Talabostat is a prolineboronate ester derivative patented by Boehringer Ingelheim Pharmaceuticals, Inc. as an antineoplastic agent. Talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity. Talabostat has been shown to cause caspase-1 activation and IL-1β induction in macrophages, which in turn causes upregulation of the cytokines and chemokines that characterize the responses to talabostat, both in vitro and in tumor-bearing mice. Talabostat may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. In clinical trials, the combination of talabostat and cisplatin was well tolerated compared to historical data using cisplatin alone. The most frequent adverse events were nausea, vomiting, fatigue, anemia, edema, and constipation. Unfortunately was no evidence that Talabostat enhanced the clinical activity of other anticancer drugs and further development was discontinued.