Table 2

Summary of Inhibition of FLT3 Phosphorylation in all Patients

PatientDose (mg)FLT3 genotypeFLT3 inhibitionCmax (ng/ml)Tmax (h)Modulation (strong)
150D835YWeak (25)1541/3
2WTWeak (49)1224
3ITDStrong (61, 87*)348
4100ITDStrong (40, 69*)16101/2
5WTNE366
6WTNo4510
7150WTNo75100/3
8WTNo684
9WTNo7110
10200ITDStrong (78, 78*)5143/5
11WTStrong (85)6012
12WTNo1044
14WTNo5510
15WTNE10212
16WTNE848
22G846SStrong (67)1396
13250WTStrong (96)11183/3
17WTStrong (70)1184
18WTNE604
19WTNE1158
20WTNE8010
21WTStrong (80)1398
23300WTStrong (72)20183/4
24WTNE768
25WTNE1086
27WTWeak (35)4810
28WTStrong (71)1484
29WTStrong (89)1168
26350WTStrong (70)170101/1
  • a Strong and weak inhibition are defined as 50–100% and 20–50% inhibition of predose phosphorylation, respectively. Numbers in parentheses denote maximum inhibition observed for each patient. For FLT3-ITD patients, inhibition of both upper and lower FLT3 species combined and lower band only* are shown. ITD sequences were VDFREYE (592–598), KYFYVDFRE (588–596); and DFREY (593–597) for patients 3, 4, and 10, respectively. NE, not evaluable.