A large variety of human activity are primarily responsible of striking our natural water resources. Among all, the entry of pharmaceuticals into drinking water sources is the latest threat that is caused by different human activities. The rapid growing population and restricted freshwater resources have created the necessity to treat polluted water for drinking purposes. Recently, graphene-based nanomaterials for the water purification have drawn researchers' interest owing to their specific structure and unique electrochemical properties. Therefore, this chapter discusses the utility of various graphene-based nanomaterials for the removal of pharmaceuticals from contaminated waters. At first, we discuss the fate and health hazards of pharmaceuticals if present in the water, followed by the advanced removal processes. Next, various surface modification methods for the preparation of graphene composites have been discussed. Also, the latest research reported for the removal of pharmaceuticals using graphene-based nanomaterials following adsorption, catalytic oxidation, and photocatalytic degradation processes were discussed in detail. Further, the influence of various reaction parameters on the removal efficiency has been described following the stability of graphene-based nanomaterials. Finally, recommendations have been made according to the current practices and applications in water industry to improve the contaminated water treatment processes. © 2019 Elsevier Inc. All rights reserved.