BACKGROUND: This review outlines the features of the pharmacokinetics of the perfusion radiopharmaceutical 99mTc-MIBI, which allows the assessment of myocardial mitochondrial dysfunction, and shows the main clinical applications of the phenomenon of increased 99mTc-MIBI washout rate. AIM: To systematize the data of fundamental (experimental) and clinical studies evaluating and estimating mitochondrial dysfunction according to myocardial perfusion scintigraphy data and perform meta-analysis of clinical studies in this field. MATERIALS AND METHODS: PubMed, Scopus, Google Scholar, and eLibrary databases were searched until mid-2023. The following keywords, their combinations, and Russian-language counterparts were used: mitochondrial dysfunction, 99mTc-MIBI, 99mTc-Tetrofosmin, myocardial perfusion scintigraphy, reverse redistribution, washout, and washout rate. In the meta-analysis, a random-effects model was used to calculate the mean difference estimate. RESULTS: Forty articles were selected for systematic analysis: 13 were experimental, 24 were original clinical papers, 2 were clinical cases, and 1 was a review. Six studies using a case–control design were selected for the meta-analyses. The total number of patients in the systematic review and meta-analysis were 551 and 196, respectively. In the analysis of the literature, the severity of the reverse redistribution phenomenon and 99mTc-MIBI washout rate correlated with mitochondrial and myocardial microstructure, left ventricular contractility and hemodynamics, natriuretic peptide levels, exercise tolerance, coronary atherosclerosis severity, myocardial oxidative metabolism, and risk of cardiovascular events. The meta-analysis showed that the washout rate was statistically significantly accelerated in individuals with cardiac pathologies, relative to controls (mean difference score, 9.5771 [95%]; confidence interval, 6.6001–12.5540; z=6.3053, p 0.0001). CONCLUSION: The assessment of mitochondrial function by 99mTc-MIBI washout evaluation may provide additional insights into the functional status of cardiac muscles.