When and How to Use Somatostatin Analogues

• Autores: Wouter W. de Herder
• Localización: Endocrinology and metabolism clinics of North America, ISSN 0889-8529, Vol. 47, Nº. 3, 2018 (Ejemplar dedicado a: Innovations in the Management of Neuroendocrine Tumors), págs. 549-555
• Idioma: inglés
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• Resumen

  • he research group of the winner of the 1977 Nobel Prize in Physiology or Medicine, Roger Guillemin, discovered the peptide hormone somatostatin.

    Somatostatin exerts an inhibitory role in the hormone secretion by the pituitary, pancreas, and gastrointes-tinal tract. It acts via interaction with specific somatostatin receptor (SSTR) subtypes expressed on target tissues. Five human SSTR subtypes have been recognized (named SSTR1–5), each being involved a distinct signaling pathway.

    SSTR2 predominates in gastrointestinal and pancreatic neuroendocrine tumors (GEP-NETs).

    Octreotide was the first biologically stable somatostatin analogue (SSA) that became available.

    This compound binds with high, low, and moderate affinity to SSTR2, SSTR3, and SSTR5, respectively.

    A short-acting immediate-release formula-tion of octreotide (Sandostatin, Novartis, Basel, Switzerland) was initially developed. Along-acting repeatable depot formulation, Sandostatin LAR (Novartis), is currently indicated for long-term treatment of the severe diarrhea and flushing episodes associated with the carcinoid syndrome and long-term treatment of the profuse watery diarrhea associated with VIPomas, as well as for the improvement of progressionfree survival (PFS) in patients with unresectable, well-differentiated or moderately differentiated, locally advanced or metastatic NETs from a midgut origin