Oxidative stress can present as a cause or as an inherent metabolic state with respect to several diseases in which isoforms of the NAD(P)H oxidase complex (Nox isoforms) are among the leading producers of reactive oxygen species (ROS). Control of the redox homeostasis through the inhibition of the NAD(P)H oxidase complex is a tool of great pharmacological interest. This systematic review investigated and analyzed the literature that addresses the inhibitors of the NAD(P)H oxidase complex, while focusing on the mechanisms of action and their potential clinical applications. This is a piece of documentary research that has as its sources scientific articles available through scientific databases; these works were derived through a search of the ScienceDirect.com database, using the keywords NAD(P)H oxidase"and Nox inhibitor. Several studies have shown that inhibitors of Nox can control oxidative stress associated with the source or exacerbation of various pathologies. However, most scientific reports refer to either the use of non-selective compounds for this target or substances that cannot be used in vivo, due to the risk of serious toxic effects. Based on these results, we determine the need for a search of specific inhibitors for Nox isoforms, which can be used in clinical settings to treat pathological processes in which excessive ROS production occurs.