Bacopa monnieri (BM) is of immense therapeutic potential in today’s world. This review is aimed to project the beneficial role of BM in disorders affecting the brain, including Alzheimer’s disease, Parkinson’s disease, stroke, epilepsy and depression. The active constituents and metabolites responsible for the effects of BM could be bacoside A and B, bacopaside I and II, bacopasaponin C, betulinic acid, asiatic acid, loliolide, ebelin lactone and quercetin. The mechanistic role of BM in brain disorders might be related to its ability to modulate neurotransmission, neurogenesis, neuronal/glial plasticity, intracellular signaling, epigenetics, cerebral blood flow, energy metabolism, protein folding, endoplasmic reticulum stress, neuroendocrine system, oxidative stress, inflammation and apoptosis. We have also discussed CDRI-08, clinical trials, safety, emerging formulation technologies, as well as BM combinations and dietary supplements. To propel the clinical translation of BM in disorders affecting the brain, strategies to improve brain delivery via novel formulations and integration of the preclinical findings into large and well-defined clinical trials, in appropriate age groups and sex, specifically in patient population against existing medications as well as placebo, are essentially required.