Authors: Monica R Gadelha Luiz Eduardo Wildemberg Marcello D Bronstein Federico Gatto Diego Ferone
Publish Date: 2017/02/07
Volume: 20, Issue: 1, Pages: 100-108
Abstract
Firstgeneration 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 firstgeneration 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 Ecadherin ZAC1 filamin A and βarrestin expression in the somatotropinomas In patients resistant to firstgeneration 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 nextgeneration 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 firstline therapy a shift from a trialanderror treatment to a personalized one could be possibleMRG 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
Keywords: