TABLE 5.

Summary of autophagy inhibitors.

Drugs	Target	Biological models	Status of the study	Biological effects	References
Chloroquine (CQ)	Lysosomal pH	Human breast cancer MCF-7 cells; human colorectal cancer cells	Approved by FDA; phase I clinical trial	Inhibition of protective autophagy by blocking autophagosome fusion and degradation; autophagy inhibition at the late stage of the pathway; evidence of preliminary antitumor activity	Sui et al. (2013)
Hydroxychloroquine (HCQ)	Lysosomal pH	Human esophageal, hepatocellular carcinoma, lung, and pancreatic cancer cells	Approved by FDA; phase I clinical trial	Inhibition of autophagosome fusion with lysosomes and autophagosome degradation; autophagy inhibition at the late stage of the pathway; induction of autophagic tumor cell death; safely dose escalated in cancer patients	Sui et al. (2013)
HCQ + tamoxifen	Lysosomes, estrogen receptor-ɑ (ERɑ)	Human breast cancer cells in female athymic mice	In vivo models; cancer cell lines; phase I clinical trial	Reduced drug resistance; In vitro and in vivo promotion of antiestrogenic therapy	Cook et al. (2014)
HCQ + temsirolimus	Lysosomes, mTOR pathway	Human renal carcinoma cell lines	Cancer cell lines	Induction of apoptosis and cell death; promotion of mitochondrial damage with mTOR down-regulation; tumor growth suppression	Lee et al. (2015)
3- methyladenine (3-MA)	Autophagosome formation, class III PI3K inhibitor	Human chronic myelogenous leukemia K562 cell line	Cancer cell lines	Inhibition on the formation of autophagosomes; autophagy inhibition at the early stage of the pathway; aggravated chromatin condensation; enhanced SDT-induced apoptosis and necrosis	Su et al. (2015)
Bafilomycin A1 (Ba A1)	Autophagolysosome formation, vacuolar-type H (+)-ATPase inhibitor	Murine sarcoma S180 cell line	Cancer cell lines	Inhibition on the fusion between autophagosomes and lysosomes; autophagy inhibition at the late stage of the pathway; enhanced SDT induced caspase-3 and PARP cleavage; enhanced SDT-induced cell death and anti-tumor effect	Wang et al. (2010a)
Monensin	Endocytic and lysosomal pH	Human non-small lung cancer NCI-H1299 cell line	Cancer cell lines	Inhibition on the fusion between autophagosomes and lysosomes; autophagy inhibition at the late stage of the pathway; enhanced cell cycle arrest and apoptosis; tumor growth suppression	Choi et al. (2013)
Wortmannin	Autophagosome formation, class III PI3K inhibitor	Hepatocytes from male wistar rats	Cells	Inhibition of autophagosome formation; potent inhibition of mammalian PtdIns 3-kinase; autophagy inhibition at the early stage of the pathway	Wang et al. (2010b)
2- (4-morpholinyl)-8-phenyl-chromone (LY294002)	Autophagosome formation, class III PI3K inhibitor	Chinese hamster ovary (CHO) cell line	CHO cell lines	Inhibition of autophagosome formation; promotion of rolipram-induced PDE4A4 aggregate/foci formation; potent inhibition of autophagic sequestration; autophagy inhibition at the early stage of the pathway	Christian et al. (2010)