Dulaglutide for the treatment of type 2 diabetes

Amblee, Ambika

doi:10.1358/dot.2014.50.4.2132740

Cited by 12 publications

(10 citation statements)

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“…To extend the half-life, DPP-4-resistant GLP-1 analogues with GLP-1 receptor agonist properties have been developed, including exenatide, liraglutide, lixisenatide, albiglutide, and dulaglutide that have been approved by the Food and Drug Administration (FDA). [29][30][31][32][33] On the other hand, DPP-4 inhibitors have been developed and used to prevent degradation of endogenously released GLP-1 and GIP, consequently enhancing plasma level of active incretins in circulation, prolonging the actions of the incretin, consequently leading to increased insulin level. 34 In patients with T2DM, the 'incretin effect' is reduced, thus scientists have adopted the 'incretin concept' in attempts to develop incretin-based therapeutic agents.…”

Section: Dpp-4 and Incretins As Therapeutic Targets For T2dmmentioning

confidence: 99%

Clinical pharmacology of dipeptidyl peptidase 4 inhibitors indicated for the treatment of type 2 diabetes mellitus

Chen

Zhou

et al. 2015

Clin Exp Pharma Physio

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SUMMARYDipeptidyl peptidase-4 (DPP-4) inhibitors are a class of oral antidiabetic drugs that improve glycaemic control without causing weight gain or increasing hypoglycaemic risk in patients with type 2 diabetes mellitus (T2DM). The eight available DPP-4 inhibitors, including alogliptin, anagliptin, gemigliptin, linagliptin, saxagliptin, sitagliptin, teneligliptin, and vildagliptin, are small molecules used orally with identical mechanism of action and similar safety profiles in patients with T2DM. DPP-4 inhibitors may be used as monotherapy or in double or triple combination with other oral glucoselowering agents such as metformin, thiazolidinediones, or sulfonylureas. Although DPP-4 inhibitors have the same mode of action, they differ by some important pharmacokinetic and pharmacodynamic properties that may be clinically relevant in some patients. The main differences between the eight gliptins include: potency, target selectivity, oral bioavailability, elimination half-life, binding to plasma proteins, metabolic pathways, formation of active metabolite(s), main excretion routes, dosage adjustment for renal and liver insufficiency, and potential drug-drug interactions. The off-target inhibition of selective DPP-4 inhibitors is responsible for multiorgan toxicities such as immune dysfunction, impaired healing, and skin reactions. As a drug class, the DPP-4 inhibitors have become accepted in clinical practice due to their excellent tolerability profile, with a low risk of hypoglycaemia, a neutral effect on body weight, and once-daily dosing. It is unknown if DPP-4 inhibitors can prevent disease progression. More clinical studies are needed to validate the optimal regimens of DPP-4 inhibitors for the management of T2DM when their potential toxicities are closely monitored.

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Section: Dpp-4 and Incretins As Therapeutic Targets For T2dmmentioning

confidence: 99%

Clinical pharmacology of dipeptidyl peptidase 4 inhibitors indicated for the treatment of type 2 diabetes mellitus

Chen

Zhou

et al. 2015

Clin Exp Pharma Physio

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“…The biological half‐life of endogenous GLP‐1 is 1.5–5 min and GIP has a serum half‐life of 5–7 min . In order to extend the half‐life of GLP‐1 and GIP, DPP‐4‐resistant GLP‐1 analogues have been developed which have GLP‐1 receptor agonist properties; these analogues have been approved by the FDA and include exenatide, liraglutide, lixisenatide, albiglutide and dulaglutide . Besides the development of DPP‐4‐resistant GLP‐1 analogues, DPP‐4 inhibitors have been extensively investigated and clinically used to prevent the degradation of endogenous GLP‐1 and GIP.…”

Section: Dpp‐4 and Incretins As Therapeutic Targets For T2dmmentioning

confidence: 99%

“…49 In order to extend the half-life of GLP-1 and GIP, DPP-4-resistant GLP-1 analogues have been developed which have GLP-1 receptor agonist properties; these analogues have been approved by the FDA and include exenatide, liraglutide, lixisenatide, albiglutide and dulaglutide. [53][54][55][56][57] Besides the development of DPP-4-resistant GLP-1 analogues, DPP-4 inhibitors have been extensively investigated and clinically used to prevent the degradation of endogenous GLP-1 and GIP. Consequently, the DPP-4 inhibitors result in an enhanced plasma level of biologically active incretins in circulation, prolongation of incretin actions, leading to an increase in insulin level.…”

Section: Glp-1 and Gip As Incretin Hormonesmentioning

confidence: 99%

An update on the clinical pharmacology of the dipeptidyl peptidase 4 inhibitor alogliptin used for the treatment of type 2 diabetes mellitus

Chen

Zhou

et al. 2015

Clin Exp Pharma Physio

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SUMMARYAlogliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor that is a class of relatively new oral hypoglycaemic drugs used in patients with type 2 diabetes (T2DM), can be used as monotherapy or in combination with other anti-diabetic agents, including metformin, pioglitazone, sulfonylureas and insulin with a considerable therapeutic effect. Alogliptin exhibits favorable pharmacokinetic and pharmacodynamic profiles in humans. Alogliptin is mainly metabolized by cytochrome P450 (CYP2D6) and CYP3A4. Dose reduction is recommended for patients with moderate or worse renal impairment. Side effects of alogliptin include nasopharyngitis, upper-respiratory tract infections and headache. Hypoglycaemia is seen in about 1.5% of the T2DM patients. Rare but severe adverse reactions such as acute pancreatitis, serious hypersensitivity including anaphylaxis, angioedema and severe cutaneous reactions such as Stevens-Johnson syndrome have been reported from post-marketing monitoring. Pharmacokinetic interactions have not been observed between alogliptin and other drugs including glyburide, metformin, pioglitazone, insulin and warfarin. The present review aimed to update the clinical information on pharmacodynamics, pharmacokinetics, adverse effects and drug interactions, and to discuss the future directions of alogliptin.

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“…According to their half-lives in circulation, exenatide and lixisenatide are categorized as short-acting GLP-1RAs, while liraglutide is categorized as a long-acting GLP-1RA. More recently, exenatide LAR, dulaglutide, and semaglutide have been developed as once-weekly injectable GLP-1RAs having much longer half-lives in circulation (exenatide LAR, >24 h; dulaglutide, approximately 90 h; and semaglutide approximately 1 week) to lessen the burden of injections [12][13][14] ; exenatide, lixisenatide, and liraglutide require once or twice daily injection. On the other hand, exenatide LAR, dulaglutide, and semaglutide are categorized as ultralong-acting GLP-1RAs.…”

Section: Introductionmentioning

confidence: 99%

Effects of glucagon‐like peptide‐1 receptor agonists on secretions of insulin and glucagon and gastric emptying in Japanese individuals with type 2 diabetes: A prospective, observational study

Kuwata

Yabe

Murotani

et al. 2021

J of Diabetes Invest

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Aims/Introduction: Differences in the glucose-lowering mechanisms of glucagon-like peptide-1 receptor agonists (GLP-1RAs) have been noted. Clarifying these differences could facilitate the choice of optimal drugs for individuals with type 2 diabetes and requires investigation in a clinical setting. Materials and Methods: A single-arm, prospective, observational study was conducted to evaluate the effects of various GLP-1RAs on postprandial glucose excursion, secretions of insulin and glucagon as well as on the gastric emptying rate. Participants were subjected to meal tolerance tests before and 2 weeks and 12 weeks after GLP-1RA initiation. Effects on postprandial secretions of glucose-dependent insulinotropic polypeptide (GIP) and apolipoprotein B48 were also investigated. Results: Eighteen subjects with type 2 diabetes received one of three GLP-1RAs, i.e., lixisenatide, n = 7; liraglutide, n = 6; or dulaglutide, n = 5. While 12-week administration of all of the GLP-1RAs significantly reduced HbA1c, only lixisenatide and liraglutide, but not dulaglutide, significantly reduced body weight. Postprandial glucose elevation was improved by all of the GLP-1RAs. Postprandial insulin levels were suppressed by lixisenatide, while insulin levels were enhanced by liraglutide. Postprandial glucagon levels were suppressed by lixisenatide. The gastric emptying rate was significantly delayed by lixisenatide, while liraglutide and dulaglutide had limited effects on gastric emptying. GIP secretion was suppressed by lixisenatide and liraglutide. Apolipoprotein B48 secretion was suppressed by all of the GLP-1RAs. Conclusions: All of the GLP-1RAs were found to improve HbA1c in a 12-week prospective observational study in Japanese individuals with type 2 diabetes. However, differences in the mechanisms of the glucose-lowering effects and body weight reduction were observed.

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Dulaglutide for the treatment of type 2 diabetes

Cited by 12 publications

References 0 publications

Clinical pharmacology of dipeptidyl peptidase 4 inhibitors indicated for the treatment of type 2 diabetes mellitus

Clinical pharmacology of dipeptidyl peptidase 4 inhibitors indicated for the treatment of type 2 diabetes mellitus

An update on the clinical pharmacology of the dipeptidyl peptidase 4 inhibitor alogliptin used for the treatment of type 2 diabetes mellitus

Effects of glucagon‐like peptide‐1 receptor agonists on secretions of insulin and glucagon and gastric emptying in Japanese individuals with type 2 diabetes: A prospective, observational study

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