Targeted therapy with kinase inhibitors in aggressive endocrine tumors

Vincenzo Marotta, Maria Domenica Franzese, Michela Del Prete, Maria Grazia Chiofalo, Valeria Ramundo, Raffaella Esposito, Francesca Marciello, Luciano Pezzullo, Annachiara Carratù, Mario Vitale, Annamaria Colao, Antongiulio Faggiano

Research output: Contribution to journalArticlepeer-review


Introduction: Kinase inhibitors (KIs) are a class of anticancer drugs that inhibit activity of the enzymes protein kinases, which regulate crucial cellular processes and have a demonstrated role in human oncogenesis. Treatment of advanced forms of endocrine cancer which are not responsive to cytotoxic chemotherapies is challenging and use of KIs is gaining a growing role in this field. Areas covered: The authors summarize the main genetic alterations known to be linked to endocrine tumors, indicating the rationale for utilizing KIs. Furthermore, they present an updated analysis of clinical trials available on PubMed Central, which were pertinent to the activities of KIs in aggressive endocrine cancer. The authors also discuss the adverse effects of KIs and summarize likely involved underlying mechanisms. Expert opinion: KIs are effective in obtaining a radiological disease control and an improvement of progression-free survival in several forms of endocrine cancer but will never deliver a knockout blow of the disease, due to mechanisms of adaptation to circumvent the specific molecular blockade. The new frontier of KIs treatment is to identify agents that could synergize activity of KIs. The true goal will be to perform an overall genotyping of each tumor, thus predicting the impact of combined targeted therapies in the context of a particular constellation of mutant genes.

Original languageEnglish
Pages (from-to)1187-1203
Number of pages17
JournalExpert Opinion on Pharmacotherapy
Issue number9
Publication statusPublished - Jun 2013


  • Cancer therapy
  • Endocrine tumors
  • Kinase inhibitors
  • Protein kinases

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology


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