Table 3.

Summary of pharmacokinetics of RO4987655 in patients following oral administration

Day 1Day 15
RegimenNAUC0–12h ng·h/mL (% CV)Cmax ng/mL (% CV)t½ h (% CV)NAUC0–12h ng·h/mL (% CV)Cmax ng/mL (% CV)t½ h (% CV)Accumulation indexa
1.5 mg (twice daily)4278 (27%)88.0 (30%)4.7 (12%)4460 (18%)105 (30%)6.0 (19%)1.65
2.0 mg (twice daily)3321 (7%)72.9 (64%)3.7 (50%)3629 (12%)129 (25%)7.6 (47%)1.96
3.0 mg (twice daily)4596 (44%)171 (39%)3.4 (20%)4861 (47%)176 (58%)4.0 (20%)1.15
4.0 mg (twice daily)4608 (38%)142 (51%)4.2 (11%)41053 (13%)183 (61%)6.1 (16%)1.90
5.0 mg (twice daily)4797 (64%)209 (89%)3.3 (20%)41157 (60%)201 (66%)3.8 (8%)1.45
6.5 mg (twice daily)31005 (35%)207 (51%)3.3 (12%)41458 (21%)282 (36%)3.9 (28%)1.45
8.5 mg (twice daily)b91660 (39%)425 (50%)3.4 (25%)92577 (48%)530 (53%)8.0 (157%)1.50
10.5 mg (twice daily)42282 (43%)601 (66%)3.7 (66%)22638 (12%)399 (45%)8.1 (87%)1.16

Abbreviations: CV, coefficient of variation; t½, plasma half-life.

  • aAccumulation index represents AUCday 15/AUCday 1.

  • bMTD.