Short and long term effects of tibolone in postmenopausal women

Formoso, Giulio; Perrone, Enrica; Maltoni, Susanna; Balduzzi, Sara; D'Amico, Roberto; Bassi, Maria Chiara; Basevi, Vittorio; Marata, Anna Maria; Magrini, Nicola; Maestri, Emilio

doi:10.1002/14651858.cd008536.pub2

Cited by 36 publications

(36 citation statements)

References 68 publications

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“…Similar results have been reported in randomized clinical trials for selective estrogen receptor modulators and other hormonally active compounds (including raloxifene 266,267 and tibolone, 268 a commonly used therapy in Europe with both estrogenic and androgenic properties). Raloxifene (60 mg versus placebo) had no effect on the risk of nonfatal stroke (HR, 1.10; 95% CI, 0.92-1.32) but increased the risk of fatal strokes (HR, 1.49; 95% CI, 1.00-1.24; P=0.05).…”

Section: May 2014supporting

confidence: 80%

Guidelines for the Prevention of Stroke in Women

Bushnell¹,

McCullough²,

Awad³

et al. 2014

Stroke

772

414

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1545Purpose-The aim of this statement is to summarize data on stroke risk factors that are unique to and more common in women than men and to expand on the data provided in prior stroke guidelines and cardiovascular prevention guidelines for women. This guideline focuses on the risk factors unique to women, such as reproductive factors, and those that are more common in women, including migraine with aura, obesity, metabolic syndrome, and atrial fibrillation. Results-We provide current evidence, research gaps, and recommendations on risk of stroke related to preeclampsia, oral contraceptives, menopause, and hormone replacement, as well as those risk factors more common in women, such as obesity/metabolic syndrome, atrial fibrillation, and migraine with aura. Conclusions-To more accurately reflect the risk of stroke in women across the lifespan, as well as the clear gaps in current risk scores, we believe a female-specific stroke risk score is warranted. (Stroke. 2014;45:1545-1588.)

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Section: May 2014supporting

confidence: 80%

Guidelines for the Prevention of Stroke in Women

Bushnell¹,

McCullough²,

Awad³

et al. 2014

Stroke

772

414

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“…Tibolone (OrgOD14) is a unique single-agent, tissue-selective agent for symptomatic postmenopausal women. Its metabolites have estrogenic, progestagenic, and androgenic properties 2 . Both, its 3a-OH metabolite (Org4094), and 3b-OH metabolite (Org30126) bind to estrogen receptor (ER) alpha, while its D-metabolite (OM38) binds to the androgen-(AR), and progesterone receptor (PR) 3 .…”

Section: Introductionmentioning

confidence: 99%

The impact of testosterone, tibolone and black cohosh on purified mammary and placental 17β-hydroxysteroid dehydrogenase type 1

Stute

Kalkhake

Kiesel³

et al. 2014

Journal of Enzyme Inhibition and Medicinal Chemistry

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Context: Mammary and placental 17b-hydroxysteroid dehydrogenase type 1 (17bHSD1). Objective: To assess the impact of testosterone, tibolone, and black cohosh on purified mammary and placental 17bHSD1. Materials and methods: 17bHSD1 was purified from human mammary gland and placenta by column chromatography, its activity was monitored by a radioactive activity assay, and the degree of purification was determined by gel electrophoresis. Photometric cofactor transformation analysis was performed to assess 17bHSD1 activity without or in presence of testosterone, tibolone and black cohosh. Results: 17bHSD1 from both sources displayed a comparable basal activity. Testosterone and tibolone metabolites inhibited purified mammary and placental 17bHSD1 activity to a different extent, whereas black cohosh had no impact. Discussion: Studies on purified enzymes reveal the individual action of drugs on local regulatory mechanisms thus helping to develop more targeted therapeutic intervention. Conclusion: Testosterone, tibolone and black cohosh display a beneficial effect on local mammary estrogen metabolism by not affecting or decreasing local estradiol exposure.

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“…4,5,[12][13][14] The effect of tibolone is less investigated. 10,15,16 In 2012, the International Agency for…”

mentioning

confidence: 99%

Postmenopausal hormone therapy and the risk of breast cancer in Norway

Román

Sakshaug

Graff-Iversen

et al. 2015

Intl Journal of Cancer

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There is convincing evidence that combined estrogen-progestin therapy (EPT) increases the risk of breast cancer. However, the effect of different formulations, preparations and routes of administration is largely unknown. Estrogen only-therapy (ET) is, in general, not associated or weakly associated with breast cancer risk. We investigated the effect of hormone therapy (HT) with ET, EPT, and tibolone on risk of invasive breast cancer. Information on HT use was obtained from the Norwegian Prescription Database, and breast cancer incidence from the Cancer Registry of Norway. Poisson regression was used to estimate the incidence rate ratios (RR). We analyzed data from 686,614 Norwegian women, aged 45-79 years in January 2004, followed until December 2008, of whom 178,383 (26%) were prescribed HT. During the average 4.8 years of follow-up, 7,910 invasive breast cancers were registered. Compared with nonusers, current users of estradiol-norethisterone acetate (NETA)(EPT) had a RR of 2.74 (95% CI: 2.55-2.95). Users of the high dose estradiol-NETA formulation Kliogest V R had a RR of 3.26 (95% CI: 2.84-3.73), while users of the low dose Activelle V R had a RR of 2.76 (95% CI: 2.51-3.04). Current users of tibolone had a RR of 1.91 (95% CI: 1.61-2.28). Current users of ET with oral or transdermal estradiol had a RR of 1.40 (95% CI: 1.16-1.68), and 1.40 (95% CI: 1.00-1.95), respectively. The increased incidence rates approximates one extra invasive breast cancer case diagnosed for every 259 women using estradiol-NETA for one year, and one extra case for every 475 women using tibolone. In conclusion, use of estradiol-NETA and tibolone preparations is associated with an increased breast cancer risk.

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Short and long term effects of tibolone in postmenopausal women

Cited by 36 publications

References 68 publications

Guidelines for the Prevention of Stroke in Women

Guidelines for the Prevention of Stroke in Women

The impact of testosterone, tibolone and black cohosh on purified mammary and placental 17β-hydroxysteroid dehydrogenase type 1

Postmenopausal hormone therapy and the risk of breast cancer in Norway

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