Taspoglutide

Human clinical Weight Loss & Metabolism 2 sources

Taspoglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist originally developed for the treatment of type 2 diabetes. While it demonstrated significant efficacy in improving glycemic control and promoting weight loss in Phase III clinical trials, its development was ultimately halted due to high incidences of gastrointestinal side effects and hypersensitivity reactions.

01Dosing reference

Amount

10-20 mg (historical clinical trial dose)

Frequency

Once weekly

Cycle

Continuous (in historical trials)

Reference figures, not a recommendationThese values reflect amounts described in the literature and vendor documentation this database indexes. Use the reconstitution calculator to convert them into syringe units.

02Mechanism of action

GLP-1 Receptor Activation

Taspoglutide binds to and activates the GLP-1 receptor, mimicking the action of endogenous incretin hormones.

Insulin Secretion & Glucagon Suppression

It stimulates glucose-dependent insulin release from pancreatic beta cells and suppresses glucagon secretion from alpha cells.

Gastric Emptying & Satiety

It slows gastric emptying and promotes satiety in the brain, leading to reduced food intake and subsequent weight loss.

03Human evidence

Significant reductions in HbA1c and body weight compared to placebo and active comparators.

Observed in the T-emerge Phase III clinical trial program involving patients with type 2 diabetes.

High rates of adverse events, particularly nausea, vomiting, and injection-site hypersensitivity reactions.

Observed across multiple Phase III trials, leading to the discontinuation of the drug's development by Roche.

04Preclinical evidence

Demonstrated prolonged half-life and sustained GLP-1 receptor activation compared to native GLP-1.

Pharmacokinetic studies in animal models.

Improved glucose tolerance and stimulated insulin secretion in diabetic animal models.

In vivo studies using rodent models of type 2 diabetes.

05What is known vs. unknown

Reasonably established

Taspoglutide is a long-acting GLP-1 receptor agonist designed for once-weekly subcutaneous administration.
It effectively lowers blood glucose levels (HbA1c) and promotes weight loss in individuals with type 2 diabetes.
Its clinical development was abandoned by Roche in 2010 due to unacceptable rates of gastrointestinal side effects and systemic allergic reactions.
It shares the same fundamental mechanism of action as other successful GLP-1 agonists like exenatide and liraglutide.

Unknowns & limits

The exact immunological mechanism causing the high rate of hypersensitivity reactions remains not fully elucidated.
Long-term cardiovascular outcomes were never fully established since the Phase III program was terminated early.

06Safety & regulatory context

Regulatory statusTaspoglutide is not an FDA-approved medication. Its clinical development was halted in Phase III trials due to a high incidence of severe gastrointestinal side effects (nausea and vomiting) and systemic hypersensitivity (allergic) reactions. As an abandoned investigational drug, it is not legally available for human use and is restricted to preclinical research contexts, if available at all.

07Compared with Exenatide

Taspoglutide vs. Exenatide

Key difference

While both are GLP-1 receptor agonists, exenatide successfully navigated clinical trials and achieved FDA approval, whereas taspoglutide was abandoned due to hypersensitivity reactions.

When researchers discuss each

Researchers discuss exenatide as a pioneering, successful GLP-1 therapy, while taspoglutide is often cited as a case study in drug development failure due to tolerability and immunogenicity issues.

08Glossary

GLP-1 Receptor Agonist

A class of drugs that mimic the incretin hormone GLP-1 to stimulate insulin release and lower blood sugar.

Hypersensitivity Reaction

An exaggerated or inappropriate immune response to a drug, often presenting as an allergic reaction.

Incretin

Metabolic hormones that stimulate a decrease in blood glucose levels by increasing the amount of insulin released from the pancreas.

09Knowledge check

Q1Why was the clinical development of taspoglutide halted?

Q2What is the primary mechanism of action for taspoglutide?

Q3Which limitation in the available clinical evidence most directly prevents firm conclusions about taspoglutide's long-term cardiovascular effects?

Q4When researchers contrast taspoglutide with exenatide in the dossier, which point is emphasized as the key difference?

Q5Which statement best describes taspoglutide's regulatory status and legal availability according to the dossier?

10Sources

More in Weight Loss & Metabolism

See all

AOD-9604

Weight Loss & Metabolism

Human clinical

AOD-9604 is a modified fragment of human growth hormone (HGH) that includes amino acids 177-191. Research indicates it mimics the fat-burning effects of HGH by stimulating lipolysis and inhibiting lipogenesis, without the adverse effects on blood sugar or tissue growth typically associated with full-length HGH.

250-500 mcg/day

MOTS-c

Weight Loss & Metabolism

Early human

MOTS-c is a naturally occurring mitochondrial-derived peptide that plays a key role in regulating metabolic homeostasis and energy production. Research indicates it acts as an 'exercise mimetic' by activating AMPK, improving insulin sensitivity, and enhancing physical performance in animal models.

5-10 mg

GLP3-RT (Retatrutide)

Weight Loss & Metabolism

Human clinical

Retatrutide is an investigational triple hormone receptor agonist that targets GLP-1, GIP, and glucagon receptors. Clinical trials have shown unprecedented weight loss efficacy, surpassing dual agonists, by combining appetite suppression with increased energy expenditure.

N/A - Investigational Drug

Research and educational use onlyNothing on this site is medical advice, a prescription, or a recommendation for human use. Compounds documented here are research chemicals. Consult a qualified clinician before making any health decision.