Objective: The purpose of this article is to review the pharmacological aspects of ertugliflozin and its clinical trials, which led to Food and Drug Administration (FDA) approval for the treatment of type 2 diabetes mellitus (T2DM). Data Sources: A MEDLINE/PubMed (May 2013 to October 2018) search was conducted using the following keywords: ertugliflozin, sodium glucose co-transporter 2 inhibitor, SGLT2 inhibitor, type 2 diabetes mellitus, hyperglycemia. Study Selection and Data Extraction Quantify: We included English-language articles evaluating ertugliflozin pharmacology, pharmacokinetics, efficacy, and safety in humans for blood glucose reduction in human subjects. Data Synthesis: Ertugliflozin has been FDA approved and considered both safe and efficacious for the treatment of T2DM with hemoglobin A 1C reductions ranging from −0.6% to −1.16%. Safety outcomes appear to be similar to that of other SGLT2 inhibitors. Relevance to Patient Care and Clinical Practice: With this approval, patients and clinicians now have another oral option for treating this difficult disease while minimizing hypoglycemia and other unwanted adverse drug reactions. Conclusions: With the number of patients with diabetes growing, additional safe and effective treatment options available for clinicians and patients is important. Ertugliflozin appears to be an effective and safe therapy as both single and add-on therapy.