- |||||||||| taspoglutide (BIM51077) / Ipsen
Journal: Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes. (Pubmed Central) - Feb 9, 2022 Here, we report cryoelectron microscopy (cryo-EM) structures and cryo-EM 3D variability analysis of semaglutide- and taspoglutide-bound GLP-1R-Gs protein complexes. These reveal similar peptide interactions to GLP-1 but different motions within the receptor and bound peptides, providing insights into the molecular determinants of GLP-1R peptide engagement.
- |||||||||| Lyxumia (lixisenatide) / Zealand Pharma, Sanofi
Clinical, Retrospective data, Review, Journal, Adverse events: Association of Glucagon-like Peptide 1 Analogs and Agonists Administered for Obesity with Weight Loss and Adverse Events: A Systematic Review and Network Meta-analysis. (Pubmed Central) - Dec 10, 2021 These reveal similar peptide interactions to GLP-1 but different motions within the receptor and bound peptides, providing insights into the molecular determinants of GLP-1R peptide engagement. Direct meta-analysis showed significant WLOP with: -1.44kg (95% CI, -2.14 to -0.74) with dulaglutide ≥1.5 mg; -1.82kg (-2.42 to -1.23) with exenatide immediate release (IR); -2.20kg (-4.31 to -0.08) with exenatide extended release (ER); -3.20kg (-6.53 to 0.15) with efpeglenatide; -2.72kg (-3.35 to -2.09) with liraglutide ≤1.8mg; -4.49kg (-5.26 to -3.72) with liraglutide >1.8mg; -0.62kg (-1.22 to -0.02) with lixisenatide; -4.33kg (-5.71 to -3.00) with semaglutide SQ 50%) in WL and AEs reflected magnitude, not direction of effect.
- |||||||||| simvastatin / Generic mfg., taspoglutide (BIM51077) / Roche
P1 data, Journal: Assessment of Drug-Drug Interactions between Taspoglutide, a Glucagon-Like Peptide-1 Agonist, and Drugs Commonly Used in Type 2 Diabetes Mellitus: Results of Five Phase I Trials. (Pubmed Central) - Sep 5, 2020 Overall, multiple doses of taspoglutide did not result in changes in the pharmacokinetics of digoxin, an oral contraceptive containing ethinylestradiol and levonorgestrel, lisinopril, warfarin, and simvastatin that would be considered of clinical relevance. Therefore, no dose adjustments are warranted upon co-administration.
- |||||||||| Symlin (pramlintide) / AstraZeneca, taspoglutide (ITM-077) / Teijin, taspoglutide (BIM51077) / Roche
Journal: PEGylated prodrugs of antidiabetic peptides amylin and GLP-1. (Pubmed Central) - Oct 27, 2019 Thus, taspoglutide was released even after an incubation period of 24 h in serum with the content of degraded taspoglutide being below 2% in the prodrug at this time point. This PEG-prodrug technology could provide precisely tuned long-acting anti-diabetic and anti-obesity therapies and even once-monthly administration intervals when combined with other formulation strategies.
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