The use of drugs interfering with somatostatin receptors (ssR) is now consolidated practice in diagnostics and therapy, stimulating the development of new and more efficient molecules offering improved pharmacodynamics. Over the years, we have passed from the use of native somatostatin to mini-somatostatin and then octapeptides, above all octreotide. Subsequently, peptides were synthesized with specific affinities for a single receptorial subtype, like compound BIM23268 and compound CH275. More recently, somatostatin analogs were synthesized with a non-peptide structure. Another important aspect in the history of sst analogs is represented by the development of new pharmaceutical formulas for these drugs in order to improve patient compliance by reducing dose frequency.