Sirpiglenastat (DRP-104) is a glutamine antagonist, a prodrug of DON, with antitumor activity that acts by inhibiting glutamine metabolism and stimulating the innate and adaptive immune system.

Treatment with Sirpiglenastat (DRP-104) exhibits broad immune cell modulation effects, including an increase in T cells, NK cells, and macrophages. Sirpiglenastat also reduces the levels of pro-tumorigenic cytokines such as VEGF and KC (IL-8)[1].

In CT26 bearing mice, treatment with Sirpiglenastat (DRP-104) at a dose of 0.5 mg/kg through subcutaneous injection once a day for 5 days results in a 90% inhibition of tumor growth by day 12, with a median survival of 36 days[1].Additionally, Sirpiglenastat treatment (0.5 mg/kg; s.c) significantly inhibits tumor growth in the H22 model[1].