Tenalisib (RP6530) is primarily used in the development of cancer therapies, particularly for hematological malignancies such as lymphomas and leukemias. It functions as a selective inhibitor of phosphoinositide 3-kinase (PI3K), specifically targeting the delta and gamma isoforms, which are involved in B-cell and tumor microenvironment signaling. Due to its selectivity, it shows potential in reducing tumor growth and survival while minimizing toxicity compared to broader PI3K inhibitors. It has been investigated in clinical trials for relapsed or refractory non-Hodgkin lymphoma, including subtypes like chronic lymphocytic leukemia (CLL) and diffuse large B-cell lymphoma (DLBCL). Its targeted mechanism supports immune modulation within the tumor environment, enhancing anti-tumor immune responses. Research also explores its use in combination with other agents such as monoclonal antibodies or targeted therapies to improve treatment outcomes.