Among heterocyclic compounds, the various biological activities and the easily modifiable chemical structure of benzimidazole compounds make them important in drug development. Currently, the demand for treatments targeting multiple biological pathways is increasing. In the treatment of multifaceted diseases, drugs exhibiting multiple therapeutic effects and low toxicity are particularly advantageous. In this context, the ability of benzimidazole compounds to form hybrid structures that target multiple biological mechanisms is noteworthy. In this review, studies on the multifaceted biological activities of hybrid benzimidazole derivatives—including benzimidazole–triazole, benzimidazole–thiazole, benzimidazole–oxadiazole, benzimidazole–quinoline, benzimidazole–hydrazone, benzimidazole-benzimidazole, benzimidazole–thiadiazole, benzimidazole–piperazine, benzimidazole-imidazole, benzimidazole-benzothiazole, benzimidazole–coumarin, benzimidazole–indole, benzimidazole-Schiff base and benzimidazole-urea reported in the literature over the past 5 years are discussed. In addition, this review also examines molecular modeling and structure–activity relationship studies to elucidate their therapeutic potential, highlighting the contribution of hybrid benzimidazole derivatives to the development of effective drugs.