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Published in: Drugs 4/2018

01-03-2018 | AdisInsight Report

Ertugliflozin: First Global Approval

Author: Anthony Markham

Published in: Drugs | Issue 4/2018

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Abstract

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.
Literature
1.
go back to reference 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.CrossRefPubMed 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.CrossRefPubMed
7.
go back to reference European Medicines Agency. CHMP summary of opinion: Steglujan (ertugliflozin/sitagliptin). 2018. European Medicines Agency. CHMP summary of opinion: Steglujan (ertugliflozin/sitagliptin). 2018.
8.
go back to reference 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 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
9.
go back to reference 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.PubMed 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.PubMed
10.
go back to reference 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, 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.
11.
go back to reference 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.CrossRefPubMedPubMedCentral 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.CrossRefPubMedPubMedCentral
12.
go back to reference 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. 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.
13.
go back to reference 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. 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.
14.
go back to reference 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. 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.
15.
go back to reference 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. 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.
16.
go back to reference 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.CrossRefPubMed 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.CrossRefPubMed
17.
go back to reference 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. 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.
18.
go back to reference 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. 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.
20.
go back to reference 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.CrossRefPubMedPubMedCentral 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.CrossRefPubMedPubMedCentral
21.
go back to reference 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. 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.
22.
24.
go back to reference 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.CrossRefPubMed 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.CrossRefPubMed
25.
go back to reference 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.CrossRefPubMed 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.CrossRefPubMed
Metadata
Title
Ertugliflozin: First Global Approval
Author
Anthony Markham
Publication date
01-03-2018
Publisher
Springer International Publishing
Published in
Drugs / Issue 4/2018
Print ISSN: 0012-6667
Electronic ISSN: 1179-1950
DOI
https://doi.org/10.1007/s40265-018-0878-6

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