Estrogens in the Feedback Regulation of Gonadotropin Secretion in Men: Effects of Administration of Estrogen to Agonadal Subjects and the Antiestrogen Tamoxifen and the Aromatase Inhibitor δ‘-Testolactone to Eugonadal Subjects

Gooren, Louis; Veen, E. A. Van Der; Kessel, H. Van; Harmsen‐Louman, W.

doi:10.1111/j.1439-0272.1984.tb00414.x

Cited by 17 publications

(4 citation statements)

References 22 publications

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“…Studies in men with aromatase deficiency provided evidence that estrogens are required for the negative feedback on LH secretion (6). The evidence comes also from studies with aromatase inhibitors and tamoxifen, which, by reducing tissue estrogen availability and by blocking central estrogen receptors, reduce the negative feedback of estrogen derived from testosterone on gonadotropin secretion (9). In the current study, we found that tamoxifen stimulates LH, FSH, and testosterone production, responses expected from the abrogation of estrogen-mediated feedback inhibition (Fig.…”

Section: Discussionmentioning

confidence: 97%

“…Thus, the pharmacological effects of tamoxifen are unique because it simultaneously probes peripheral endocrine and central paracrine effects of estrogen. The central estrogen antagonism of tamoxifen is well established, especially on the regulation of the gonadal axis in men (9,10). Raloxifene, a newer generation SERM, is widely used for the treatment of osteoporosis in both men and women because of its estrogen-like effects on bone (11).…”

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confidence: 99%

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Neuroendocrine Regulation of Growth Hormone and Androgen Axes by Selective Estrogen Receptor Modulators in Healthy Men

Birzniece

Sata

Sutanto

2010

The Journal of Clinical Endocrinology & Metabolism

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Section: Discussionmentioning

confidence: 97%

mentioning

confidence: 99%

Neuroendocrine Regulation of Growth Hormone and Androgen Axes by Selective Estrogen Receptor Modulators in Healthy Men

Birzniece

Sata

Sutanto

2010

The Journal of Clinical Endocrinology & Metabolism

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“…The present study shows that tamoxifen predictably reduced GH secretion through a central estrogen antagonistic effect. E 2 derived from aromatisation also mediates the negative feedback of testosterone on LH secretion (3,24). Thus, by blocking central estrogen action, tamoxifen removes testosterone feedback inhibition, enhancing LH secretion and increasing testosterone production in men (5).…”

Section: Discussionmentioning

confidence: 99%

Estrogen receptor antagonism uncovers gender-dimorphic suppression of whole body fat oxidation in humans: differential effects of tamoxifen on the GH and gonadal axes

Birzniece

2015

European Journal of Endocrinology

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Context: Tamoxifen, a selective estrogen receptor modulator, suppresses GH secretion in women but not in men. It increases testosterone levels in men. As GH and testosterone stimulate fat metabolism, the metabolic consequences of tamoxifen may be greater in women than in men. Objective: To determine whether tamoxifen suppresses fat oxidation (Fox) to a greater degree in women than in men.Design: An open-label study of ten healthy postmenopausal women and ten healthy men receiving 2-week treatment with tamoxifen (20 mg/day). Endpoint measures: GH response to arginine stimulation, serum levels of IGF1, testosterone and LH (men only), sex hormone binding globulin (SHBG) and whole body basal and postprandial Fox. Results: In women, tamoxifen significantly reduced the mean GH response to arginine stimulation (D K87%, P!0.05) and circulating IGF1 levels (D K23.5G5.4%, P!0.01). Tamoxifen reduced postprandial Fox in women (D K34.6G10.3%; P!0.05). In men, tamoxifen did not affect the GH response to arginine stimulation but significantly reduced mean IGF1 levels (D K24.8G6.1%, P!0.01). Tamoxifen increased mean testosterone levels (D 52G14.2%; P!0.01). Fox was not significantly affected by tamoxifen in men. Conclusion: Tamoxifen attenuated the GH response to stimulation and reduced postprandial Fox in women but not in men. We conclude that at a therapeutic dose, the suppressive effect of tamoxifen on fat metabolism is gender-dependent. Higher testosterone levels may mitigate the suppression of GH secretion and Fox during tamoxifen treatment in men.

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“…They maintained serum testosterone and estradiol at constant physiological levels with infusion of testosterone, and then compared serum luteinising hormone (LH) and follicle stimulating hormone (FSH) levels before and during testolactone and estradiol administration, and no differences were found. Gooren et al [102] have investigated the impact of estrogens in the feedback regulation of gonadotropin secretion. They have studied basal and luteinizing hormone-releasing hormone (LRH)-stimulated gonadotropin in a group of orchidectomized male-to-female transsexuals on estrogen treatment.…”

Section: Fertility and Sterilitymentioning

confidence: 99%

Testolactone: The Rise and Fall of a Drug

Savić

Kuzminac

Nikolić

2023

DDC

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Testolactone is structurally related to testosterone and belongs to the first generation of aromatase inhibitors. It is a non-selective irreversible aromatase enzyme inhibitor that was one of the first steroids used in the clinical treatment of breast cancer. The use of testolactone in the treatment of breast cancer started in 1970, although its ability to inhibit aromatase was not discovered until 1975. Its use was primarily based on the inhibition of estrogen synthesis, which was applied in the treatment of estrogen-dependent breast cancers, in the treatment of disorders of sex steroid excess, familial male-limited precocious puberty, or in the treatment of patients with McCune–Albright syndrome, etc. The weak inhibitory activity of testolactone, and the moderate clinical response, prevented its widespread use, which ultimately resulted in withdrawal from the drug market in 2008. This review paper is dedicated to testolactone, its rise in the second half of the 20th century, and its fall in the first decade of the 21st century. Regardless of withdrawal from the market, for many years testolactone was a drug that improved the quality of life of patients facing one of the most serious diseases today, and for this reason, this paper describes medicinal application, synthesis, and modifications of testolactone.

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Estrogens in the Feedback Regulation of Gonadotropin Secretion in Men: Effects of Administration of Estrogen to Agonadal Subjects and the Antiestrogen Tamoxifen and the Aromatase Inhibitor δ‘-Testolactone to Eugonadal Subjects

Cited by 17 publications

References 22 publications

Neuroendocrine Regulation of Growth Hormone and Androgen Axes by Selective Estrogen Receptor Modulators in Healthy Men

Neuroendocrine Regulation of Growth Hormone and Androgen Axes by Selective Estrogen Receptor Modulators in Healthy Men

Estrogen receptor antagonism uncovers gender-dimorphic suppression of whole body fat oxidation in humans: differential effects of tamoxifen on the GH and gonadal axes

Testolactone: The Rise and Fall of a Drug

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