Table 1.

Checkpoint abrogators in clinical trials (http://www.cancer.gov; http://www.clinicaltrial.gov)

Compound	Target	Agents in combination	Cancer types	Status (number of trials)
UCN-01	Chk1, other kinases	monotherapy	refractory systemic anaplastic large cell and mature T-cell lymphoma	Phase II, active
		irinotecan	resitant solid tumors or locally recurrent or matastic triple-negative breast cancer	Phase I, active
		perifosine	relapsed or refractory acute leukemia, CML, high risk MDS	Phase I, active
		monotherapy	advanced or metastatic renal cell carcinoma	Phase II, closed
		monotherapy	metastatic melanoma	Phase II, closed
		monotherapy	refractory solid tumors or lymphoma	Phase I, closed
		monotherapy	advanced solid tumors and chronic lymphoproliferative disorder	Phase I, completed
		fludarabine	relapsed or refractory CLL or small lymphocytic lymphoma	Phase I and II, closed
		fludarabine	recurrent or refractory low-grade or indolent lymphoid malignancies	Phase I, completed
		fluorouracil	gemcitabine-refractory metastatic pancreatic cancer	Phase II, completed
		fluorouracil	advanced or refractory solid tumors	Phase I, completed
		fluorouracil + leucovorin (triple)	metastatic or unresectable solid tumors	Phase I, completed
		topotecan	recurrent, persistent, or progressive advanced ovarian cancers	Phase I and II, completed
		topotecan	relapsed or progresed small cell lung cancer platinum-based chemotherapy	Phase II, closed
		cytarabine	refractory or relapsed AMI or MDS	Phase I, closed
		cisplatin	advanced solid tumors	Phase I(2), completed
		carboplatin	advanced solid tumors	Phase I, completed
		gemcitabine	unresectable or matastatic adenocarcinoma of the pancreas	Phase I, completed
		prednisone	refractory solid tumors or lymphomas	Phase I, closed
AZD7762	Chk1, Chk2	gemcitabine	advanced solid malignancies	Phase I (2), active
		irinotecan	advanced solid malignancies	Phase I, active
LY2603618	Chk2	gemcitabine	pancreatic cancer	Phase I, active
		pemetrexed	metastatic non-small cell lung cancer	Phase I, active
CBT501	Chk1, Chk2	cisplatin	solid tumors	Phase I, active (1)/closed (1)
		cisplatin	malignant pleural mesothelioma	Phase II, active
		pemetrexed + cisplatin (triple)	non-small cell lung cancer	Phase II, active
PF-00477736	Chk1>Chk2	gemcitabine	advanced solid tumors	Phase I, active
SCH 900776	Chk1	gemcitabine	solid tumors or lymphoma	Phase I, active
		cytarabine	acute leukemia	Phase I, active
XL844	Chk1, Chk2	gemcitabine	advanced malignacies(solid tumor and lymphoma)	Phase I, closed
MK-1775	Wee1	monotherapy	advanced solid tumors	Phase I, active
		gemcitabine
		cisplatin
		carboplatin
7-AAD	Hsp90, Chk1	irinotecan	solid tumors	Phase I, active