Tibolone as Hormonal Therapy and Neuroprotective Agent.

Juan Pablo Del Río, Santiago Molina, Oscar Hidalgo-Lanussa, Luis Miguel Garcia-Segura, George E Barreto

Journal: Trends in endocrinology and metabolism: TEM 2021;31(10):742-759

PMID: 32507541

Full Text on Elsevier Science View on PubMed

Abstract

Tibolone (TIB), a selective tissue estrogenic activity regulator (STEAR) in clinical use by postmenopausal women, activates hormonal receptors in a tissue-specific manner. Estrogenic activity is present mostly in the brain, vagina, and bone, while the inactive forms predominate in the endometrium and breast. Conflicting literature on TIB's actions has been observed. While it has benefits for vasomotor symptoms, bone demineralization, and sexual health, a higher relative risk of hormone-sensitive cancer has been reported. In the brain, TIB can improve mood and cognition, neuroinflammation, and reactive gliosis. This review aims to discuss the systemic effects of TIB on peri- and post-menopausal women and its role in the brain. We suggest that TIB is a hormonal therapy with promising neuroprotective properties.

Address: Reproductive Health Research Institute, Santiago, Chile; Translational Psychiatry Laboratory, Clínica Psiquiátrica Universitaria, Hospital Clínico, Universidad de Chile, Santiago, Chile; Millennium Nucleus to Improve the Mental Health of Adolescents and Youths (Imhay), Santiago, Chile.; Tallahassee Community College, Tallahassee, FL, USA.; Departamento de Nutrición y Bioquímica, Pontificia Universidad Javeriana, Bogotá, Colombia.; Instituto Cajal, CSIC, Madrid, Spain; Centro de Investigación Biomédica en Red Fragilidad y Envejecimiento Saludable (CIBERFES), Instituto de Salud Carlos III, Madrid, Spain.; Department of Biological Sciences, School of Natural Sciences, University of Limerick, Limerick, Ireland; Health Research Institute, University of Limerick, Limerick, Ireland. Electronic address: [email protected].

DOI: 10.1016/j.tem.2020.04.007

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MeSH Terms: Brain, Estrogen Receptor Modulators, Female, Humans, Menopause, Neuroprotective Agents, Norpregnenes