PF-04620110 (PF04620110; PF 04620110) is a novel, potent, orally bioactive, and selective diglyceride acyltransferase-1 (DGAT1) inhibitor with the potential to treat type 2 diabetes mellitus. It inhibits DGAT1 with an IC50 of 19 nM. PF-04620110 has been advanced to clinical trials on the basis of the excellent pharmacologic and pharmacokinetic profiles. F-04620110 shows high selectivity versus a broad panel of off-target pharmacologic end points. In vivo DGAT-1 inhibition has been demonstrated through reduction of plasma triglyceride levels in rodents at doses of ≥0.1 mg/kg following a lipid challenge.