The escalation in infections from World Health Organization (WHO)‐listed priority pathogens has made development of new antibacterial agents a critical priority. In this context, use of therapeutic secondary metabolites (SMs) from Actinobacteria as new drugs presents a promising avenue. However, majority of them fail to reach market due to low aqueous solubility and hence low bioavailability. Even though nanosuspension technology has been effectively used to address these challenges, use of this technology for nanox02010;listed priority pathogens has made development of new antibacterial agents a critical priority. In thitransformation of crude metabolites from Actinobacteria is still an unattempted area. Herein, for the first time, development of water‐soluble nanosuspension of water‐insoluble therapeutic metabolites produced by Streptomyces californicus strain ADR1 to develop a biocompatible material to be used as potential nanomedicine is reported. The nanosuspension (N‐SM) is characterized by UV‐vis spectroscopy, transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and dynamic light scattering (DLS). The nanosuspension reduces the MIC values by 50% against Gram‐positive priority pathogens and eradicates established biofilms with fivefold efficiency incomparison to SMs. The nanosuspension also displays antioxidant activity. The findings open up future possibilities of using this novel nanosuspension as an effective antibacterial agent in various therapeutic and biomedical applications like wound dressings, coatings on medical equipment, and surgical implants.