T0185

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. In the liver, it is converted by SLC27A2 into a CoA thioester, which interacts with the CoA binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. It mimics the immune and antitumor effects seen with ACLY gene deletion. Additionally, EVT0185 elevates levels of tumor-infiltrating B cells and the chemokine CXCL13. It is applicable in cancer research, including hepatocellular carcinoma (HCC).