Talabostat mesylate is a non-selective inhibitor of the S9 family of serine proteases (IC50s: DPPIV = <4nM, DPP8 = 4nM, DPP9 = 11nM, QPP = 310nM, FAP = 560nM, PEP = 390nM).1 Toxicity caused by DPP8/9 inhibition observed with non-selective DPPIV inhibitors limits their use as a diabetes treatment. However, Talabostat displays potent antitumor effects dependent on an intact host immune response.2 It mediates tumor regression by accelerating the expansion of tumor-specific T cells.3 Additionally, DPP8/9 inhibition by Talabostat activates the proprotein form of Caspase-1 leading to a proinflammatory form of cell death in monocytes and macrophages - pyroptosis.4 Pyroptosis induction by DPP8/9 inhibition has been shown to be caused by activation of the inflammasome sensor protein NLRP1B.5
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