Effects
Glitazars combine the lipid-lowering effects of fibrates (lower triglycerides and LDL, increase HDL) with the antidiabetic effect of glitazones, which increase tissue sensitivity to insulin.
Mechanism of action
Glitazars have a dual mechanism of action. On the one hand, they activate the nuclear receptor PPAR-alpha, the drug target of fibrates, and on the other hand, they activate PPAR-gamma, the target of glitazones.
Indications
Metabolic diseases, disorders of blood lipid levels, hyperglycemia or diabetes mellitus, metabolic syndrome.
Active ingredients (selection).
The development of the majority of active ingredients was discontinued because of adverse effects:
| Aleglitazar | Roche Pharma | Development discontinued |
| Farglitazar | GlaxoSmithKline | Development canceled |
| Muraglitazar | Bristol-Myers Squibb | Development discontinued, cardiovascular side effects. |
| Navaglitazar | Eli Lilly | Development canceled |
| Ragaglitazar | NovoNordisk | Development aborted, tumor growth in rodents. |
| Tesaglitazar | AstraZeneca | Development aborted, elevated creatinine, reduced GFR. |
