Table 3 Agents targeting CSC-associated signaling pathways and microenvironment in ongoing clinical trials

From: Targeting cancer stem cell pathways for cancer therapy

Drug name	Target	Condition	Phase	Sample size	NCT number	Current status
Hedgehog inhibitors
Vismodegib (GDC-0449)	Smoothened	Recurrent or refractory medulloblastoma	II	31	NCT00939484	Completed, has results
		Basal cell carcinoma		28	NCT01700049	Completed, has results
		Sarcoma		78	NCT01700049	Completed, has results
		Recurrent small-cell lung carcinoma		168	NCT01700049	Completed, has results
		Metastatic pancreatic cancer		98	NCT01088815	Completed, has results
		Ovarian cancer		104	NCT00739661	Completed, has results
		Metastatic colorectal cancer		199	NCT00636610	Completed, has results
Sonidegib (LDE225)		Basal cell carcinoma	II	10	NCT01350115	Completed, has results
		Relapsed medulloblastoma		20	NCT01708174	Completed, has results
		Acute myeloid leukemia		70	NCT01826214	Completed, has results
		Pancreatic adenocarcinoma		20	NCT01431794	Completed, has results
		Advanced or metastatic hepatocellular carcinoma		9	NCT02151864	Completed
		Recurrent plasma cell myeloma		28	NCT02086552	Active, not recruiting, has results
		Advanced pancreatic cancer		39	NCT01485744	Active, not recruiting
		Advanced breast cancer	I	12	NCT02027376	Completed, has results
Glasdegib		Acute myeloid leukemia	II	255	NCT01546038	Completed, has results
BMS-833923 (XL139)		Solid tumors	II	12	NCT01413906	Completed
		Small-cell lung carcinoma		5	NCT00927875	Completed
		Metastatic gastric, gastroesophageal, esophageal adenocarcinomas		39	NCT00909402	Completed
		Advanced or metastatic basal cell carcinoma		53	NCT00670189	Completed
		Leukemia		70	NCT01357655	Terminated, has results
Taladegib (LY2940680)		Localized esophageal or gastroesophageal junction cancer	II	9	NCT02530437	Active, not recruiting
Taladegib (LY2940680)		Small-cell lung carcinoma	II	26	NCT01722292	Terminated, has results
LEQ-506		Solid tumors	I	57	NCT01106508	Completed
G-024856		BCC	I
Patidegib (IPI-926)		Basal cell carcinomas	II	36	NCT02828111	Completed, has results
		Metastatic or locally advanced chondrosarcoma		105	NCT01310816	Completed
		Metastatic pancreatic cancer		122	NCT01130142	Completed
		Recurrent head and neck cancer	I	9	NCT01255800	Completed
Notch inhibitors
MK-0752	γ-Secretase	Advanced breast cancer	I	103	NCT00106145	Completed
		Pancreatic cancer	I	44	NCT01098344	Completed
		Metastatic breast cancer	I/II	30	NCT00645333	Completed, has results
RO4929097		Recurrent melanoma	II	14	NCT01196416	Completed, has results
		Advanced or metastatic sarcoma		78	NCT01154452	Completed, has results
		Recurrent renal cell carcinoma		12	NCT01141569	Completed, has results
		Advanced solid tumors		20	NCT01131234	Completed
		Recurrent and/or metastatic epithelial ovarian cancer, fallopian tube cancer, or primary peritoneal cancer		45	NCT01175343	Completed, has results
		Metastatic pancreas cancer		18	NCT01232829	Completed, has results
		Recurrent colon cancer		37	NCT01116687	Completed, has results
		Recurrent or refractory non-small-cell lung cancer		7	NCT01070927	Completed
Nirogacestat (PF-03084014)		Metastatic cancer pancreas	II	3	NCT02109445	Terminated, has results
		Fibromatosis	II	17	NCT01981551	Active, not recruiting
		Triple-negative breast neoplasms	II	19	NCT02299635	Terminated, has results
LY900009		Advanced cancer	I	35	NCT01158404	Completed, has results
Crenigacestat (LY3039478)	Pan-Notch	Advanced solid tumor	I	12	NCT02836600	Active, not recruiting
Crenigacestat (LY3039478)		T cell acute lymphoblastic leukemia, T cell lymphoblastic lymphoma	I/II	36	NCT02518113	Completed, has results
AL101		Adenoid cystic carcinoma	II	36	NCT03691207	Recruiting
CB-103		Advanced or metastatic solid tumors and hematological malignancies	I/II	165	NCT03422679	Recruiting
BMS-906024		Advanced or metastatic solid tumors	I	94	NCT01292655	Completed
BMS-906024		Lymphoblastic leukemia, acute T cell	I	31	NCT01363817	Completed
Demcizumab (OMP-21M18)	DLL4	Pancreatic cancer	II	207	NCT02289898	Completed, has results
Demcizumab (OMP-21M18)		Non-squamous, non-small-cell neoplasm of lung	II	82	NCT02259582	Completed, has results
Brontictuzumab (OMP-52M51)		Adenoid cystic carcinoma	Not applicable	1	NCT02662608	Completed, has results
Enoticumab (MEDI528)		Advanced solid malignancies	I	83	NCT00871559	Completed
MEDI0639		Solid tumors	I	58	NCT01577745	Completed, has results
Wnt inhibitors
Ipafricept (OMP-54F28)	Wnt receptor	Solid tumors	I	26	NCT01608867	Completed
		Pancreatic cancer	I	26	NCT02050178	Completed
		Ovarian cancer	I	37	NCT02092363	Completed
		Hepatocellular cancer	I	10	NCT02069145	Completed
Vantictumab (OMP-18R5)		Metastatic breast cancer	I	37	NCT01973309	Completed
		Solid tumors	I	35	NCT01345201	Completed
		Pancreatic cancer	I	30	NCT02005315	Completed
PRI-724	β-Catenin/CBP	Colorectal adenocarcinoma	II	0	NCT02413853	Withdrawn
		Acute myeloid leukemia		49	NCT01606579	Completed
		Solid tumors		23	NCT01302405	Terminated
		Advanced pancreatic cancer		20	NCT01764477	Completed
CWP232291		Acute myeloid leukemia	I	69	NCT01398462	Completed
CWP232291		Multiple myeloma	I	25	NCT02426723	Completed
LGK974	Porcupine	Metastatic colorectal cancer	I	20	NCT02278133	Completed
LGK974		Pancreatic cancer	I	170	NCT01351103	Recruiting
ETC-1922159		Solid tumors	I	65	NCT02521844	Active, not recruiting
Other signaling pathways inhibitors
Galunisertib (LY2157299)	TGF-β	Prostate cancer	II	60	NCT02452008	Recruiting
LY3200882		Colorectal cancer	II	31	NCT04031872	Not yet recruiting
AVID200		Malignant solid tumor	I	36	NCT03834662	Recruiting
Trabedersen (AP 12009)		Pancreatic neoplasms	II	62	NCT00844064	Completed
		Breast cancer		16	NCT01959490	Completed, has results
		Glioblastoma		141	NCT00431561	Completed
Fresolimumab (GC1008)		Non-small-cell lung carcinoma	II	60	NCT02581787	Recruiting
		Metastatic Breast Cancer		23	NCT01401062	Completed, has results
		Carcinoma Renal cell Melanoma		29	NCT00356460	Completed
Vactosertib (TEW-7197)		Advanced-stage solid tumors	I	35	NCT02160106	Completed
NIS793		Breast cancer Lung cancer Hepatocellular cancer	I	220	NCT02947165	Recruiting
Ruxolitinib	JAK	Metastatic breast cancer	III	29	NCT01594216	Completed
Ruxolitinib		Myeloproliferative neoplasms	III	309	NCT00952289	Completed, has results
AZD4205		Advanced non-small-cell lung cancer	II	120	NCT03450330	Recruiting
SAR302503		Hematopoietic neoplasm	II	97	NCT01523171	Completed
SB1518	JAK/FLT3	Acute myelogenous leukemia	II	76	NCT00719836	Completed
PI3K inhibitors
Alpelisib	PI3K	Advanced breast cancer	II	90	NCT03386162	Recruiting
Buparlisib (BKM120)		Triple-negative metastatic breast cancer	II	50	NCT01629615	Completed
BYL719		Advanced or metastatic gastric cancer	I	18	NCT01613950	Completed
SF1126		Advanced or metastatic solid tumors	I	44	NCT00907205	Completed
SAR245409	PI3K and mTOR	Advanced or metastatic solid tumors	I	146	NCT01390818	Completed, has results
EGFR inhibitors
Bevacizumab	EGFR	Breast cancer	I	75	NCT01190345	Completed
Matuzumab (EMD 72000)		Esophageal cancer	II	72	NCT00215644	Completed, has results
Matuzumab (EMD 72000)		Non-small-cell lung carcinoma	II	150	NCT00111839	Completed, has results
Metabolism inhibitors
Venetoclax (ABT-199)	BCL-2	Acute myelogenous leukemia	II	32	NCT01994837	Completed, has results
Pegzilarginase	Recombinant pegylated arginase	Small-cell lung cancer	II	84	NCT03371979	Active, not recruiting
131I-TLX-101	LAT1	Glioblastoma multiforme	II	44	NCT03849105	Recruiting
Rifampicin	FAS	Advanced solid tumors	I	36	NCT03077607	Completed, has results
TVB-2640	FAS	Advanced breast cancer	II	80	NCT03179904	Recruiting
IM156	AMPK	Advanced solid tumor	I	36	NCT03272256	Recruiting
Telaglenastat	Glutaminase	Solid tumors	II	85	NCT03965845	Recruiting
CB-1158	Arginase	Advanced solid tumors	II	5	NCT03361228	Completed
Niche inhibitors
Plerixafor (Mozobil)	CXCR4	Advanced pancreatic, ovarian, and colorectal cancers	I	26	NCT02179970	Completed
BL-8040		Metastatic pancreatic adenocarcinoma	II	23	NCT02907099	Active, not recruiting
BKT140		Multiple myeloma	II	16	NCT01010880	Completed
BMS-936564		Relapsed/refractory multiple myeloma	I	46	NCT01359657	Completed
BMS-936564		Acute myelogenous leukemia	I	98	NCT01120457	Completed
LY2510924		Solid tumor	I	9	NCT02737072	Terminated, has results
MSX-122		Refractory metastatic or locally advanced solid tumors	I	27	NCT00591682	Suspended
USL311		Advanced solid tumors and relapsed/recurrent Glioblastoma multiforme	II	120	NCT02765165	Recruiting
AMD3100		Acute myeloid leukemia	II	52	NCT00512252	Completed, has results
Reparixin	CXCR1/2	Breast cancer	II	20	NCT01861054	Terminated
Defactinib (VS-6063)	FAK	Non-small-cell lung cancer	II	55	NCT01951690	Completed

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Table 3 Agents targeting CSC-associated signaling pathways and microenvironment in ongoing clinical trials

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