Abstract: The present disclosure provides SETD2 protein inhibitors, and methods, uses, compositions, and kits for treating diseases, disorders, or conditions in a subject with a SETD2 protein inhibitor and a Second Therapeutic Agent, wherein the Second Therapeutic Agent comprises one or more BTK inhibitors, one or more anti-CD20 monoclonal antibodies, one or more alkylating agents, one or more topoisomerase II inhibitors, one or more vinca alkaloids, one or more platinum-based drugs, one or more nucleoside anticancer agents, one or more PI3K inhibitors, one or more CDK4/6 inhibitors, one or more CARM1 inhibitors, one or more inhibitors of enzymes of DNA damage repair, one or more SYK inhibitors, or one or more MEK inhibitors, or a combination thereof.

Abstract: The present disclosure provides SETD2 protein inhibitors, and methods, compositions, and kits for treating diseases, disorders, or conditions in a subject with a SETD2 protein inhibitor and, optionally, a second therapeutic agent, wherein the second therapeutic agent comprises one or more glucocorticoid receptor agonists, one or more immunomodulatory drugs, one or more proteasome inhibitors, one or more Bcl-2 inhibitors, one or more pleiotropic pathway modulators, one or more XPO1 inhibitors, one or more histone deacetylase inhibitors, or one or more EZH2 inhibitors, or a combination thereof.