Beta-alanine, a non-essential amino acid and the rate-limiting precursor for the synthesis of muscle carnosine, plays a pivotal physiological role in regulating intramuscular acid–base balance, particularly during high-intensity exercise. Its primary mechanism involves buffering hydrogen ions to delay the onset of metabolic acidosis and subsequent muscle fatigue. This mini review aims to synthesize the current scientific literature to elucidate the bioactivity of beta-alanine and critically evaluate its ergogenic and potential therapeutic effects on overall health and wellbeing. Substantial evidence from clinical trials demonstrates that beta-alanine supplementation effectively augments intramuscular carnosine concentrations, leading to marked improvements in anaerobic exercise capacity and fatigue resistance. These benefits extend beyond athletic populations to clinical cohorts experiencing age-related muscle deterioration. Furthermore, emerging research suggests indirect cardiovascular and cognitive benefits, potentially mediated through enhanced exercise tolerance, reduced systemic oxidative stress, and anti-inflammatory activity. Notably, beta-alanine may help preserve endothelial function and reduce cardiometabolic risk factors. Preliminary findings also suggest that carnosine confers neuroprotective properties through its antioxidant and antiglycation activities, although direct evidence for cognitive enhancement in humans remains limited and warrants further investigation. Significant research gaps persist, including a lack of standardized dosing protocols, limited long-term safety data, and insufficient exploration of its effects in older adults and other patient populations. This review underscores the necessity for rigorous, long-term, and standardized clinical trials involving diverse cohorts to fully delineate the therapeutic potential of beta-alanine as a versatile nutraceutical agent for enhancing physical, metabolic, and cognitive health.