TABLE 4

Mean AUC0–72 h and percentage of total radioactivity AUC0–72 h values of mavoglurant and its metabolites in the plasma of four healthy male human subjects after a single oral dose of 200 mg of [14C]mavoglurant

The components are listed in the order of the chromatographic elution. Mean ± S.D., n = 4.

Metabolite/ComponentMol.wt.aAUC0–72 hbPercentage of Total Radioactivity AUC0–72 h
g/molnmol·h/l
M14351.44536 ± 19489.21 ± 5.85
M13301.3231 ± 380.439 ± 0.175
M15285.34688 ± 22839.15 ± 5.36
M16271.4628 ± 4441.21 ± 1.02
M18347.44766 ± 9398.77 ± 2.4
M19 + M20c418.5/505.52557 ± 17594.18 ± 1.54
M22505.52147 ± 4493.89 ± 0.65
M23 + M24c345.4/400.41689 ± 7133.14 ± 1.72
M25 + M26c255.4/409.51964 ± 13923.51 ± 2.75
M27359.41829 ± 17162.86 ± 1.7
M28375.4547 ± 1910.956 ± 0.14
M7329.4462 ± 4350.734 ± 0.556
M6343.46996 ± 163812.5 ± 1.63
M29505.5639 ± 64.71.18 ± 0.22
M5489.51917 ± 5683.42 ± 0.75
M3329.41483 ± 10302.43 ± 0.88
M2329.41002 ± 9261.56 ± 0.93
M1329.41706 ± 16592.63 ± 1.7
M30345.43501 ± 29125.54 ± 2.8
M31357.41153 ± 2761.99 ± 0.8
Mavoglurant313.47197 ± 666711.2 ± 7.67
Mavoglurant (by LC-MS/MS)d313.47098 ± 6917NA
M12327.4549 ± 3880.821 ± 0.355
Sum of additional components—578 ± 6350.896 ± 0.724
Total components detected—52,339 ± 18,50891.5 ± 4.55
Lost during sample processing—4490 ± 23588.45 ± 4.53
Total components in the original sample—56,829 ± 17,844100

  • NA, not applicable.

  • ↵a The molecular weights (Mol.wt.) of the components are calculated from the elemental composition listed in Table 2.

  • ↵b To obtain ng·h/ml units, multiply the AUC value with the metabolite’s mol.wt. divided by 1000; for total radioactivity, the reference mol.wt. of mavoglurant (313.4) divided by 1000 is used to obtain ng-eq·h/ml units.

  • ↵c Coeluting metabolites. The relative percentages in the peak could not be quantified by LC-MS with off-line radioactivity detection.

  • ↵d Mavoglurant AUC0–72 h calculated from values measured by LC-MS/MS.