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Metabolic Stabilization

Corresponding ligands

chGRPR (Tx)
Metabolically Unstable Biovector

Improved Protease Resistance

Current receptor-targeted peptide radiopharmaceuticals often derive from endogenous regulatory peptides. It is therefore not surprising that these ligands often exhibit only suboptimal metabolic stability in vivo. 

Especially in the context of radioligand therapy, ligands with high metabolic stability and optimized pharmacokinetic profiles are favoured. One such example is AMTG, a therapeutic antagonist that binds with low nanomolar activity to gastrin-releasing peptide receptors (GRPR; BB2). 

Apart from being remarkably better in vivo stability, this RM2 analogue offers improved preclinical parameters; such as higher affinity.