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. 2022 Apr 21;14(9):2072. doi: 10.3390/cancers14092072

Table 5.

Summary of studies suggesting antitumor effect of gliptins mediated by promotion of antitumor immune response.

Tumor TYPE Gliptin Proposed Mechanism Notes, Reference
Melanoma, colorectal carcinoma Sitagliptin Preserved bioactivity of CXCL10, leading to increase CXCR3-dependent infiltration of CD4+ and CD8+ lymphocytes. No effect of sitagliptin on tumor growth in DPP-IV KO mice suggests that sitagliptin does not have a direct cytotoxic effect [157].
Hepatic cancer Anagliptin, vildagliptin, sitagliptin Preserved bioactivity of CXCL10, leading to increase CXCR3-dependent infiltration of NK cells. Gliptins do not affect the growth of hepatocellular carcinoma cells in vitro (up to 100 µM) [68].
Hepatic and breast cancer Sitagliptin Preserved bioactivity of CCL11, leading to increased infiltration of eosinophils. No effect of sitagliptin on hepatic carcinoma cell growth (up to 12.3 µM) [67].
Ovarian cancer Sitagliptin Infiltration of the tumors by CXCR3+ T lymphocytes [82]
Lung cancer Vildagliptin Increased expression of surfactant proteins in cancer cells, resulting in higher amounts and pro-inflammatory activity of macrophages and NK cells. The antitumor effect of vildagliptin was preserved in CD26−/− animals. No cytotoxicity observed for 0.3–1.3 mM vildagliptin in vitro, increased surfactant protein expression after treatment with 10–20 µM vildagliptin [160].