Chimeric compounds able to bind both SST and dopamine (DA) receptors were synthesized, on the basis of simultaneous presence and heterodimerization of these receptors on the same normal and tumor cells in pituitary gland and gastrointestinal tract, and on the clinical evidence that the cotreatment with octreotide and the DA agonist bromocriptine inhibits GH secretion in acromegalic patients more efficiently than the single agents [54, 84]. Here, SST is linked to neoplasm.