Table 1.

Checkpoint abrogators in clinical trials

CompoundTargetAgents in combinationCancer typesStatus (number of trials)
UCN-01Chk1, other kinasesMonotherapyRefractory systemic anaplastic large cell and mature T-cell lymphomaPhase II, active
IrinotecanResistant solid tumors or locally recurrent or metastatic triple-negative breast cancerPhase I, active
PerifosineRelapsed or refractory acute leukemia, chronic myelogenous leukemia, high-risk myelodysplastic syndromePhase I, active
MonotherapyAdvanced or metastatic renal cell carcinomaPhase II, closed
MonotherapyMetastatic melanoma phase II, closed
MonotherapyRefractory solid tumors or lymphomaPhase I, closed
MonotherapyAdvanced solid tumors and chronic lymphoproliferative disordersPhase I, completed
FludarabineRelapsed or refractory chronic lymphocytic leukemia or small lymphocytic lymphomaPhase I and II, closed
FludarabineRecurrent or refractory low-grade or indolent lymphoid malignanciesPhase I, completed
FluorouracilGemcitabine-refractory metastatic pancreatic cancerPhase II, completed
FluorouracilAdvanced or refractory solid tumorsPhase I, completed
FluorouracilMetastatic or unresectable solid tumorsPhase I, completed
+ Leucovorin (triple)
TopotecanRecurrent, persistent, or progressive advanced ovarian cancersPhase I and II, completed
TopotecanRelapsed or progressed small cell lung cancer platinum-based chemotherapyPhase II, closed
CytarabineRefractory or relapsed acute myelogenous leukemia or myelodysplastic syndromePhase I, closed
CisplatinAdvanced solid tumorsPhase I (2), completed
CarboplatinAdvanced solid tumorsPhase I, completed
GemcitabineUnresectable or metastatic adenocarcinoma of the pancreasPhase I, completed
PrednisoneRefractory solid tumors or lymphomasPhase I, closed
AZD7762Chk1, Chk2GemcitabineAdvanced solid malignanciesPhase I (2), active
IrinotecanAdvanced solid malignanciesPhase I, active
LY2603618Chk2GemcitabinePancreatic cancerPhase I, active
PemetrexedMetastatic non-small cell lung cancerPhase I, active
CBT501Chk1, Chk2CisplatinSolid tumorsPhase I, active (1)/closed (1)
CisplatinMalignant pleural mesotheliomaPhase II, active
PemetrexedNon-small cell lung cancerPhase II, active
+ Cisplatin (triple)
PF-00477736Chk1, Chk2GemcitabineAdvanced solid tumorsPhase I, active
SCH 900776Chk1GemcitabineSolid tumors or lymphomaPhase I, active
CytarabineAcute leukemiaPhase I, active
XL844Chk1, Chk2GemcitabineAdvanced malignancies (solid tumor and lymphoma)Phase I, closed
MK-1775Wee1MonotherapyAdvanced solid tumorsPhase I, active
Gemcitabine
Cisplatin
Carboplatin
7-AADHsp90, Chk1IrinotecanSolid tumorsPhase I, active