We succeeded in developing formulations of poorly water-soluble drug S-892216 by applying solubility enhancement technologies. Oral solution and solid dispersion suspension were developed as formulations for human ADME studies, and their efficient absorption was confirmed through a rat pharmacokinetic study. In developing solid dispersion-coated tablets as the to-be-marketed formulation, PVPVA was selected as a suitable polymer from the results of both the dog pharmacokinetic study and stability testing. Our findings indicate that the to-be-marketed formulation will facilitate rapid and efficient evaluation of S-892216 through human ADME studies as well as large-scale clinical studies.