Phenformin (PFM)

Phenformin is an antidiabetic drug from the biguanide class. Phenformin hydrochloride is a white crystalline powder, with a melting point of 175 to 178°C; it is soluble at 1 in 8 parts of water and 1 in 15 of ethanol, and practically insoluble in chloroform and ether. Phenformin is well absorbed after oral administration. The major metabolic reaction is aromatic hydroxylation to form 4–hydroxyphenformin, which is then conjugated with glucuronic acid. Phenformin, along with buformin and metformin, inhibits the growth and development of cancer. The anticancer property of these drugs may be due to their ability to disrupt the Warburg effect and revert the cytosolic glycolysis characteristic of cancer cells to normal oxidation of pyruvate by the mitochondria.[14] Metformin reduces liver glucose production in diabetics and disrupts the Warburg effect in cancer by AMPK activation and inhibition of the mTor pathway.