The Superior Therapeutic Properties of SOM230 Originate from Unique Structural Elements

Abstract

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.

Keywords

• Cyclohexapeptide template
• Solid phase synthesis
• Srif analogue
• Superior therapeutic properties