Abstract
It is well known that the immune surveillance system plays a crucial role in disease control for patients with malignant neoplasm. Although chemotherapy remains the leading approach in the treatment of hematologic malignancies, immune system-targeting antibody agents, such as immune checkpoint inhibitors, are currently under clinical investigation. While treatments with small-molecule compounds do not aim to target the immune system, some compounds potentiate treatment efficacy by enhancing the immune response to neoplasms. Immunomodulatory drugs, including thalidomide, lenalidomide, and pomalidomide, are known to be effective in reducing multiple myeloma cells by enhancing natural killer cell activity. Among the tyrosine kinase inhibitors used in the clinical practice, dasatinib is the only agent that confers cytotoxic lymphocyte expansion and the phenomenon is associated with favorable outcomes in patients with Philadelphia chromosome-positive leukemia. In this paper the underlying mechanisms that confer activation of immune system and the clinical significance of immunomodulation by small-molecule compounds are highlighted.