Chloroquine (CQ) and hydroxychloroquine (HCQ) are antimalarial drugs with potential anticancer properties, primarily through their ability to suppress autophagy. This review summarizes experimental and clinical studies on the use of CQ and HCQ in combination with conventional chemotherapy drugs to enhance cancer treatment. CQ and HCQ have been tested in various malignancies, including breast, ovarian, pancreatic, and lung cancers, showing increased sensitivity to cytotoxic agents and reduced tumor growth. They inhibit autophagy, which can protect cancer cells from chemotherapy, thereby enhancing treatment efficacy. However, clinical trials have shown inconsistent results, possibly due to factors such as patient variability and disease stage. Despite this, CQ and HCQ remain promising adjuvants in cancer therapy, particularly when combined with drugs like doxorubicin, paclitaxel, cisplatin, gemcitabine, and tyrosine kinase inhibitors. The development of more specific autophagy inhibitors is needed to improve therapeutic outcomes and reduce side effects. Overall, CQ and HCQ show potential as effective adjuvants in cancer treatment, but further research is required to optimize their use.Chloroquine (CQ) and hydroxychloroquine (HCQ) are antimalarial drugs with potential anticancer properties, primarily through their ability to suppress autophagy. This review summarizes experimental and clinical studies on the use of CQ and HCQ in combination with conventional chemotherapy drugs to enhance cancer treatment. CQ and HCQ have been tested in various malignancies, including breast, ovarian, pancreatic, and lung cancers, showing increased sensitivity to cytotoxic agents and reduced tumor growth. They inhibit autophagy, which can protect cancer cells from chemotherapy, thereby enhancing treatment efficacy. However, clinical trials have shown inconsistent results, possibly due to factors such as patient variability and disease stage. Despite this, CQ and HCQ remain promising adjuvants in cancer therapy, particularly when combined with drugs like doxorubicin, paclitaxel, cisplatin, gemcitabine, and tyrosine kinase inhibitors. The development of more specific autophagy inhibitors is needed to improve therapeutic outcomes and reduce side effects. Overall, CQ and HCQ show potential as effective adjuvants in cancer treatment, but further research is required to optimize their use.