TABLE 3

IC50 derived from dose-response curves of BTK and TEC occupancy in human CLL PBMCs

DrugPBMC DonorBTK IC50 (nM)TEC IC50 (nM)BTK/TEC SelectivityaMean ± S.D.
IbrutinibDonor 11.391.961.411.32 ± 0.27
Donor 21.452.121.46
Donor 31.301.290.99
Donor 41.371.931.41
AcalabrutinibDonor 17.8610.251.301.09 ± 0.11
Donor 211.9311.530.97
Donor 39.7910.191.04
Donor 410.8411.521.06
  • a BTK/TEC selectivity is defined as TEC IC50/BTK IC50.