Description: CA-327 is a novel potent, orally available, small molecule and dual inhibitor of TIM3 and PD-L1 with potential anticancer activities. In addition to PD-1, there are several other checkpoints involved in the modulation of immune responses to tumor cells. One such checkpoint is T-cell immunoglobulin and mucin domain containing protein-3 (TIM3), which shares some structural similarity with PD-L1. TIM3 is also a potent suppressor of T cell functions and is co-expressed with programmed cell death-1 (PD-1) receptors on certain T cells. TIM3 modulates immune response by binding to one or more of its ligands: galectin 9 (GAL9), phosphatidyl serine, high mobility group protein B1 (HMGB1) and Ceacam-1. Animal studies have demonstrated that combined inhibition of PD-L1 and TIM3 results in improved anti-tumor responses in certain tumor models, highlighting their independent roles in regulating immune response to tumors.