Nomegestrol acetate is an anti-aromatase agent in human MCF-7aro breast cancer cells

Chétrite, G.; Pasqualini, Jörge R.

doi:10.1515/hmbci.2010.054

Cited by 3 publications

(1 citation statement)

References 52 publications

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“… 36 NOMAC on the other hand does not cause increased proliferation in normal or human breast cancer cells. 37 – 39 NOMAC/E2 was found to cause less breast cell proliferation when compared to E2 alone 36 and has some anti-proliferative effect on human breast cancer cells. 40 Intermittent compared to continuous use of NOMAC/E2 is also associated with less breast cell proliferation and estrogen α receptor expression.…”

Section: Safetymentioning

confidence: 95%

Nomegestrol acetate/17-beta estradiol: a review of efficacy, safety, and patient acceptability

Akintomide¹,

Panicker²

2015

OAJC

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Nomegestrol acetate (NOMAC) 2.5 mg with 17-beta estradiol (E2) 1.5 mg is a new combined oral contraceptive (COC) formulation and is the first monophasic E2 pill to be marketed, having been licensed for use in Europe in 2011. It is available to be taken daily in a regimen of 24 active pills followed by four placebo pills. NOMAC is a highly selective 19-nor progestogen derivative with specific binding to progesterone receptors, anti-estrogenic activity and no androgenic, mineralocorticoid nor glucocorticoid effects. E2 is an estrogen that is identical to endogenous estrogen. While it has been in use for only a short period of time, current evidence suggests that NOMAC/E2 is just as effective, safe, and acceptable as existing COC preparations. Two large Phase III trials conducted in the Americas and across Europe, Australia, and Asia showed lower cumulative pregnancy rates in the NOMAC/E2 groups compared to the drospirenone (DRSP) 3 mg in combination with ethinyl estradiol (EE) 30 µg (DRSP/EE) groups but this difference was not statistically significant. NOMAC/E2 exhibits a good safety profile and has less effects on cardiovascular risk, hemostatic, metabolic, and endocrine factors in comparison to COCs containing EE in combination with levonorgestrel (LNG) or DRSP. NOMAC/E2 has also been found to cause less breast cell proliferation when compared to E2 alone and has some anti-proliferative effect on human breast cancer cells. NOMAC/E2 is considered acceptable as its compliance, continuation rates, and bleeding patterns were similar to COCs containing DRSP/EE and LNG 150 µg combined with EE 30 µg or LNG 100 µg combined with EE 20 µg (LNG/EE). However, discontinuation was found to be slightly higher in the NOMAC/E2 groups in the two large Phase III trials comparing NOMAC/E2 use with DRSP/EE. As the scientific literature has limited information on NOMAC/E2, further experience with NOMAC/E2 is required.

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Section: Safetymentioning

confidence: 95%

Nomegestrol acetate/17-beta estradiol: a review of efficacy, safety, and patient acceptability

Akintomide¹,

Panicker²

2015

OAJC

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The pharmacology of nomegestrol acetate

Ruan

Seeger²,

Mueck³

2012

Maturitas

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The formation and transformation of hormones in maternal, placental and fetal compartments: biological implications

Pasqualini¹,

Chétrite

2016

Hormone Molecular Biology and Clinical Investigation

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The fetal endocrine system constitutes the earliest system developing in fetal life and operates during all the steps of gestation. Its regulation is in part dependent on the secretion of placental and/or maternal precursors emanating across the feto-maternal interface. Human fetal and placental compartments possess all the enzymatic systems necessary to produce steroid hormones. However, their activities are different and complementary: the fetus is very active in converting acetate into cholesterol, in transforming pregnanes to androstanes, various hydroxylases, sulfotransferases, while all these transformations are absent or very limited in the placenta. This compartment can transform cholesterol to C21-steroids, convert 5-ene to 4-ene steroids, and has a high capacity to aromatize C19 precursors and to hydrolyze sulfates. Steroid hormone receptors are present at an early stage of gestation and are functional for important physiological activities. The production rate of some steroids greatly increases with fetal evolution (e.g. estriol increases 500-1000 times in relation to non-pregnant women). Other hormones, such as glucocorticoids, in particular the stress hormone cortisol, adipokines (e.g. leptin, adiponectin), insulin-like growth factors, are also a key factor for regulating reproduction, metabolism, appetite and may be significant in programming the fetus and its growth. We can hypothesize that the fetal and placental factors controlling hormonal levels in the fetal compartment can be of capital importance in the normal development of extra-uterine life.

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Nomegestrol acetate is an anti-aromatase agent in human MCF-7aro breast cancer cells

Cited by 3 publications

References 52 publications

Nomegestrol acetate/17-beta estradiol: a review of efficacy, safety, and patient acceptability

Nomegestrol acetate/17-beta estradiol: a review of efficacy, safety, and patient acceptability

The pharmacology of nomegestrol acetate

The formation and transformation of hormones in maternal, placental and fetal compartments: biological implications

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