Albiglutide: First Global Approval

Poole, RM; Nowlan, Mary

doi:10.1007/s40265-014-0228-2

Cited by 42 publications

(19 citation statements)

References 11 publications

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“…It has a half-life of~8 days in humans and is currently in a phase II clinical trial for the treatment of type II diabetes mellitus (109). The recently FDA-approved drug, albiglutide, is a DPPIV-resistant GLP-1 dimer fused to human albumin and has a half-life of 6-7 days, which enables weekly dosing for the treatment of type 2 diabetics (110,111).…”

Section: And Fusion To Long-live Plasma Proteinsmentioning

confidence: 99%

Strategic Approaches to Optimizing Peptide ADME Properties

2014

AAPS J

491

429

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Development of peptide drugs is challenging but also quite rewarding. Five blockbuster peptide drugs are currently on the market, and six new peptides received first marketing approval as new molecular entities in 2012. Although peptides only represent 2% of the drug market, the market is growing twice as quickly and might soon occupy a larger niche. Natural peptides typically have poor absorption, distribution, metabolism, and excretion (ADME) properties with rapid clearance, short half-life, low permeability, and sometimes low solubility. Strategies have been developed to improve peptide drugability through enhancing permeability, reducing proteolysis and renal clearance, and prolonging half-life. In vivo, in vitro, and in silico tools are available to evaluate ADME properties of peptides, and structural modification strategies are in place to improve peptide developability.

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Section: And Fusion To Long-live Plasma Proteinsmentioning

confidence: 99%

Strategic Approaches to Optimizing Peptide ADME Properties

2014

AAPS J

491

429

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“…Furthermore, while many albumin-fusions are still in clinical trials, the first (Tanzeum ® ) was approved by FDA in 2014, which is a fusion of glucagon-like peptide-1 (GLP-1) to the Nterminal end. This drugs is used for treatment of type II diabetes and has a half-life of 5 days in humans [241,242]. A list of therapeutic molecules that has been genetically fused to albumin is shown in Table 3.…”

Section: Genetic Fusion To Albuminmentioning

confidence: 99%

The role of albumin receptors in regulation of albumin homeostasis: Implications for drug delivery

Bern

Sand

Nilsen

et al. 2015

Journal of Controlled Release

162

135

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“…14,15 Several of these, including exenatide and liraglutide, are currently available for treating type 2 diabetes. 16,17,18 Exenatide and liraglutide have both been shown to improve markers of endothelial function in vitro and in animal models. [19][20][21] Additional studies with liraglutide confirmed that this effect is dependent on the GLP-1 receptor.…”

Section: Introductionmentioning

confidence: 99%

The effect of liraglutide on endothelial function in patients with type 2 diabetes

Nandy

Johnson

Basu

et al. 2014

Diabetes and Vascular Disease Research

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This single-centre, 12-week, double-blind, placebo-controlled trial assessed how the human glucagon-like-peptide 1 analogue liraglutide impacted endothelial function in adult patients (n = 49) with type 2 diabetes and no overt cardiovascular disease. Patients were randomized to liraglutide, placebo or glimepiride. At baseline and Week 12, venous occlusion plethysmography was used to measure forearm blood flow (FBF) in response to acetylcholine (ACh) and sodium nitroprusside (SNP) before and after l-N G -monomethyl arginine (L-NMMA) infusion. At Week 12, AChmediated FBF increased with liraglutide and decreased with placebo; however, the between-treatment difference was not significant (p = 0.055). Inhibition of ACh-mediated FBF after L-NMMA infusion increased with liraglutide and decreased with placebo; this between-treatment difference was also not significant (p = 0.149). No change in FBF was observed with SNP. Liraglutide did not significantly impact endothelium-dependent vasodilation after 12 weeks; however, additional investigations looking at the effect of liraglutide on endothelial function in alternative vasculature and during the postprandial period are warranted.

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Albiglutide: First Global Approval

Cited by 42 publications

References 11 publications

Strategic Approaches to Optimizing Peptide ADME Properties

Strategic Approaches to Optimizing Peptide ADME Properties

The role of albumin receptors in regulation of albumin homeostasis: Implications for drug delivery

The effect of liraglutide on endothelial function in patients with type 2 diabetes

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