Coix lacryma-jobi var. ma-yuen contains functionally important nutritional constituents. Monascus pilosus is a microorganism used for the preparation of koji, and it also contains biologically active components. Therefore, production of koji with Monascus pilosus contributed to the development of foods of high nutritional value. However, there has been no detailed study on solid fermentation of Coix lacryma-jobi var. ma-yuen with Monascus pilosus. In the present study, we performed solid fermentation and traced the time-dependent production of functional constituents during the fermentation process. The production of free amino acid, γ-aminobutyric acid (GABA), anti-oxidant activity, and OD500 value was found to increase with the growth of Monascus pilosus.