taspoglutide (BIM51077) / Ipsen - LARVOL DELTA

Comparison of the efficacy and safety of GLP-1 receptor agonists on cardiovascular events and risk factors: A review and network meta-analysis. (PubMed, Diabetes Obes Metab) - "This study compared the cardiovascular benefits of different GLP-1RAs, including reductions in cardiovascular events and improvements in multiple cardiovascular risk factors. However, due to limitations in the quantity and quality of the included studies, the conclusions should be interpreted with caution. Future large-scale, high-quality clinical trials are needed to validate these findings and further optimize comprehensive cardiovascular management strategies for patients."

Journal • Retrospective data • Review • Cardiovascular • Dyslipidemia • Gastrointestinal Disorder

Glucagon-like Peptide-1 Receptor Agonists for Adult Obesity: Where Next? (ISPOR-EU 2024) - "The most commonly assessed GLP-1 RAs were liraglutide and semaglutide (48%), followed by exenatide (24%) and dulaglutide (21%). Other less commonly identified agents included danuglipron, cotadutide, taspoglutide and mazdutide (2% each)... This research highlights growing interest and evidence in GLP-1 RAs for obesity management. Further research is needed to continue evaluating the long-term efficacy and safety of these interventions."

Clinical • Cardiovascular • Diabetes • Genetic Disorders • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Obesity • Polycystic Ovary Syndrome • Type 2 Diabetes Mellitus

Efficacy and Safety of Glucagon-Like Peptide 1 Analogs and Agonists (aGLP1) in Overweight/Obese Patients: a Systematic Review and an Updated Network Meta-Analysis (ENDO 2023) - "Also, tirzepatide 15 mg outperformed liraglutide > 1.8 mg (-4.24; 95% CrI: -6.85, -1.85), liraglutide = 1.8 mg (-6.51; 95% CrI: -8.92, -4.2), dulaglutide < 1.5 mg (-8.02; 95% CrI: -10.89, -5.38), dulaglutide = 1.5 mg (-7.48; 95% CrI: -10.52, -4.32), exenatide (-7.31; 95% CrI: -9.91, -4.9), semaglutide < 2.4 mg (-3.98; 95% CrI: -6.67, -1.26), tirzepatide 5 mg (-3.45; 95% CrI: -5.87, -0.93), efpeglenatide (-5.53; 95% CrI: -9.32, -1.86), taspoglutide (-7.78; 95% CrI: -11.79, -3.99) and lixisenatide (-8.3; 95% CrI: -12.34, -4.48). Tirzepatide 15 mg appears to be the most effective aGLP1 for weight reduction while it is similar to other aGLP1 regarding acceptability and safety. Taspoglutide was remarkably inferior to other aGLP1 considering discontinuation risk.*Unless otherwise noted, all abstracts presented at ENDO must not be released to the press or the public until the date and time of presentation. For oral presentations, the abstracts are embargoed until the..."

Retrospective data • Review • Genetic Disorders • Obesity

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, EClinicalMedicine) - "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."

Adverse events • Clinical • Journal • Retrospective data • Review • Genetic Disorders • Obesity

Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes. (PubMed, Cell Rep) - "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."

Journal • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

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, Clin Pharmacokinet) - "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."

Journal • P1 data • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

A direct comparison of long and short-acting GLP-1 receptor agonists (taspoglutide once weekly and exenatide twice daily) on postprandial metabolism after 24 weeks of treatment (Diabetes Obes Metab) - PMID: 23911196; P3, N=148; NCT00717457; Sponsor: Hoffmann-La Roche; "The 2-h postprandial, mean0-3 h and iAUC0-3 h glucose during the MTT was reduced to a similar extent in all groups and the time profile of the postprandial glucose showed a similar pattern. Taspo10 and Taspo20, but not EXE, significantly increased insulin from baseline (both mean and iAUC0-3 h). "

P3 data • Diabetes

A study of taspoglutide versus exenatide for the treatment of patients with type 2 diabetes mellitus inadequately controlled with metformin, thiazolidinedione or a combination of both (clinicaltrials.gov) - P3, N=1,189; Active, not recruiting ➔ Completed

Trial completion • Diabetes

Effects of taspoglutide on glycemic control and body weight in obese patients with type 2 diabetes (T-emerge 7 study) (Obesity (Silver Spring)) - P3, N=305; NCT00823992; Sponsor:Hoffmann-La Roche; PMID: 23404788; "Weight loss at week 24 was significantly greater with taspoglutide than placebo...target HbA1c levels (≤6.5%) were achieved by 49% and 16% of patients, respectively, while 72% and 36% achieved HbA1c levels ≤7%."

P3 data • Diabetes

Efficacy and safety of taspoglutide monotherapy in drug-naive type 2 diabetic patients after 24 weeks of treatment: Results of a randomized, double-blind, placebo-controlled phase 3 study (T-emerge 1) (Diabetes Care) - P3, N=373; HbA(1c) reductions from baseline were greater with taspoglutide 10 and 20mg than PBO (least squares mean [SE] changes: -1.01% [0.07], -1.18% [0.06], and -0.09% [0.07], respectively; both p<0.0001 vs. PBO); Decreases in bodyweight were greater with taspoglutide 10mg (-1.45kg [0.32]) and with 20mg (-2.25kg [0.30]) than PBO (-1.23kg [0.31]; p=0.61 and p=0.02 for taspoglutide 10 and 20mg vs. PBO, respectively)

P3 data • Diabetes

Efficacy and safety of taspoglutide versus sitagliptin for type 2 diabetes mellitus (T-emerge 4 trial) (Diabetes Ther) - P3, N=666; NCT00754988; After 24 weeks, least squares mean (SE) HbA(1c) reductions were greater with taspoglutide 10mg (-1.23% [0.06]) and 20 mg (-1.30% [0.06]) vs sitagliptin (-0.89% [0.06]) or pbo (-0.10% [0.08]); Mean treatment differences with taspoglutide 10mg and 20mg were -0.34 (-0.49, -0.19) and -0.41 (-0.56, -0.26) vs sitagliptin; and -1.13 (-1.31, -0.95) and -1.20 (-1.38, -1.02) vs pbo

P3 data • Diabetes

The fate of taspoglutide, a weekly GLP-1 receptor agonist, versus twice-daily exenatide for type 2 diabetes: The T-emerge 2 trial (Diabetes Care) - P3, N=1,189; NCT00717457; Both doses of taspoglutide reduced HbA(1c) significantly more than exenatide (taspoglutide 10mg: -1.24% [SE 0.09], difference -0.26, -0.37 to -0.15, p<0.0001; taspoglutide 20mg: -1.31% [0.08], difference -0.33, -0.44 to -0.22, p<0.0001; exenatide: -0.98% [0.08]); Taspoglutide reduced body weight (taspoglutide 10mg, -1.6kg; taspoglutide 20 mg, -2.3kg) as did exenatide (-2.3kg), which was greater than with taspoglutide 10mg (p<0.05)

P3 data • Diabetes

Eight weeks of treatment with long-acting GLP-1 analog taspoglutide improves postprandial insulin secretion and sensitivity in metformin-treated patients with type 2 diabetes (Metabolism) - PMID: 23831441; P2, N=80; NCT00423501; Sponsor: Hoffmann-La Roche; "After 8 weeks of treatment, taspoglutide 5, 10, and 20mg QW doses vs. placebo improved mean PPG0-240 min (relative change from baseline: -22.1%, -25.9%, and -22.9% vs. -8.1%; P<0.005) and mean postprandial ISR0-240 min (+14%, +18%, and +23% vs. +1%; P<0.005 vs dose)."

P2 data • Diabetes

Taspoglutide, a once-weekly glucagon-like peptide1 analogue, vs. insulin glargine titrated to target in patients with type 2 diabetes: An open-label randomized trial (Diabet Med) - P3, N=1,049; NCT00755287; After 24 weeks, least-square mean changes from baseline in HbA(1c) in pts receiving taspoglutide 10mg or taspoglutide 20mg were non-inferior to insulin glargine; Treatment difference of (0.07%; -0.06 to 0.21 and -0.14; -0.28 to -0.01, for taspoglutide 10 and 20mg, respectively, vs. insulin glargine) was observed; Compared with insulin glargine, taspoglutide provided non-inferior HbA(1c) reductions associated with less hypoglycaemia, but more gastrointestinal adverse events

P3 data • Diabetes

Efficacy and safety of taspoglutide in patients with type 2 diabetes inadequately controlled with metformin plus pioglitazone over 24 weeks: T-emerge 3 trial (J Clin Endocrinol Metab) - P3, N=326; A greater proportion of taspoglutide-treated patients reached HbA1c target 7% or less (69.8 and 76.1% vs. 35.1%); With taspoglutide 10mg and 20mg vs. pbo, significantly greater reductions in fasting plasma glucose [-1.87mmol/liter (-34mg/dl) and -2.12mmol/liter (-38mg/dl) vs. -0.57mmol/liter (-10mg/dl); p<0.0001], improvements in homeostasis model assessment of β-cell function score (20.65 and 33.52 vs. -2.03; p<0.0001), and significant weight loss (-0.64kg and -1.04kg vs. 0.59kg; p<0.01) were observed

P3 data • Diabetes

PEGylated prodrugs of antidiabetic peptides amylin and GLP-1. (PubMed, J Control Release) - "Specifically, the release kinetics of linker sequences LVPR, LDPR, and LVPRLVPR were tested in combination with GLP-1 analog taspoglutide, amylin, and amylin analog pramlintide in mouse serum. 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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