TABLE 1

In vitro and in vivo (i.v./p.o.) comparison of metabolic profiles of FK3453 in h-PXB mice and r-PXB mice

	Retention Time (Minute)	Mass	h-PXB Mice				r-PXB Mice
			In Vitro	In Vivo			In Vitro	In Vivo
			Hepatocytes	Plasma	Urine	Feces	Hepatocytes	Plasma	Urine	Feces
FK3453	20.0	M	27.5%^{^a}	+	0.1%^{^b}	0.1%^{^b}	58.4%^{^a}	+	0.1%^{^b}	1.1%^{^b}
A-M	16.5	M + 16	76.1%^{^a}	+	31.6%^{^b}	21.1%^{^b}	5.1%^{^a}	+	6.5%^{^b}	32.3%^{^b}
M1	10.0	M + 192	+	+	+	–	+	+	+	–
M2	10.5	M + 30	–	–	+	–	+	+	+	+
M3	11.8	M − 42	+	+	+	–	+	+	+	+
M4	12.4	M + 32	+	+	+	+	+	+	+	+
M5	12.5	M + 192	+	+	+	–	–	–	–	–
M6	13.2	M + 32	–	–	–	–	+	+	+	–
M7	13.5	M + 14	+	–	+	–	–	–	–	–
M8	13.7	M + 192	+	+	+	–	+	+	+	–
M9	14.8	M + 16	–	–	–	–	+	+	+	+
M10	15.6	M + 16	–	–	–	–	+	–	+	+
M11	17.2	M − 2	+	+	–	–	+	+	–	–
M12	17.4	M + 16	–	–	–	–	+	+	+	–

+, Metabolites detected by UV or MS.
–, not detected.
↵a Percentage of values of hepatocytes indicate the ratios of remaining FK3453 and formation of A-M after 2-h incubation with FK3453 (10 μM).
↵b Percentage of values of urine and feces indicate excretion ratio as percentage of dose (i.v.).