The invention relates to a pharmaceutical composition comprising as active ingredient an effective amount of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the prophylaxis and therapy of Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy. Another object of the invention concerns the use of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the enhancement of insulin sensitivity and the preservation or increase of ß-cell compensation.