Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response[1][2].
Sirpiglenastat (DRP-104) treatment shows broad immune cell modulation effects including increased T, NK, and macrophages. Sirpiglenastat decreases pro-tumorigenic cytokines such as VEGF and KC (IL-8)[1].
CT26 bearing mice treated with Sirpiglenastat (DRP-104) (0.5 mg/kg; s.c.; once a day; for 5 days) shows tumor growth inhibition at day 12 of 90%. Median survival days are 36 days[1].
Sirpiglenastat (0.5 mg/kg; s.c) treatment significantly inhibits tumor growth in the H22 model[1].
| Animal Model: | CT26 bearing mice[1] |
| Dosage: | 0.5 mg/kg |
| Administration: | s.c.; once a day; for 5 days |
| Result: | Showed tumor growth inhibition in mice. |
[1]. Yumi Yokoyama, et al. DRP-104, a novel broad acting glutamine antagonist, induces distinctive immune modulation mechanisms and synergistic efficacy in combination with immune checkpoint blockade. J Immunother Cancer. 2019 Nov 6;7(Suppl 1):282.
[2]. Yumi Yokoyama, et al. DRP-104, a broad acting glutamine antagonist, synergizes with immune checkpoint blockade in vivo. Cancer Res 2021;81(13_Suppl):Abstract nr 1563.