravastatin, based on in vitro transport parameters and scaling factors, was developed and can be used to predict the pharmacokinetics and DDIs associated with hepatic uptake transporters. Expand
Effect of Different Durations and Formulations of Diltiazem on the Single‐Dose Pharmacokinetics of Midazolam: How Long Do We Go?
TLDR
The data suggest that dosing diltiazem XR for 2 days predicts the change in midazolam AUC as reliably as 5 days of XR dosing and 2 days of CR dosing. Expand
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