Article Figures & Data
Figures
- Fig. 1.
(A) Extracted ion chromatograms showing the metabolite profile of timolol following incubations in human suspended hepatocytes (4 hours) and the HµREL model (up to 7 days). (B) Proposed metabolic pathways of timolol. Metabolites highlighted in boxes are consistent with previously published human metabolite data. In vivo data were obtained from Tocco et al. (1980).
- Fig. 2.
(A) Extracted ion chromatograms showing the metabolite profile of meloxicam following incubations in human suspended hepatocytes (4 hours) and the HµREL model (up to 7 days). (B) Proposed metabolic pathways of meloxicam. Metabolites highlighted in boxes are consistent with previously published human metabolite data. In vivo data were obtained from Schmid et al. (1995).
- Fig. 3.
(A) Extracted ion chromatograms showing the metabolite profile of linezolid following incubations in human suspended hepatocytes (4 hours) and the HµREL model (up to 7 days). (B) Proposed metabolic pathways of linezolid. Metabolites highlighted in boxes are consistent with previously published human metabolite data. In vivo data were obtained from Slatter et al. (2001).
- Fig. 4.
(A) Extracted ion chromatograms showing the metabolite profile of XK469 following incubations in human suspended hepatocytes (4 hours) and the HµREL model (up to 7 days). (B) Proposed metabolic pathways of XK469. Metabolites highlighted in boxes are consistent with previously published human metabolite data. In vivo data were obtained from Anderson et al. (2005).
Tables
- TABLE 1
Summary of metabolites observed following incubation in human hepatocyte suspension and the HµREL coculture model and comparison with reported in vivo metabolite data
Compound Metabolite Observed m/z Hepatocyte Suspension HµREL Coculture Model Reported In Vivo Timolol Parent Drug 317.1638 X X X T1 Tim + Gluc 493.1955 — X T2 Tim – C2H2 291.1485 — X X T3 Tim + 2O (a) 349.1536 — X X T4 Tim + 2O (b) 349.1537 — X X T5 Tim + O (a) 333.1592 X X X T6 Tim + O (b) 333.1589 — X Meloxicam Parent Drug 352.0417 X X X M1 Melox + O + Gluc 544.0679 — X M2 Melox Cleavage 216.0323 — Trace X M3 Melox + O 368.0368 — Trace M4 Melox-COOH 382.0154 — X X M5 Melox-OH 368.0362 Trace X X M6 Melox + 4H + O 372.0676 — X Linezolid Parent Drug 338.1505 X X X L1 Lin + 2O (a) 370.1403 Trace X X L2 Lin + 2O (b) 370.1404 X X X L3 Lin – C2H2 312.1352 — Trace X L4 Lin + H2O (a) 356.1611 — Trace X L5 Lin + H2O (b) 356.1614 — Trace X L6 Lin – C2H2O 296.1402 — Trace X L7 Lin + 2O – C2H4O 326.1147 — X X L8 Lin + O – 2H 352.1300 — Trace X XK469 Parent Drug 345.0632 X X X X1 XK469-Cys-2H (a) 464.0670 — X X2 XK469-Cys-2H (b) 464.0668 — X X3 XK469-AcetylCys-2H 506.0775 — X X4 XK469-Taur 452.0668 — X X X5 XK469-Gly 402.0844 — X X X6 XK469-OH 361.0580 Trace X X X-Gluca XK469-Gluc 521.0946 — X X —, Not detected.
↵a Multiple glucuronide conjugates were observed.
X; observed metabolite.
Data Supplement
- Supplemental Table -
Fragmentation of Parent Drug and Key Fragment Ions of Metabolites
- Supplemental Table -
