Table 2.

DLTs and dose modifications during dose escalation (stage 1)

DLTsSignificant AEs either reaching DLT criteria outside first cycle or necessitating dose reductions/discontinuations#
DoseNEvents (n)DescriptionEvents (n)Reason
2 mg300
21/28 d
4 mg300
21/28 d
8 mg300
21/28 d
16 mg300
21/28 d
32 mg702G3 fatigue
21/28 dG3 hepatic encephalopathy#
40 mg41G4 hyperglycemia1G4 hyperglycemia#
21/28 d
40 mg1406G3 liver dysfunction (n = 2)
28/28 dG3 pneumonitis#
G3 rash (n = 2); 1#
G5 pneumonitis#
50 mg603G3 intestinal fistula#
21/28 dG3 rectal hemorrhage#
G5 colitis#
50 mg502G3 liver dysfunction (n = 2)
28/28 d
70 mg82G3 rash5G3 hyperglycemia#
21/28 dG3 hyperglycemiaG3 mucosal inflammation (n = 2); 1#
G3 pneumonitis#
G3 rash#
All563Hyperglycemia (n = 2)19Colitis
RashFatigue
Hepatic encephalopathy
Hyperglycemia (n = 2)
Intestinal fistula
Liver dysfunction (n = 4)
Mucosal inflammation (n = 2)
Pneumonitis (n = 3)
Rash (n = 3)
Rectal hemorrhage
  • #Discontinuation of apitolisib.