Pioglitazon synes at virke via aktivering af specifikke kernereceptorer (peroxisom proliferator- aktiveret receptor gamma), der medfører forøget insulinfølsomhed i lever -, fedt - og skeletmuskelceller hos dyr.
Pioglitazone appears to act via activation of specific nuclear receptors (peroxisome proliferator activated receptor gamma) leading to increased insulin sensitivity of liver, fat and skeletal muscle cells in animals.