Despite anti-tumor effects reported for DGAT inhibitors in pre-clinical cancer models, the side effects of DGAT inhibitors, especially gastrointestinal adverse events, were observed in finished clinical trials, and ubiquitous expression of DGATs in the whole body and an unsatisfactory pharmacokinetic profile may partially limit the application of current inhibitors of DGAT1 and DGAT2 in cancer patients [166, 167]. The gene discussed is DGAT1; the disease is cancer.