Rivaroxaban (RIV) is an oral anticoagulant that is the first available orally active direct inhibitor of factor Xa. This study focuses on a critical review of the mechanisms of action, characteristics, operations, physicochemical properties of RIV, and analytical methodologies to quantify the concentration of the agent in bulk, pharmaceutical formulations, dissolution media, and biological samples. The major analytical methodology for the determination of RIV is reverse-phase HPLC coupled with UV detection and LC-MS/MS. This technique is particularly beneficial to detect and analyze RIV in plasma samples. The methodologies published in literature until recently were tabulated and the sample preparation techniques prior to analyzes of the biological matrix were discussed. Based on this critical literature screening, it was concluded that the researchers may easily apply or modify the published methodologies depending on their purpose on further studies since the chemical and physical properties of RIV allows this agent to be extracted and analyzed by employing different analytical strategies.