efatutazone

Efatutazone is a third-generation thiazolidinedione and a highly potent, selective, orally bioavailable agonist of peroxisome proliferator-activated receptor gamma (PPAR-gamma). As a small molecule drug, it binds to and activates PPAR-gamma—a nuclear hormone receptor and ligand-dependent transcription factor—leading to the induction of cell differentiation and apoptosis, which results in reduced cellular proliferation. Efatutazone has demonstrated antineoplastic activity in preclinical models by inhibiting tumor cell proliferation and enhancing apoptosis, especially when combined with cytotoxic agents such as paclitaxel. It was investigated for use in various cancers including lymphoma, liposarcoma, solid tumors, multiple myeloma, recurrent thyroid cancer (notably anaplastic thyroid cancer), metastatic colorectal cancer (in combination with FOLFIRI), and others. Clinical development reached phase 2 trials but has since been discontinued[1][2][3][5][6][7][8].

Other names

efatutazoneinolitazoneefatutazone dihydrochloride