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-Gluc^{^a}	XK469-Gluc	521.0946	—	X	X

—, Not detected.
↵^a Multiple glucuronide conjugates were observed.
X; observed metabolite.