Pharmacokinetic parameters of telithromycin in clinical interaction studies with simvastatin acid
| Perpetrator Drug | Dose | MW | [Ig] | [Cmax] or [C12 h] | fu | [C12h u] | [Iin max] | [Iin max u] |
|---|---|---|---|---|---|---|---|---|
| mg | μM | μM | ||||||
| Telithromycin (coadministered) | 800 | 812 | 22.5 | 2.76 | 0.35 | NA | 7.25 | 2.538 |
| Telithromycin (12 h apart) | 800 | 812 | NA | 0.246 | 0.35 | 0.086 | NA | NA |
[C12 h], Plasma concentration for total (bound plus unbound) drug at T = 12 h (0.2 mg/l) measured in the clinical interaction study with simvastatin acid (Study Number 1048, HMR3647 AUC profile; Ketek FDA approval package review 4); [Cmax], Cmax for total [bound plus unbound) drug measured in the clinical interaction study with simvastatin acid (Study Number 1048; Ketek FDA approval package review 4 (Clinical Pharmacology Biopharmaceutics Review Part 4, accessed via Drugs@FDA database; www.accessdata.fda.gov/drugsatfda_docs/nda/2004/21-144_Ketek_BioPharmr_P4.pdf)]; fu, median fraction unbound [taken from the Ketek drug label accessed via Drugs@FDA database; www.accessdata.fda.gov/drugsatfda_docs/label/2010/021144s014lbl.pdf]; [Ig], maximal enterocyte concentration; [Iin max], maximum hepatic inlet concentration; calculated as described in Materials and Methods using telithromycin-specific values of FaFg = 0.57 (www.accessdata.fda.gov/drugsatfda_docs/label/2010/021144s014lbl.pdf) and ka = 0.012 min (0.740 h) (Ikawa et al., 2014). NA, not applicable to DDI.