SOM230: a new therapeutic modality for Cushing's disease

A rational drug design approach involving transposition of functional groups from SRIF into a reduced size cyclohexapeptide template has led to the discovery of SOM230, a novel, stable cyclohexapeptide somatostatin mimic which exhibits unique high affinity binding to human somatostatin receptors (sst1-5). This unique receptor subtype binding profile, in particular the exceptional high affinity binding to sst5, led to SOM230 being approved by EMEA and FDA in 2012 as the first effective pituitary directed therapeutic modality for Cushing's disease

The Superior Therapeutic Properties of SOM230 Originate from Unique Structural Elements

A rational drug design approach involving transposition of functional groups from SRIF into a reduced size cyclohexapeptide template has led to the discovery of SOM230, a novel, stable cyclohexapeptide somatostatin mimic which exhibits unique high affinity binding to human somatostatin receptors (sst1-5). SOM230 has potent, long lasting inhibitory effects on growth hormone and insulin-like growth factor-1 release and is a promising development candidate currently under evaluation in phase II clinical trials