Table 1.

Checkpoint kinase inhibitors in clinical trials

AgentStructureChk1 IC50 (nmol/L)Chk2 IC50 (nmol/L)CombinationTumor settingPhaseStatus
UCN-01*Embedded Image1010IrinotecanBreast, gastric, head/neck, NSCL, small cell, ovarian, pancreas, prostateIOngoing
CisplatinBladder, melanoma, thyroidI
TopotecanLungII
XL844Structure undisclosed2.20.2CLLITerminated
GemcitabineAggressive or indolent NHL, solid tumorsIOngoing
PF-00477736Embedded Image0.49 (Ki)47 (Ki)GemcitabineSolid tumorsIOngoing
AZD7762Embedded Image5<10GemcitabineSolid tumorsIOngoing
IrinotecanSolid tumorsI
  • Abberviations: NSCL, non–small cell lung; CLL, chronic lymphocytic leukemia; NHL, non–Hodgkin's lymphoma.

  • * Nonselective kinase inhibitor with known activity against checkpoint kinases—only ongoing trials in combination with DNA-damaging agents listed.