SCD1 inhibitor MTI-301

An orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor, with potential antineoplastic and immunomodulating activities. Upon oral administration, SCD1 inhibitor MTI-301 targets, binds to the saturated fatty acid (SFA) pocket and inhibits the activity of SCD1, thereby preventing the oxidation of SFAs to monounsaturated fatty acids (MUFAs). This prevents fatty acid synthesis in cancer cells and the fatty acid-mediated promotion of tumor growth, metastasis and drug resistance. This leads to endoplasmic reticulum (ER) stress and induces apoptotic cell death. Inhibition of SCD1 may also activate the adaptive immune response and may promote T-cell-mediated tumor immune responses. In addition, MTI-301 may sensitize cancers to immune checkpoint inhibitors. SCD1, an enzyme converting SFAs to MUFAs, promotes fatty acid synthesis in cancer cells and is upregulated in certain types of cancer. SCD1 plays a key role in tumor immunosuppression.