The present invention is based on the unexpected discovery that a combination of certain known drugs exhibits synergistic effects in treating metabolic syndrome and various other diseases. In particular, the invention comprises a pharmaceutical composition comprising: (1) a therapeutically effective quantity of a first agent that is Metformin or a salt thereof (2) a therapeutically effective quantity of a second agent that is Aspirin (3) a therapeutically effective quantity of a third agent that serotonin creatinine sulfate complex (4) a non-ionic surfactant and (5) a solvent that is a lower alkanol. A preferred composition comprises metformin hydrochloride, aspirin, and serotonin creatinine sulfate complex for the first, second, and third agents. The invention further comprises methods for the use of these compositions for the treatment of metabolic syndrome, hyperproliferative diseases including cancer, and other diseases and conditions.