Based on the observation that amino acid transporters (e.g., LAT-1) are overexpressed in various cancer cells for their survival, we speculated that amino acid conjugated prodrug of gemcitabine might be an effective way to improve gemcitabine uptake by overexpressing amino acid transporters in pancreatic cancer cells as well as overall physicochemical property. This evidence concerns the gene SLC7A5 and pancreatic neoplasm.