TABLE 3

Estimated AUC_0–120h of siponimod and metabolites in the plasma of healthy men after a single 10-mg oral dose of [¹⁴C]siponimod

The AUC_{0–120 h} is mean ± S.D., N = 4 (nmol_*h/l), mean values of N = 4 subjects and individual values.

Peak	Compound/Metabolite	AUC_{0–120 h}	% of Total [¹⁴C]
M3	Glucuronide of M5	1850 ± 268	18.4 ± 5.11
M5	Formed by hydroxylation	156 ± 29.0	1.51 ± 0.34
M6	Formed by hydroxylation	170 ± 39.9	1.63 ± 0.33
M7	Formed by hydroxylation	282 ± 87.8	2.75 ± 1.11
P29.6	Unknown	378 ± 103	3.72 ± 1.49
P30.5	Unknown	192 ± 57.4	1.82 ± 0.47
P73.0	Formed during sample processing	190 ± 91.7	1.74 ± 0.62
Siponimod	Parent drug	6320 ± 2920	57.1 ± 5.91^{^a}
	Sum of unknown trace metabolites	204 ± 29.8	2.02 ± 0.59
	Lost during sample processing and HPLC^{^b}	1040 ± 578	9.30 ± 2.10
Total [¹⁴C]^{^c}		10800 ± 3700	100 ± (NC)

AUC_{0–120 h}, area under the concentration-time curve from 0 to 120 h; NC, not calculable, not meaningful.
↵^a Here, 58.8%, including P73 formed by methyl-esterification of parent drug during sample preparation.
↵^b This might be due to the formation of metabolite M17, which has a long half-life.
↵^c Total of radiolabeled components.