Table 3.

Pharmacokinetic results from single-dose analysis

Median (range)Mean (SD) (CV%)
Dose, mgnTmax, hCmax, ng/mLCmax/D, ng/mL/mgTlast, hAUClast, h ng/mLAUClast/D, h ng/mL/mg
21/730322.2 (8.0–23.8)1,500 (615) (40.9)50.1 (20.5) (40.9)23.2 (0.853) (3.7)27,600 (12,800) (46.5)919 (427) (46)
6038.0 (8.0–24.1)1,910 (1,320) (69.2)31.8 (22.0) (69.2)24.2 (0.347) (1.4)39,000 (24,500) (62.8)649 (409) (63.0)
12044.1 (2.0–8.0)8,960 (3,230) (36.1)74.7 (26.9) (36.1)24.1 (0.199) (0.8)1,79,000 (53,200) (29.7)1,494 (443) (30.0)
22538.0 (8.0–8.1)8,260 (4,610) (55.9)36.7 (20.5) (55.9)23.3 (1.29) (5.5)1,55,000 (84,700) (54.8)687 (377) (55.0)
40096.5 (4.0–25.4)17,300 (14,000) (80.9)43.3 (35.1) (80.9)23.7 (0.748) (3.2)3,01,000 (2,50,000) (83.3)752 (414) (55.0)
600198.0 (4.0–23.9)15,600 (8,550) (54.7)26.1 (14.2) (54.7)21.7 (6.09) (28.1)2,74,000 (1,86,000) (67.9)456 (309) (68.0)
90038.0 (4.0–23.7)28,100 (19,100) (68.0)31.2 (21.2) (68.0)24.0 (0.376) (1.56)5,90,000 (4,20,000) (71.2)656 (467) (71.0)
CDD10044.1 (4.0–8.0)5,200 (1,730) (33.2)52.0 (17.3) (33.2)24.4 (0.692) (2.8)1,03,000 (35,500) (34.4)1,030 (353) (34.0)
40034.0 (2.0–24.0)12,500 (4,340) (34.8)31.1 (10.8) (34.8)24.2 (0.337) (1.4)2,50,000 (77,000) (30.1)816 (713) (31.0)
600218.0 (2.0–24.4)13,900 (10,800) (77.9)23.2 (18.1) (77.9)23.3 (3.52) (15.1)2,51,000 (1,93,000) (76.9)418 (322) (77.0)

Abbreviations: 21/7, 21 consecutive days on treatment followed by 7 days off treatment; AUClast, area under the concentration–time curve up to the last measurable concentration; Cmax, maximum concentration; CDD, continuous once-daily dosing; CV, coefficient of variation; D, dose normalized; tmax, time to maximum concentration; t1/2, z, terminal elimination half-life.