Table 6.
Side Effects of Dual/Pan PPAR Agonists (Ligands)
| Dual/pan PPAR Modulators | Side Effect | Cause of Side Effects | Remarks |
|---|---|---|---|
| 1. Dual (PPAR α/γ) | |||
| Tesaglitazar (1) |
Anaemia, leucopenia, renal failure, fibrosarcomas, | Stimulation of DNA synthesis [24] | Discontinued in 2006 |
| Muraglitazar (2) |
Heart failure, myocardial infarction and stroke | Blocks calcium channel [13] | Discontinued in 2006 |
| Ragaglitazar (4) |
Anaemia, oedema, and urinary tract cancer in rodents | Causes overexpresssion of early growth response-1 (EGr-1), phosphorylation of c-Jun and ribosomal S protein [25, 26] | Discontinued in 2006 |
| Imiglitazar (6) |
Liver dysfunction | Effect of cytochrome p450? | Suspended in 2004 |
| 2. Pan PPAR (α/β,δ/γ ) agonists | |||
| Benzafibrate (9) |
|||
| Chiglitazar (10) |
None reported | None reported | Currently in Phase II |
| Netoglitazone | None reported | None reported | |