Background <p>Light wheat is the immature fruit of wheat. It is a commonly used traditional Chinese medicine in clinic. It has different effects at different stages, especially in the treatment of hyperhidrosis.</p> Methods <p>Five growth stages of Light wheat were analyzed by UPLC-MS/MS and RNA sequencing of gene expression. Metabolome and transcriptome analysis were used to explore the formation mechanism of Light wheat and MetMap analysis was used to analyze the pharmacodynamic material basis.</p> Results <p>Different metabolic product accumulation and gene expression patterns were observed, especially in the phenylpropane synthesis pathway and flavonoid and flavonol biosynthesis. The main findings include the following: the harvest period of main metabolites is stage C to stage D. The key regulatory genes for the formation of Light wheat, include module core genes and possible pharmacological substances.</p> Conclusion <p>This study preliminarily explores the metabolic and transcriptional dynamics during Light wheat development; the critical harvesting period for the accumulation of pharmacologically active compounds in Light wheat has been preliminarily identified and provided an important theoretical basis for its pharmacodynamic material basis.</p>