M.L Constanzer

TL;DR: Practical, experimental approaches for studying, identifying, and eliminating the effect of matrix on the results of quantitative analyses by HPLC-MS/MS are described and it is demonstrated that, for the investigational drug under study, the matrix effect was clearly observed when ISP interface was utilized but it was absent when the HN interface was employed.

TL;DR: Positron emission tomography imaging with [(18)F]SPA-RQ allows brain NK( 1) receptor occupancy by aprepitant to be predicted from plasma drug concentrations and can be used to guide dose selection for clinical trials of NK(1) receptor antagonists in central therapeutic indications.

TL;DR: 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.

TL;DR: The effect of aprepitant on in vivo CYP3A4 activity in humans with oral midazolam used as a sensitive probe of CYP4 activity was evaluated in this study.

TL;DR: The pharmacokinetics of aprepitant administered following the 3‐day regimen recommended to prevent CINV, which was generally well tolerated, were defined and consistent daily plasma exposures of apREPitant were obtained following this regimen.