Pharmacol Res. 2021 Mar 25:105582. doi: 10.1016/j.phrs.2021.105582. Online ahead of print.
Chloroquine (CQ) and hydroxychloroquine (HCQ) are the most common drugs used to relieve acute and chronic inflammatory diseases, In this article, we present a review about the use of CQ and HCQ in antitumor therapies based on related-autophagy mechanisms. These molecules break/discontinue autophagosome-lysosome fusions in initial phases and enhance antiproliferative action of chemotherapeutics. Their sensitizing effects of chemotherapy when used as an adjuvant option in clinical trials against cancer. However, human related-MDR genes are also under risk to develop chemo or radioresistance because cancer cells have ability to throw 4-aminoquinolines out from digestive vacuoles well. Additionally, they also have antitumor mechanism unrelated to autophagy, including cell death from apoptosis and necroptosis and immunomodulatory/anti-inflammatory characteristics. On the other hand, the link between some mechanisms, clinical efficacy and safety observed in vivo has not yet been fully defined.