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Aleglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that was developed by Hoffmann-La Roche as an oral treatment for type 2 diabetes. Its large Phase III cardiovascular outcomes trial (AleCardio) was halted early for safety signals and lack of efficacy, and all development was discontinued in 2013.
- Studied for improving insulin sensitivity and lipid profile in type 2 diabetes
- Intended to combine glucose-lowering and cardiovascular benefit in one drug
- Increased heart failure, gastrointestinal bleeding, and renal dysfunction in its major cardiovascular outcomes trial
Overview
Another dual PPAR agonist that promised better glucose and lipid control but ran into the same cardiovascular safety wall that killed similar drugs like muraglitazar and tesaglitazar.
Mechanism
Aleglitazar activates both PPAR-alpha and PPAR-gamma nuclear receptors. PPAR-gamma activation improves sensitivity and lowers blood glucose, while PPAR-alpha activation improves lipid profiles by lowering triglycerides and raising HDL cholesterol. This dual activation was intended to address both glycemic control and cardiovascular risk factors in type 2 diabetes.
receptor fingerprint
PPAR-alphaAgonist
PPAR-gammaAgonist
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
In the Phase III AleCardio trial in patients with type 2 diabetes and recent acute coronary syndrome, aleglitazar did not reduce cardiovascular events and was associated with increased rates of heart failure, gastrointestinal bleeding, bone fractures, and renal dysfunction. The trial was stopped early for futility and safety concerns, leading Roche to terminate all aleglitazar studies in 2013.
Subjective profileweighing the evidence above
Dead, and rightly so. The dual-PPAR idea was reasonable on paper, but the big outcomes trial found no cardiovascular benefit alongside more heart failure, gastrointestinal bleeding, fractures and kidney trouble, and was stopped early. Nothing about that result invites a second look.
Resources
This entry is here for reference.
Research
1 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
What is Aleglitazar used for?
It was developed as a treatment for type 2 diabetes intended to improve blood sugar and lipid levels, but it was never approved after its cardiovascular safety trial failed.
How does Aleglitazar work?
It activates both PPAR-alpha and PPAR-gamma receptors, nuclear receptors that regulate glucose and lipid metabolism, to improve insulin sensitivity and cholesterol/triglyceride levels.
Is Aleglitazar well-researched?
Yes, relative to many discontinued compounds; it was tested in a large Phase III cardiovascular outcomes trial (over 7,000 patients) that was published in JAMA, which showed it failed to reduce cardiovascular risk and raised safety concerns.
Limitations of the evidence
- No reduction in cardiovascular death, MI, or stroke versus placebo
- Trial terminated early for safety and futility
Adverse effects
- Increased heart failure, gastrointestinal bleeding, and renal dysfunction in its major cardiovascular outcomes trial