entinostat + hydroxychloroquine + regorafenib

This is a combination therapy consisting of three drugs: regorafenib (an antiangiogenic tyrosine kinase inhibitor), hydroxychloroquine (HCQ, an autophagy inhibitor), and entinostat (a histone deacetylase inhibitor). The combination was investigated based on the hypothesis that HCQ and entinostat would be tolerable with regorafenib and potentiate the antitumor response in metastatic colorectal cancer. The rationale was that antiangiogenic therapy causes hypoxic stress within tumor cells, which activates autophagy as a survival mechanism. Entinostat increases dependence on autophagy through epigenetic mechanisms, while hydroxychloroquine blocks autophagy by blunting lysosomal acidification.

Other names

HCQ + entinostat + regorafenibhydroxychloroquine + entinostat + regorafenib