Fig. 2: PK-PD analysis of BI 894999 in patient samples.
From: Therapeutic impact of BET inhibitor BI 894999 treatment: backtranslation from the clinic
a Day 1 BI 894999 plasma concentration-time profiles from patients treated under Sch B (orange line) or Sch C (blue line). Mean Cmax of 5 nM for 55 patients in Sch B (MTD at 2.5 mg) and of 19 nM for 19 patients in Sch C (MTD at 6/3 mg) are displayed. b Nanostring analysis of pathway modulation markers HEXIM1 and HIST2H2BF. Fold change 2 h, 4 h, 8 h and 23.5 h after Day 1 treatment are plotted. c Details for clinical schedules. MTD was determined for NC, but not yet for DLBCL. d Measurement of platelet counts comparing Sch B and Sch C at different doses including MTD. Better tolerability at an increasing cumulative dose (over 6 weeks) in Sch C (72 mg) compared to Sch B (70 mg). Red boxes indicate the Nadir platelet counts at the MTD levels for Sch B (2.5 mg) and Sch C (6/3 mg).
