This article reviews the pollution status of anticancer drugs present in the Yodo River basin located in the Kansai district of Japan, covering both the soluble and insoluble (adsorbed on the river sediments and suspended solids) levels. Procedures ranging from sampling in the field and instrumental analytical methods to the data processing for mass balance estimation of the target basin are also described. All anticancer drugs concerned with this article were detected in sewage and river waters, where the presence of bicalutamide (BLT) was identified at considerably high concentrations (maximum 254 ng/L in the main stream, 151 ng/L in tributaries, and 1032 ng/L in sewage treatment plant (STP) effluents). In addition, sorption distribution coefficient (logKd) values showed a tendency to become higher in the silty sediments at Suita Bridge than in the sandy sediments at Hirakata Bridge; these trends were supported by the results of the laboratory-scale sorption experiment. STPs were concluded to be the main sources of the anticancer drug load in the river, and a mass flux evaluation revealed that the effect of attenuation in the river environment was small. The effectiveness of ozonation in the sewage treatment process for removal of these anticancer drugs was further confirmed. The present article should be of value for facilitating the environmental risk assessment of a wide range of drugs in a broader geographical area.