Background. People with neuropsychiatric disorders have been found to have abnormal brain activity, which is associated with the persistent functional impairment found in these patients. Recently, transcranial direct current stimulation (tDCS) has been shown to normalize this pathological brain activity, although the results are inconsistent. Objective. We explored whether tDCS alters and normalizes brain activity among patients with neuropsychiatric disorders. Moreover, we examined whether these changes in brain activity are clinically relevant, as evidenced by brain-behavior correlations. Methods. A systematic review was conducted according to PRISMA guidelines. Randomized controlled trials that studied the effects of tDCS on brain activity by comparing experimental and sham control groups using either electrophysiological or neuroimaging methods were included. Results. With convergent evidence from 16 neurophysiological/neuroimaging studies, active tDCS was shown to be able to induce changes in brain activation patterns in people with neuropsychiatric disorders. Importantly, anodal tDCS appeared to normalize aberrant brain activation in patients with schizophrenia and substance abuse, and the effect was selectively correlated with reaction times, task-specific accuracy performance, and some symptom severity measures. Limitations and Conclusions. Due to the inherent heterogeneity in brain activity measurements for tDCS studies among people with neuropsychiatric disorders, no meta-analysis was conducted. We recommend that future studies investigate the effect of repeated cathodal tDCS on brain activity. We suggest to clinicians that the prescription of 1-2 mA anodal stimulation for patients with schizophrenia may be a promising treatment to alleviate positive symptoms. This systematic review is registered with registration number CRD42020183608.