Taspoglutide
A once-weekly GLP-1 analogue that lowered glucose but was stopped for intolerance and hypersensitivity
Taspoglutide is a human GLP-1 analogue made resistant to the enzyme DPP-4 and given once a week. Its phase 3 T-emerge trials lowered HbA1c and weight, but development stopped because of gastrointestinal intolerance and serious hypersensitivity reactions, and no regulator approved it.
What is it?
Taspoglutide was built as a human GLP-1 analogue resistant to DPP-4, the enzyme that destroys native GLP-1 within minutes, and formulated for weekly injection. Early trials looked promising: in eight weeks on metformin, HbA1c fell by about a point at every dose and post-meal insulin secretion rose.
In the T-emerge programme taspoglutide did what a GLP-1 agonist should: HbA1c fell by about a percentage point, more than with sitagliptin or twice-daily exenatide and as much as with insulin glargine, with some weight loss. The trouble was tolerability and immunity. Nausea and vomiting were common, allergic and injection-site reactions exceeded the comparators', and about half of patients developed anti-taspoglutide antibodies.
T-emerge 3 shows the trade clearly: on top of metformin and pioglitazone, HbA1c fell 1.4 points against 0.45 on placebo, while up to 44% had nausea, a quarter vomited and a quarter had injection-site reactions. Supporting studies filled in the rest: exposure rose with kidney impairment, varied by injection site, and did not interact with common drugs.
Discontinuations ran higher than expected, and the programme was stopped; a 2015 analysis names gastrointestinal intolerance and serious hypersensitivity reactions as the reasons. Drugs@FDA lists no application. Its afterlife is scientific: its structure bound to the GLP-1 receptor has been solved alongside semaglutide's, and thyroid work with it supported the view that human C-cells carry little GLP-1 receptor.
Mechanism of Action
Taspoglutide is a DPP-4-resistant human GLP-1 analogue designed for once-weekly injection; it activates the GLP-1 receptor like the rest of the class.
GLP-1 receptor
Cryo-electron microscopy shows it binding the receptor much as GLP-1 does, with different motions within the receptor than semaglutide.
Insulin after meals
Raised post-meal insulin secretion and lowered post-meal glucose in metformin-treated patients.
DPP-4 resistant
Designed to resist the enzyme that inactivates native GLP-1, enabling weekly dosing.
Published Research
Phase 3 trials and a cardiovascular analysis read from their PubMed abstracts; taspoglutide has no label.
A single dose in type 2 diabetes
In 48 patients, single doses lowered 24-hour and post-meal glucose for up to 14 days at 30 mg, with dose-dependent, transient gastrointestinal events, supporting weekly dosing.
T-emerge 1: monotherapy
In drug-naive type 2 diabetes, 24 weeks of taspoglutide 10 or 20 mg weekly cut HbA1c by 1.01 and 1.18 points against 0.09 on placebo; weight fell more only on 20 mg (-2.25 against -1.23 kg), and GI and injection-site events were more common.
T-emerge 2: against exenatide
Weekly taspoglutide controlled glucose better than twice-daily exenatide, but nausea (53-59% against 35%) and vomiting (33-37% against 16%) were more frequent, allergic and injection-site reactions more common, and antibodies appeared in 49%.
T-emerge 4: against sitagliptin
Taspoglutide outperformed sitagliptin on HbA1c and weight, but GI, allergic and injection-site reactions drove higher discontinuation, and anti-taspoglutide antibodies were confirmed in 46%.
Against insulin glargine
HbA1c reductions on taspoglutide 10 and 20 mg (-0.91% and -0.98%) were non-inferior to titrated glargine (-0.84%), with more gastrointestinal events and significantly less hypoglycaemia.
T-emerge 7: obese patients
In obese adults with type 2 diabetes, 24 weeks of taspoglutide lowered HbA1c by 0.81% against 0.09% on placebo and weight by 3.2 against 1.9 kg; nausea and vomiting were the commonest adverse events.
Against exenatide after meals
Weekly taspoglutide and twice-daily exenatide improved post-meal glucose to a similar extent, but only taspoglutide raised post-meal insulin from baseline.
T-emerge 3: on metformin and pioglitazone
Over 24 weeks, HbA1c fell 1.35 and 1.40 points on 10 and 20 mg against 0.45 on placebo, but nausea (35% and 44%), vomiting (21% and 24%) and injection-site reactions (24%) were far more common than on placebo.
Phase 2 with metformin
After 8 weeks, HbA1c fell 0.9 to 1.2 points across weekly and fortnightly doses against 0.2 on placebo, with up to 2.8 kg weight loss; nausea was dose-dependent and transient.
Higher doses tested
In 129 patients titrated from 20 mg to 30 or 40 mg weekly, gastrointestinal adverse events did not increase with titration, and 53% to 72% reached HbA1c under 7% against 19% on placebo.
Beta-cell function after 8 weeks
In metformin-treated patients, 5 to 20 mg weekly lowered post-meal glucose by 22% to 26% and raised post-meal insulin secretion by 14% to 23%, against small changes on placebo.
Kidney impairment
Exposure rose as kidney function fell: total exposure was 38% and peak level 93% higher in severe renal impairment, with more gastrointestinal side effects.
Where to inject
In healthy overweight volunteers, exposure differed by injection site, with the lowest peak and the least nausea and vomiting after abdominal injection, which was therefore recommended.
Drug interactions
Repeated taspoglutide doses did not change the pharmacokinetics of digoxin, an oral contraceptive, lisinopril, warfarin or simvastatin enough to need dose adjustment.
Cardiovascular safety and the stop
Pooled trial data showed no excess cardiovascular risk (hazard ratio 0.94, 95% CI 0.57-1.56); longer-term data never came because development stopped over gastrointestinal intolerance and serious hypersensitivity reactions.
Against pioglitazone
In 760 patients on a sulphonylurea with or without metformin, taspoglutide matched pioglitazone on glucose with weight loss instead of gain, but more GI and injection-site events; higher-than-expected discontinuations stopped the programme.
Thyroid C-cells: rat against human
Taspoglutide and liraglutide modestly raised calcitonin in rat thyroid C-cell cultures but had no effect in human cultures, which showed little or no GLP-1 receptor.
Dosing Data
It was never approved. Phase 3 trials used 10 or 20 mg once weekly under the skin, preferably into the abdomen.
Educational information, not medical advice. Each dose above is tagged with its source: an approved label, a published human study, animal data, or amounts reported by users. None is a recommendation for you. An unapproved compound has no established safe or effective human dose, and products sold for “research use only” are not made or tested for people. Talk to a doctor before acting on anything on this site, including before you start, stop or change any medicine or dose. Full medical disclaimer.
Side Effects & Contraindications
Reported Side Effects
From the trials.
Contraindications & Cautions
No label exists.
Legal Status
Never approved.
Frequently Asked Questions
?Why was taspoglutide stopped?
Because of gastrointestinal intolerance and serious hypersensitivity reactions, which drove high discontinuation in the T-emerge trials.
?Did it work?
On glucose, yes: HbA1c fell about a point, more than with sitagliptin or twice-daily exenatide.
?Is it sold anywhere?
No regulator approved it, and Drugs@FDA lists no application.
?What were the antibodies?
Anti-taspoglutide antibodies were confirmed in 46% of patients in T-emerge 4 and 49% in T-emerge 2, alongside more allergic reactions than with the comparators.
References
- [clinical-trial] Kapitza C, et al. "Pharmacokinetic and pharmacodynamic properties of taspoglutide, a once-weekly, human GLP-1 analogue, after single-dose administration in patients with Type 2 diabetes." Diabet Med, 2009;26(11):1156-64. PMID: 19929995.
- [clinical-trial] Raz I, et al. "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, 2012;35(3):485-7. PMID: 22301126.
- [clinical-trial] Rosenstock J, et al. "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, 2013;36(3):498-504. PMID: 23139373.
- [clinical-trial] Bergenstal RM, et al. "Efficacy and safety of taspoglutide versus sitagliptin for type 2 diabetes mellitus (T-emerge 4 trial)." Diabetes Ther, 2012;3(1):13. PMID: 23138449.
- [clinical-trial] Nauck M, et al. "Taspoglutide, a once-weekly glucagon-like peptide 1 analogue, vs. insulin glargine titrated to target in patients with Type 2 diabetes: an open-label randomized trial." Diabet Med, 2013;30(1):109-13. PMID: 22937895.
- [review] Seshasai SR, et al. "Cardiovascular safety of the glucagon-like peptide-1 receptor agonist taspoglutide in people with type 2 diabetes: an individual participant data meta-analysis of randomized controlled trials." Diabetes Obes Metab, 2015;17(5):505-10. PMID: 25656522.
- [clinical-trial] Pratley RE, et al. "Efficacy and tolerability of taspoglutide versus pioglitazone in subjects with type 2 diabetes uncontrolled with sulphonylurea or sulphonylurea-metformin therapy: a randomized, double-blind study (T-emerge 6)." Diabetes Obes Metab, 2013;15(3):234-40. PMID: 22958426.
- [clinical-trial] Hollander P, et al. "Effects of taspoglutide on glycemic control and body weight in obese patients with type 2 diabetes (T-emerge 7 study)." Obesity (Silver Spring), 2013;21(2):238-47. PMID: 23404788.
- [clinical-trial] Gastaldelli A, et al. "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, 2014;16(2):170-8. PMID: 23911196.
- [pubmed] Henry RR, et al. "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, 2012;97(7):2370-9. PMID: 22539590.
- [pubmed] Nauck MA, et al. "Treatment with the human once-weekly glucagon-like peptide-1 analog taspoglutide in combination with metformin improves glycemic control and lowers body weight in patients with type 2 diabetes inadequately controlled with metformin alone: a double-blind placebo-controlled study." Diabetes Care, 2009;32(7):1237-43. PMID: 19366970.
- [pubmed] Ratner R, et al. "Safety and tolerability of high doses of taspoglutide, a once-weekly human GLP-1 analogue, in diabetic patients treated with metformin: a randomized double-blind placebo-controlled study." Diabet Med, 2010;27(5):556-62. PMID: 20536952.
- [pubmed] Gastaldelli A, et al. "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, 2013;62(9):1330-9. PMID: 23831441.
- [pubmed] Giraudon M, et al. "Effect of varying degrees of renal impairment on the pharmacokinetics and tolerability of taspoglutide." Diabetes Obes Metab, 2017;19(4):537-544. PMID: 27981717.
- [pubmed] Sturm-Pellanda C, et al. "Subcutaneous Bioavailability of Taspoglutide at 3 Different Injection Sites in Healthy Overweight/Obese Subjects." Clin Ther, 2015;37(11):2439-48. PMID: 26412802.
- [pubmed] Bogman K, et al. "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." Clin Pharmacokinet, 2019;58(9):1205-1214. PMID: 30968335.
- [pubmed] Boess F, et al. "Effect of GLP1R agonists taspoglutide and liraglutide on primary thyroid C-cells from rodent and man." J Mol Endocrinol, 2013;50(3):325-36. PMID: 23463748.
Sources & Citations
Studies were read from their PubMed abstracts; no label exists. Read October 6, 2026.
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