Ertugliflozin (Steglatro™) is an orally active sodium glucose co-transporter type 2 inhibitor being developed by Merck and Pfizer as a treatment for type 2 diabetes mellitus (T2DM). Ertugliflozin as monotherapy and in combination with various other antidiabetic drugs was associated with improvements in glycaemic control and secondary outcome measures in the VERTIS phase III clinical trial program. Ertugliflozin and fixed-dose combinations of ertugliflozin and metformin (Segluromet™) and ertugliflozin and sitagliptin (Steglujan™) have recently been approved by the US FDA as an adjunct to diet and exercise to improve glycaemic control in adults with T2DM. These products have also received a positive opinion from the EU Committee for Medicinal Products for Human Use (CHMP). This article summarizes the milestones in the development of ertugliflozin leading to its first approval for T2DM.
This is a preview of subscription content, log in to check access.
Buy single article
Instant access to the full article PDF.
Price includes VAT for USA
Miao Z, Nucci G, Amin N, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013;41(2):445–56.
Merck & Co Inc. STEGLATRO™ (ertugliflozin) tablets, for oral use: prescribing information. 2017. http://www.merck.com/. Accessed 9 Feb 2018.
European Medicines Agency. CHMP summary of opinion: Steglatro (ertugliflozin). 2018. http://www.ema.europa.eu/. Accessed 9 Feb 2018
Merck & Co Inc. SEGLUROMET™ (ertugliflozin and metformin hydrochloride) tablets, for oral use: prescribing Information. 2017. http://www.accessdata.fda.gov/. Accessed 9 Feb 2018.
Merck & Co Inc. STEGLUJAN™ (ertugliflozin and sitagliptin) tablets, for oral use: prescribing Information. 2017. http://www.accessdata.fda.gov/. Accessed 9 Feb 2018.
European Medicines Agency. CHMP summary of opinion: Segluromet (ertugliflozin/metformin). 2018. http://www.ema.europa.eu/. Accessed 9 Feb 2018
European Medicines Agency. CHMP summary of opinion: Steglujan (ertugliflozin/sitagliptin). 2018.
Pfizer. FDA approves SGLT2 inhibitor SteglatroTM (ertugliflozin) and fixed-dose combination SteglujanTM (ertugliflozin and sitagliptin) for adults with type 2 diabetes 2017. http://www.pfizer.com/. Accessed 9 Feb 2018
Sahasrabudhe V, Saur D, Matschke K, et al. A phase 1, randomized, placebo- and active-controlled crossover study to determine the effect of single-dose ertugliflozin on QTc interval in healthy volunteers. Clin Pharmacol Drug Dev. 2018. https://doi.org/10.1002/cpdd.421.
Sahasrabudhe V, Fediuk DJ, Matschke K, et al. Effect of food on the pharmacokinetics of ertugliflozin and its fixed dose combinations: ertugliflozin/sitagliptin and ertugliflozin/metformin [abstract no. PII-123]. Clin Pharmacol Ther. 2017;101(Suppl 1):S86–7.
Sahasrabudhe V, Terra SG, Hickman A, et al. The effect of renal impairment on the pharmacokinetics and pharmacodynamics of ertugliflozin in subjects with type 2 diabetes mellitus. J Clin Pharmacol. 2017;57(11):1432–43.
Kumar V, Sahasrabudhe V, Liang Y, et al. Effect of rifampin on the pharmacokinetics of ertugliflozin in healthy subjects [abstract no. PI-063]. Clin Pharmacol Ther. 2016;99(Suppl 1):S47.
Sahasrabudhe V, Kumar V, Matschke K, et al. Lack of a clinically meaningful pharmacokinetic interaction between ertugliflozin and glimepiride or simvastatin in healthy subjects [abstract no. PI-061]. Clin Pharmacol Ther. 2016;99(Suppl 1):S46–7.
Kumar V, Liang Y, Wei H, et al. Bioequivalence of ertugliflozin/metformin fixed-dose combination tablets and co-administration of respective strengths of individual components [abstract no. PII-071]. Clin Pharmacol Ther. 2017;101(Suppl. 1):S71.
Fediuk DJ, Matschke K, Liang Y, et al. Bioequivalence of ertugliflozin/sitagliptin fixed-dose combination tablets and co-administration of respective strengths of individual components. Clin Pharmacol Ther. 2017;101(S1):S63.
Terra SG, Focht K, Davies M, et al. Phase III, efficacy and safety study of ertugliflozin monotherapy in people with type 2 diabetes mellitus inadequately controlled with diet and exercise alone. Diabetes Obes Metab. 2017;19(5):721–8.
Frias J, Goldman A, Aronson R, et al. Long-term efficacy and safety of ertugliflozin monotherapy in patients with inadequately controlled type 2 diabetes despite diet and exercise: the 52-week VERTIS MONO study [abstract no. 1208-P]. Diabetes. 2017;66:A322–3.
Rosenstock J, Frias J, Pall D, et al. Effect of ertugliflozin on glucose control, body weight, blood pressure and bone density in type 2 diabetes mellitus inadequately controlled on metformin monotherapy (VERTIS MET). Diabetes Obes Metab. 2017. https://doi.org/10.1111/dom.13103.
Hollander P, Liu J, Hill J, et al. Ertugliflozin compared with glimepiride in patients with type 2 diabetes mellitus inadequately controlled on metformin: the VERTIS SU randomized study. Diabetes Ther. 2017. https://doi.org/10.1007/s13300-017-0354-4.
Miller S, Krumins T, Zhou H, et al. Ertugliflozin and sitagliptin co-initiation in patients with type 2 diabetes: the VERTIS SITA randomized study. Diabetes Ther. 2018;9:253–68.
Dagogo-Jack S, Liu J, Eldor R, et al. Efficacy and safety of the addition of ertugliflozin in patients with type 2 diabetes mellitus inadequately controlled with metformin and sitagliptin: the VERTIS SITA2 placebo-controlled randomized study. Diabetes Obes Metab. 2017. https://doi.org/10.1111/dom.13116.
Pratley RE, Eldor R, Raji A, et al. Ertugliflozin plus sitagliptin versus either individual agent over 52 weeks in patients with type 2 diabetes mellitus inadequately controlled with metformin: the VERTIS FACTORIAL randomized trial. Diabetes Obes Metab. 2017. https://doi.org/10.1111/dom.13194.
Grunberger G, Camp S, Johnson J, et al. Ertugliflozin in patients with stage 3 chronic kidney disease and type 2 diabetes mellitus: the VERTIS RENAL randomized study. Diabetes Ther. 2017. https://doi.org/10.1007/s13300-017-0337-5.
Amin NB, Wang X, Jain SM, et al. Dose-ranging efficacy and safety study of ertugliflozin, a sodium-glucose co-transporter 2 inhibitor, in patients with type 2 diabetes on a background of metformin. Diabetes Obes Metab. 2015;17(6):591–8.
Amin NB, Wang X, Mitchell JR, et al. Blood pressure-lowering effect of the sodium glucose co-transporter-2 inhibitor ertugliflozin, assessed via ambulatory blood pressure monitoring in patients with type 2 diabetes and hypertension. Diabetes Obes Metab. 2015;17(8):805–8.
The preparation of this review was not supported by any external funding.
Conflict of interest
During the peer review process, both Merck and Pfizer were offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. A. Markham is a contracted employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
Additional information about this Adis Drug Review can be found at http://www.medengine.com/Redeem/31B99D70725E4EC0.
This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.
About this article
Cite this article
Markham, A. Ertugliflozin: First Global Approval. Drugs 78, 513–519 (2018). https://doi.org/10.1007/s40265-018-0878-6