Breastmilk (BM) is the primary source of nutrition for the newborn infant and its first six months of life. Although the importance of BM in the proper growth and development of infants has previously been recognized in various research studies, it was not until various metabolites were probed in BM that researchers discovered the various beneficial effects of BM beyond its nutritive value. Metabolomics has emerged as a discipline which aims to comprehensively profile various metabolites in food and biological fluids. Although still in its incipient stages, BM metabolomics has provided invaluable insights into the chemical interaction between mother and infant. NMR-and MS-based techniques have made it possible to explore the metabolome of BM and link it to various aspects of maternal phenotype and nutrition and breastfed infant health outcomes. In addition, recent developments in analytical approaches for BM metabolite analysis and metabolomic data analysis have allowed researchers to increase the coverage of detected metabolites using multiple platforms and have supported its functional characterization which aids in investigation of the clinical and biological importance of metabolites. These advancements can potentially aid in the development of strategies to promote healthy feeding practices for infants or novel therapeutic and nutrition advances in pediatric research.