Table 2.

Results of noncompartmental analysis for losmapimod and the primary metabolite GSK198602

Parameter	Compound	Dose	Geometric mean	95% CI	CV%
AUC0–∞ (μg h l−1)	Losmapimod	1 mg IV	54.09	38.4, 76.2	21.8
		3 mg IV	171.1	148, 198	23.3
		15 mg PO	528.0	428, 652	34.1
	GSK198602	1 mg IV	30.67	23.5, 40.0	16.8
		3 mg IV	216.5	178, 263	31.2
		15 mg PO	1096	875, 1372	36.5
AUC0–t (μg h l−1)	Losmapimod	1 mg IV	48.56	36.2, 65.1	18.6
		3 mg IV	161.7	141, 186	22.1
		15 mg PO	421.0	351, 506	29.5
	GSK198602	1 mg IV	22.42	14.6, 34.5	27.5
		3 mg IV	184.8	155, 221	28.4
		15 mg PO	717.9	616, 837	24.4
Cmax (μg l−1)	Losmapimod	1 mg IV	18.00	8.91, 36.3	46.4
		3 mg IV	59.38	46.1, 76.5	41.5
		15 mg PO	45.90	36.7, 57.4	36.3
	GSK198602	1 mg IV	5.228	4.01, 6.81	16.7
		3 mg IV	22.24	20.1, 24.6	16.1
		15 mg PO	67.31	55.5, 81.6	30.9
Tmax (h)*	Losmapimod	1 mg IV	0.250	0.17, 0.27	—
		3 mg IV	0.250	0.18, 0.75	—
		15 mg PO	3.500	2.00, 6.00	—
	GSK198602	1 mg IV	1.000	0.75, 1.50	—
		3 mg IV	1.515	1.00, 6.00	—
		15 mg PO	4.000	2.00, 10.00	—
t1/2 (h)	Losmapimod	1 mg IV	8.328	4.84, 14.3	35.2
		3 mg IV	6.488	5.14, 8.20	38.1
		15 mg PO	9.439	7.37, 12.1	40.6
	GSK198602	1 mg IV	4.014	2.96, 5.44	19.2
		3 mg IV	7.312	5.83, 9.18	36.9
		15 mg PO	12.17	16.4, 0.474	50.2
VDss (l)	Losmapimod	1 mg IV	171.8	139, 212	13.3
		3 mg IV	110.8	96.1, 128	22.7
CL (l h−1CL/F (l h−1)	Losmapimod	1 mg IV	18.49	13.1, 26.0	21.8
		3 mg IV	17.54	15.2, 20.3	23.3
		15 mg PO	28.41	23.0, 35.1	34.1

^*T_max is presented as the median and range.