pioglitazone + tyrosine kinase inhibitor

Pioglitazone + tyrosine kinase inhibitor (TKI) is a combination therapy investigated primarily for the treatment of chronic myeloid leukemia (CML), especially in patients with suboptimal response to TKI monotherapy. Pioglitazone is a thiazolidinedione class drug and acts as an agonist of peroxisome proliferator-activated receptor gamma (PPARγ), while TKIs such as imatinib, dasatinib, nilotinib, or ponatinib inhibit the BCR-ABL fusion protein's tyrosine kinase activity. The rationale for this combination is that CML stem cells are often resistant to TKIs due to their quiescent state; activation of PPARγ by pioglitazone can drive these cells out of quiescence and sensitize them to TKI-induced apoptosis. Clinical studies have shown that adding pioglitazone to ongoing TKI therapy can lead to deeper molecular responses and may help eradicate residual leukemic stem cells[2][3][4][5]. This approach has been well tolerated in clinical settings.

Brand names

GleevecSprycelTasignaBosulifIclusig

Other names

pioglitazone + TKIpioglitazone plus tyrosine kinase inhibitorpioglitazone and TKI