The composition of secondary metabolites undergoes significant changes in plants depending on the growth phase and the influence of environmental factors. Therefore, it is important to determine the harvesting time of plant material for the optimum secondary metabolite profile and therapeutic activity of the primary material. The shoots of Epilobium angustifolium are used as a healing tea due to the presence of polyphenolic compounds. The aim of this study was to assess the composition of phenolic compounds and triterpenoid saponins in E. angustifolium leaves and flowers and to estimate the dynamics of their content depending on the flowering phase. Qualitative and quantitative characterisation of polyphenols and triterpenoids in E. angustifolium samples from Ukraine of three flowering phases were performed using the high-performance liquid chromatography photo diode array (HPLC-PDA) method. During the present study, 13 polyphenolic compounds and seven triterpenoids were identified in the plant material. It was noted that the largest content and the best polyphenol profile was in late flowering. The most important polyphenolic compounds in the plant material were chlorogenic acid, hyperoside, isoquercitin, and oenothein B. The triterpenoid profile was at its maximum during mass flowering, with corosolic and ursolic acids being the dominant metabolites. The results of the analysis revealed that the quantity of many of the tested metabolites in the raw material of E. angustifolium is dependent on the plant organ and flowering phase. The largest content of most metabolites in the leaves was in late flowering. In the flowers, the quantity of the metabolites studied was more variable, but decreased during mass flowering and increased significantly again in late flowering. The results show that E. angustifolium raw material is a potential source of oenothein B and triterpenoids.