Table 2.

Plk1 inhibitors in clinical trials ¹.

Compound	Clinical Trials	Current Status	Conditions	Interventions	Outcomes 2	Refs.
BI 2536	11 Clinical trials	Phase I/II 10 Completed 1 Terminated	Advanced Solid Tumors, Acute Myeloid Leukemia, Non-Hodgkin’s Lymphoma	Monotherapy	Best responses were CR for acute myeloid leukemia and non-Hodgkin’s lymphoma; PR for non-small-cell lung cancer, pancreatic cancer, acute myeloid leukemia, and non-Hodgkin’s lymphoma	[40,41,42,43,44]
				Combination with Pemetrexed and Gemcitabine	Best response was PR for adenocarcinoma and squamous cell carcinoma
BI 6727 (Volasertib)	26 Clinical trials	25 Phase I/II 12 Completed 4 Terminated 6 Withdrawn 3 Ongoing	Acute Myeloid Leukemia Pediatric Patients with Advanced Cancers, Myelodysplastic Syndromes, Non-Hodgkin’s Lymphoma, Urothelial, Ovarian, Lung Pancreatic, Colorectal and Prostate Cancer	Monotherapy	Best responses were CR for acute myeloid leukemia; PR for non-small cell lung cancer, melanoma, ovarian cancer, acute myeloid leukemia, gastric cancer, and urothelial cancer	[46,47,48,49,50,51,52,53,54,55]
				Combination with Cytarabine, Pemetrexed, Azacitidine, Afatinib, Decitabine, Daunorubicin, Nintedanib, Mitoxantrone and Itraconazole	Best responses were CR for breast cancer in combination with Nintedanib, PR for non-small-lung cancer in combination with Pemetrexed, Nintedanib, Afatinib, and Carboplatin, PR for head and neck carcinoma in combination with Afatinib, PR for undifferentiated follicular dendritic reticulum cell sarcoma and differentiated follicular dendritic reticulum cell retroperitoneal sarcoma in combination with Cisplatin, PR for differentiated hypopharynx carcinoma in combination with Carboplatin
		1 Phase III Ongoing	Acute Myeloid Leukemia	Combination with Cytarabine	-
ON 01910.Na (Rigosertib)	36 Clinical trials	32 Phase I/II 24 Completed 1 Terminated 2 Withdrawn 3 Recruiting/ Planned 2 Ongoing	Refractory Leukemia, Myelodysplastic Syndrome, Squamous Cell Carcinoma Acute/Chronic Myeloid Leukemia, Ovarian and Lung Cancer, Advanced Solid Tumors	Monotherapy	Best response was PR for non-Hodgkin’s lymphoma, thymic cancer, and pancreatic ductal adenocarcinoma	[57,58,59,60,61,72,73]
				Combination with Nivolumab, Cisplatin, Azacitidine, Oxaplatin, Gemcitabine and Irinotecan	Best responses were CR and mCR for myelodysplastic syndrome in combination with Azacitidine
		4 Phase III 3 Completed 1 Ongoing	Metastatic Pancreatic Adenocarcinoma, Myelodysplastic Syndromes	Monotherapy	Best responses were SD and mCR for myelodysplastic syndromes
				Combination with Gemcitabine	Best response was PR for pancreatic adenocarcinoma
GSK461364	NCT00536835	Phase I Completed	Non-Hodgkin Lymphoma, Advanced Solid Malignancies	Monotherapy	Best response was SD for esophageal and ovarian cancers and endometrial carcinoma	[63]
MK-1496	NCT00880568	Phase I Completed	Advanced Solid Tumors	Monotherapy	Best response was PR for parotid gland carcinoma and small cell lung cancer	[64]
TAK-960	NCT01179399	Phase I Terminated	Advanced Nonhematologic Malignancies	Monotherapy	Discontinued strategically by sponsor due to lack of efficacy	-
NMS-1286937/Onvansertib	4 Clinical trials	Phase I/II 1 Completed 3 Recruiting	Advanced or Metastatic Solid Tumors	Monotherapy	Best response was SD for colorectal cancer, pancreatic carcinoma with a K-RAS mutation, head and neck squamous cell carcinoma, and basal cell carcinoma	[68]
			Acute Myeloid Leukemia, Metastatic Prostate Cancer, Metastatic Colorectal Cancer with a KRAS mutation	Combination with Decitabine, Cytarabine, Abiraterone, Prednisone, FOLFIRI and Bevacizumab	-
TKM-080301 (siRNA)	3 Clinical trials	Phase I/II Completed	Hepatocellular Carcinoma, Colorectal, Pancreas, Breast and Ovarian Cancer with Hepatic Metastases, Adrenocortical Carcinoma, Neuroendocrine Tumors	Monotherapy	Best response was PR for adrenocortical carcinoma	[69,70]
CYC 140	NCT03884829	Phase I Recruiting	Acute Myeloid Leukemia, Myelodysplastic Syndromes, Acute Lymphoblastic Leukemia	Monotherapy	-	-

¹ Data collected from clinicaltrials.gov. ² CR, complete remission; mCR, marrow complete remission; PR, partial response; SD, stable disease.