Antimalarial; autophagy inhibitor; endosomal acidification fusion inhibitor. In clinical trials (alongside chloroquine) for SARS-CoV-2 infection; multiple potential mechanisms, including inhibiting viral endocytosis and attenuating the "cytokine storm". Hu et al. Nat. Nanotechnol., Mar 23 2020, https://doi.org/10.1038/s41565-020-0674-9; Schrezenmeier & Dörner Nat. Rev. Rheumatol., 16:155-166, March 2020, https://doi.org/10.1038/s41584-020-0372-x.
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- Applications:Approved drug (U.S.); now approved by US FDA for COVID-19
Biochemicals & reagents
1) Boya et al. (2005), Inhibition of macroautophagy triggers apoptosis; Mol. Cell Biol., 25 1025 2) Xie et al. (2013), Coordinate autophagy and mTOR pathway inhibition enhances cell death in melanoma; PLoS One, 8 e55096 3) Pan et al. (2011), Targeting autophagy augments in vitro and in vivo antimyeloma activity of DNA-damaging chemotherapy; Clin. Cancer Res., 150 3248 4) Jeong et al. (2002), Chloroquine decreases cell-surface expression of tumor necrosis factor receptors in human histiocytic U-937 cells; Immunology, 105 83 5) Stephan et al. (2013), Successful treatment of alopecia totalis wih hydroxychloroquine: report of 2 cases; J. Am. Acad. Dermatol., 68 1048
Room Temperature (des.)
Hydroxychloroquine is a lysosomotropic agent which inhibits autophagy and triggers apoptosis in a variety of cell types (1,2). This compound augments the anticancer activity of DNA-damaging chemotherapy (3). It also has antiinflammatory activity. It decreases cell surface expression of TNFα receptors in U937 cells (4) and has been successfully used to treat alopecia (5). It is also a clinically relevant antimalaria agent. This compound is cell permeable and active in vivo.