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Table 2 Selected clinical therapeutic agents in current cancer stem cell drug treatment

From: In vitro models of cancer stem cells and clinical applications

Target Name of drug (synonyms) Mechanism of action Ref.(s)
Microenviroment/Niche Anti-CD44 monoclonal Abs CD44 activation [249]
Oblimersen sodium (G3139) Bcl2 antisense oligonucleotyde [250]
AT-101 (gossypol) Bcl2, Mcl1 inhibitor [251, 252]
ABT-263/ABT-737 Pan Bcl2 inhibitor [253]
Obatoclax (GX15-070) [254]
Sabutoclax (Bl-97C1) [255]
Anti-integrin alfa 6 monoclonal Abs Block integrin alfa 6 binding [256]
GLPG0187 Integrin alfa peptide antagonist [257]
EMD 121974 (Cilengitide) Integrin alfa beta peptide antagonist [258, 259]
Volociximab Monoclonal antibody targeting integrin alfa beta [260]
ATN-161 Integrin alfa beta peptide antagonist [261]
Pepducins CXCR4 antagonist [262]
Plerixafor (AMD3100) [263]
Neutralizing ab CXCR4 blocker [264]
Bevacizumab (Avastin) VEGF-A/VEGFR blocker [151, 265]
Cediranib/AZD2171 Tyrosine kinase inhibitor VEGFR2 [152, 266]
EphA3 monoclonal Abs EphA3 blockers Clinical trial phase I by KloBios Pharmaceuticals
Systemic infusion of enzyme PEGPH20 HA inhibitor [156]
Anthracyclines, EGFR inhibitors, cardiac glycosides, histone deacetylases, HSP90 inhibitors, microtubule targeting agents, proteasome inhibitors, topoisomerase I inhibitors HIF-1 inhibitors Reviewed in [158]
DNA vaccines Legumain, Fra-1, Stat3, FAP, HER-2 (CAFs-TAMs) Reviewed in [138]
Monoclonal Ab Sibrotozumab FAP Clinical trial phase I [267]; [139]
PAI-1 uPA/uPAR inhibitors Reviewed in [137]
Radioactive labeled Ab, siRNA Tenascin-C Reviewed in [137]
Monoclonal Ab 81C6 Clinical trial phase II [267]; [147]
NK4, anti-HGF mAbs HGF/Met [142, 143]
5-Aza-2΄-deoxycytidine DNMT1 [140]
MMPs inhibitors MMPs [141, 268]
Wnt/βcatenin pathway Anti-Frizzled (Fzd7) monoclonal antibodies (OMP-18R5) Block formation of active receptor signalling complex; binds 5 Fizzled receptors Clinical trial phase I by OncoMed; [159, 267]
Truncated Fizzled 8-Fc fusion protein (OMP-54 F28) Fzd8-Fc selectively binds Wnt ligands Clinical trial phase I by OncoMed in collaboration with Bayer Pharma AG
NSAIDs COX mechanisms [269, 270]
IWP2 o-acetyltransferase inhibitor [271]
XAV939 Tankyrase inhibitor [272]
PKF115-584 TCF/βcatenin inhibitor [273]
IWR Axin stabilizer [271]
ICG-001 CREB/βcatenin interaction inhibitor [274]
Hedgehog pathway GANT-61 Gli DNA binding inhibitor [173]
Arsenic trioxide [174]
BMS-833923 (XL139) SMO inhibitor [267]
Cyclopamine and based compounds [170]
Vismodegib (GDC-0049) [275]
mTOR/PI3K/Akt Perifosine (krx-0401, d-21266) Akt inhibitor [276]
MK-2206 [277]
GSK690693 [278]
GSK2141795 [279]
LY2780301 [280]
Rapamycin mTORC1 inhibitor [281]
Temisirolimus (CCl-779) [282]
Everolimus (SDZ RAD) [283]
Ridaforolimus (AP23573, MK-8669) [284]
OSI-027 mTORC1/2 inhibitor [285]
PP242 [286]
WAY-600 [179]
AZD8055 [287]
INK128 [288]
NVP-BKM120 PI3K inhibitor [289]
PX-866 [290]
GDC-0941 [291]
CAL-101 (GS-1101) [292]
SF1126 PI3K & mTOR inhibitor [293]
NVP-BEZ235 [294]
XL765 [295]
GDC-0980 [296]
PI-103 [297]
Metformin Inhibition of mTOR activation through AMPK [181]
Notch pathway Anti-Notch 2 and 3 monoclonal Abs (OMP-595R) Block cleavage of Notch receptor Clinical trial phase I by OncoMed
Anti-Notch 1 and 2 monoclonal Abs [298]
Anti-Notch 3 monoclonal Abs [299]
Anti-DLL4 (demcizumab) Block binding of DLLL4 to Notch receptor Clinical trial phase I by OncoMed
Anti-DLL4 monoclonal Abs (OMP-21 M18, REGN421) [160, 267]
DAPT Gamma-secretase inhibitor [300]
MRK-003 [301]
LY450139 [302]
Telomerase Imetelstat/GRN-163 L Telomerase inhibitor Clinical trial phase II by Geron Corporation; [216]
GRN-163 Antagonist of telomerase template [303]
Drug efflux PSC-833 ABCB1 inhibitor [304]
YHO-13351 ABCG2 inhibitor [305]
Redox balance and metabolism Genipin Suppression of UPC2 [228]
Phytochemicals Redox system [225, 226]
Indo-3-carbinol (I3C) Redox system (stimulates BRCA1)
Genistein Redox system (ROS scavenger, inhibitor of NFkB, Akt, PTK) [227]
CSC immunogenic responses CD133 peptide, ICT-121 Dendritic cell-based vaccine Clinical trial phase I by ImmunoCellular Therapeutics
Peptide vaccine (SL401 and SL701) Interleukin-3 receptor Clinical trial phase I and II completed by Stemline Therapeutics
VS6063 Focal adhesion kinase (inhibitor) Clinical trial phase I completed by Verastem and Pfeizer
Ipilimumab CTLA-4 blockers Clinical trial phase III by BMS/Medarex; [306]
TGN1412 CD28 agonist Clinical trial phase I [267]; [307]
MDX-1106 PD-1 antagonist Clinical trial phase I [267]; [308]
Celebrex, Rofecoxib COX2 inhibitors Reviewed in [209]
CXCR1 blocking Abs or small molecule repertaxin IL-8/CXCR1 inhibitor [210]
TGF-β type II receptor antibody or SMAD4 siRNA TGF-β/SMAD 4 [211]
Stemness BBI608 STAT3 inhibitor Clinical trial phase III [135]
BBI503 Nanog inhibitor
miRNA based therapies let-7 anti-sense oligos H-RAS and HMGA2 [197]
miR200c Bmi-1, ZEB1 [199201]
miR-34a CD44 activation [202]