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Pituitary

, Volume 20, Issue 1, pp 100–108 | Cite as

Somatostatin receptor ligands in the treatment of acromegaly

  • Monica R. Gadelha
  • Luiz Eduardo Wildemberg
  • Marcello D. Bronstein
  • Federico Gatto
  • Diego Ferone
Article

Abstract

First-generation somatostatin receptors ligands (SRL) are the mainstay in the medical treatment of acromegaly, however the percentage of patients controlled with these drugs significantly varies in the different studies. Many factors are involved in the resistance to SRL. In this review, we update the physiology of somatostatin and its receptors (sst), the use of SRL in the treatment of acromegaly and the factors involved in the response to these drugs. The SRL act through interaction with the sst, which up to now have been characterized as five subtypes. The first-generation SRL, octreotide and lanreotide, are considered sst2 specific and have biochemical response rates varying from 20 to 70%. Tumor volume reduction can be found in 36–75% of patients. Several factors may determine the response to these drugs, such as sst, AIP, E-cadherin, ZAC1, filamin A and β-arrestin expression in the somatotropinomas. In patients resistant to first-generation SRL, alternative medical treatment options include: SRL high dose regimens, SRL in combination with cabergoline or pegvisomant, or the use of pasireotide. Pasireotide is a next-generation SRL with a broader pattern of interaction with sst. In the light of the recent increase of treatment options in acromegaly and the deeper knowledge of the determinants of response to the current first-line therapy, a shift from a trial-and-error treatment to a personalized one could be possible.

Keywords

Somatostatin receptor ligands Acromegaly Somatostatin receptors Octreotide Lanreotide Pasireotide 

Notes

Compliance with ethical standards

Conflict of interest

MRG has received unrestricted research grants and lecture fees from Novartis, Ipsen and Pfizer, has participated on advisory boards of Novartis and Ionis and is PI in clinical trials by Novartis and Ipsen. LEW has no conflicts of interest to declare. MDB is speaker for Ipsen and Novartis; member of Steering Committees of Chiasma, Ipsen and Novartis; PI of clinical trials of Ipsen, Novartis and Pfizer. FG is speaker for Novartis and participated on advisory boards of Novartis, AMCo Ltd. and IONIS Pharmaceuticals. DF is speaker, participated on advisory boards and received research grants from Novartis and Ipsen.

Ethical approval

This article does not contain any studies with human participants performed by any of the authors as it is a review.

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Copyright information

© Springer Science+Business Media New York 2017

Authors and Affiliations

  • Monica R. Gadelha
    • 1
    • 2
  • Luiz Eduardo Wildemberg
    • 1
    • 2
  • Marcello D. Bronstein
    • 3
  • Federico Gatto
    • 4
  • Diego Ferone
    • 4
    • 5
  1. 1.Neuroendocrinology Research Center/Endocrinology Section, Medical School and Hospital Universitário Clementino Fraga FilhoUniversidade Federal do Rio de JaneiroRio de JaneiroBrazil
  2. 2.Neuroendocrinology Section and Molecular Genetics Laboratory, Secretaria Estadual de Saúde do Rio de JaneiroInstituto Estadual do Cérebro Paulo NiemeyerRio de JaneiroBrazil
  3. 3.Neuroendocrine Unit, Division of Endocrinology and Metabolism, Hospital das ClinicasUniversity of Sao Paulo Medical SchoolSão PauloBrazil
  4. 4.Endocrinology Unit, Department of Internal Medicine and Medical Specialties and Center of Excellence for Biomedical ResearchUniversity of GenoaGenoaItaly
  5. 5.IRCCS AOU San Martino-IST GenoaGenoaItaly

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