TABLE 5

Amounts of mavoglurant and its metabolites excreted in urine and feces, derived from metabolite profiles

Data are from four healthy male subjects treated with a single oral dose of 200 mg of [¹⁴C]mavoglurant. Radioactivity and mavoglurant were determined by liquid scintillation counting and LC-MS/MS, respectively. The components are listed in the order of the chromatographic elution. The letters A, B, C, D, and E indicate the formation of metabolites through corresponding metabolic pathways. The metabolic pathways are shown in Fig. 8. Mean ± S.D., n = 4.

Metabolite/Component	Pathway	Urine	Feces	Total
		0–96 h
M14^a	NAS	3.41 ± 1.51	ND	3.41 ± 1.51
M13^a	NAS	0.25 ± 0.054	ND	0.25 ± 0.054
M15	NAS	6.18 ± 3.68	ND	6.18 ± 3.68
M16	NAS	0.757 ± 0.323	ND	0.757 ± 0.323
M17	NAS	0.562 ± 0.161	ND	0.562 ± 0.161
M18	A	1.44 ± 0.437	ND	1.44 ± 0.437
M19 + M20^b	A/B	4.04 ± 1.72	2.95 ± 3.5	6.99 ± 1.87
M21 + M22^c	A/A	1.32 ± 0.579	ND	1.32 ± 0.579
M23 + M24^c	NAS/A	1.25 ± 0.475	0.448 ± 0.522	1.7 ± 0.985
M26 + M25^c	B/C	2.81 ± 1.99	ND	2.81 ± 1.99
M27	NAS	1.02 ± 0.283	0.766 ± 0.894	1.79 ± 1.14
M28	NAS	0.569 ± 0.184	0.689 ± 0.563	1.26 ± 0.637
M6	A	7.31 ± 1.4	5.46 ± 4.04	12.8 ± 5.21
M29	NAS	0.601 ± 0.126	ND	0.601 ± 0.126
M5	E	0.518 ± 0.187	ND	0.518 ± 0.187
M3	E	ND	0.96 ± 0.574	0.96 ± 0.574
M30	D	0.173 ± 0.109	ND	0.173 ± 0.109
Mavoglurant	—	ND	40.8 ± 14.9	40.8 ± 14.9
Sum of trace components	—	2.08 ± 1.01	ND	2.07 ± 1.01
Total of metabolites/components	—	34.3 ± 8.88	52.1 ± 13.1	86.3 ± 5.24
Total excretion in time period (0–96 h)	—	35.5 ± 9.48	55.8 ± 13.8	91.3 ± 4.63

NAS, not assignable; ND, not detected.
↵^a Coeluting metabolites. Their relative percentages could be calculated based on MS-signals.
↵^b M19 and M20 are coeluting in urine. In feces, only M19 was detected.
↵^c Coeluting metabolites. Their relative percentage could not be quantified by LC/MS with on-or off-line radioactivity detection.