Everolimus in pituitary tumor: a review of preclinical and clinical evidence

Front Endocrinol (Lausanne). 2024 Dec 16:15:1456922. doi: 10.3389/fendo.2024.1456922. eCollection 2024.

Abstract

Although pituitary tumors (PTs) are mostly benign, some PTs are characterized by low surgical resection rates, high recurrence rates, and poor response to conventional treatments and profoundly affect patients' quality of life. Everolimus (EVE) is the only FDA-approved mTOR inhibitor, which can be used for oral treatment. It effectively inhibits tumor cell proliferation and angiogenesis. It has been administered for various neuroendocrine tumors of the digestive tract, lungs, and pancreas. EVE not only suppresses the growth and proliferation of APT cells but also enhances their sensitivity to radiotherapy and chemotherapy. This review introduces the role of the PI3K/AKT/mTOR pathway in the development of APTs, comprehensively explores the current status of preclinical and clinical research of EVE in APTs, and discusses the blood-brain barrier permeability and safety of EVE.

Keywords: Everolimus; PI3K/AKT/mTOR; blood-brain barrier; pituitary tumor; safety.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents* / therapeutic use
  • Everolimus* / therapeutic use
  • Humans
  • MTOR Inhibitors / therapeutic use
  • Pituitary Neoplasms* / drug therapy
  • Signal Transduction / drug effects
  • TOR Serine-Threonine Kinases / antagonists & inhibitors
  • TOR Serine-Threonine Kinases / metabolism

Substances

  • Everolimus
  • Antineoplastic Agents
  • MTOR Inhibitors
  • TOR Serine-Threonine Kinases

Grants and funding

The author(s) declare that financial support was received for the research, authorship, and/or publication of this article. This study was supported by the National Natural Science Foundation project of China (C031002), Gansu Provincial Science Foundation of China (21JR7RA416) and Lanzhou University Second Hospital's "Cuiying Technology Innovation" Program (CY2018-ZD02).