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ethinyl estradiol + norethindrone (WC3026 / Generess Fe)

✓ Approved

Actavis · ESR1 · 小分子

什么是 ethinyl estradiol + norethindrone?

ethinyl estradiol + norethindrone 是一种小分子,由Actavis研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名WC3026, Generess Fe
公司Actavis
药物类别小分子
分子靶点ESR1, PGR
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

ethinyl estradiol + norethindrone 作用于 2 个分子靶点:

ESR1estrogen receptor 1 (ER, ESR)
PGRprogesterone receptor (NR3C3, PR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

相关研究文献

PubMedExperimental gerontology2026-08-09

Sex-specific associations of serum estradiol and the testosterone-to-estradiol ratio with handgrip strength and appendicular lean soft tissue in US adults aged 40-59 years.

Prokopidis Konstantinos K, Boccardi Virginia V, Cacciatore Stefano S, McLean Joseph J et al.

Sex steroids play a key role in skeletal muscle regulation, yet sex-specific links between estradiol, testosterone-estrogen balance, and muscle health in midlife remain sparse. In this study we evaluated associations between circulating estradiol and testosterone-to-estradiol (T/E) ratio with handgrip strength (HGS) and appendicular lean soft tissue index (ALSTI) in men and women aged 40-59 years. We analyzed data from 1350 adults [48.8 (5.7) years, 693 women] participating in NHANES 2013-2014. HGS was assessed using a handheld dynamometer, and ALSTI by dual-energy X-ray absorptiometry. Sex-specific linear and logistic regression models examined associations of estradiol and T/E with continuous and categorical muscle outcomes. Complementary analyses examined log10-transformed estradiol, T/E ratio, and total testosterone, with SHBG included in sensitivity analyses. In unadjusted analyses, higher estradiol was associated with greater ALSTI in men (b = 0.43, 95% CI 0.25 to 0.61) and higher HGS in women (b = 1.56, 95% CI 0.92 to 2.20), while higher T/E was associated with lower HGS and ALSTI in men (b = -1.87, 95% CI -3.19 to -0.55, and b = -0.74, 95% CI -1.02 to -0.46, respectively) and lower HGS in women (b = -1.84, 95% CI -2.69 to -0.99). However, these associations were largely attenuated after multivariable adjustment. In logistic models, women with lower estradiol concentrations had significantly higher odds of low HGS compared with those with higher estradiol in Model 2 (OR = 2.44, 95% CI 1.01 to 5.88), while the association with moderate estradiol levels did not reach statistical significance (OR = 2.27, 95% CI 0.98 to 5.26). These associations were attenuated after additional adjustment for SHBG. No corresponding associations were observed in men. The T/E ratio was not independently associated with low HGS after adjustment in either sex. Circulating estradiol and T/E show sex-specific associations with muscle health. Lower estradiol was associated with higher odds of low HGS in women in the primary adjusted analysis, whereas most other hormone-muscle associations were attenuated after adjustment. These findings support further longitudinal studies to clarify sex-specific hormone-muscle trajectories across midlife.

PMID 42570737
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PubMedJournal of evidence-based integrative medicine2026-08-09

Long-Term Effects of Yoga Practice on Metabolic, Hormonal, and Anthropometric Parameters in Climacteric Women.

Cota E Souza Laura Alves LA, Reis Ilka Afonso IA, Lima Angélica Alves AA

Metabolic and hormonal disturbances are common during the climacteric period and contribute to an increased risk of chronic diseases. Yoga has emerged as a promising complementary approach to promote women's health during midlife; however, long-term evidence remains limited. This longitudinal, community-based controlled study evaluated the effects of regular yoga practice over 24 months on anthropometric, metabolic, and hormonal parameters in climacteric women. A total of 182 Brazilian women aged 40-65 were followed; participants who chose to engage in yoga formed the intervention group, while sedentary women served as controls. Data were collected at baseline and after 6, 12, and 24 months. After 24 months, the yoga group showed significant reductions in BMI (-2.24 kg/m2; p = 0.008) and body fat percentage (-4.29%; p = 0.008), as well as decreases in systolic (-11.4 mm Hg; p = 0.012) and diastolic blood pressure (-5.5 mm Hg; p = 0.044). Improvements were also observed in fasting glucose (-9.1 mg/dL; p = 0.024), QUICKI (+0.03; p = 0.046), HDL-c (+9.6 mg/dL; p = 0.012), and non-HDL-c (-23.4 mg/dL; p = 0.018). Estradiol levels increased by 24.4 pg/mL in the yoga group and were significantly higher than in controls at 24 months (+40.9 pg/mL; p < 0.001), suggesting an endocrine-modulating effect. These findings support yoga as a promising nonpharmacological strategy to promote metabolic and hormonal health during the climacteric phase.

PMID 42570869
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PubMedFood & nutrition research2026-08-09

SheVari4®, a proprietary root extract from Asparagus racemosus, ameliorates menopausal health: insights from a randomized, double-blind, placebo controlled clinical trial.

Chattopadhyay Raktim R, Karmakar Subhankar S, Chakraborty Tandra R TR, Bagchi Manashi M et al.

Menopause marks the natural end of reproductive phase of women caused by decline in levels of estrogen, progesterone and other reproductive hormones. Asparagus racemosus (Shatavari) is a medicinal herb particularly known to be effective in alleviating women's reproductive health. Shatavarin IV, a steroidal saponin and a primary bioactive component in this herb, acts as a phytoestrogen by modulating the ER-alpha/ER-beta signalling, the TrkB-BDNF axis, and the Hypothalamic-Pituitary-Gonadal (HPG) and Hypothalamic-Pituitary-Adrenal (HPA) axes. In this study, the efficacy of SheVari4® on alleviating the menopause-specific endocrine dysfunction and subsequent impaired quality of life (QOL) was assessed through a randomized double-blind placebo-controlled parallel arm trial conducted on 60 pre-, peri-, and post-menopausal women. Sixty women (age 50.0 ± 7.4 years) randomized in two equal groups were administered with 100 mg SheVari4® or placebo capsules once daily for 8 weeks. Assessment of Menopause-Specific Quality of Life (MENQOL) along with domain scores across vasomotor, psychosocial, physical, and sexual function constituted primary endpoint analysis; changes in serum estradiol E2, Follicle Stimulating Hormone (FSH), progesterone, cortisol, Anti Mullerian Hormone (AMH), Sex Hormone-Binding Globulin (SHBG) and free testosterone were assessed as secondary endpoint analysis. Safety of the formulation was evaluated in terms of body mass index, blood biochemistry and liver function test. SheVari4 induced a 42.8% reduction in MENQOL versus placebo. Significant improvements in functioning (vs. placebo) were observed, respectively, across vasomotor (53.1% vs. 14.5%), psychosocial (53.6% vs. 9.9%), physical (39.2% vs. 6.5%) and sexual (29.4% vs. 10.7%) domains. The formulation also increased E2 (+36.44% vs. -2.08%) and progesterone (+0.30% vs. -2.88%) coupled with marked reduction in levels of FSH (-38.18% vs. +12.97%) and cortisol (-26.87% vs. +17.16%). Concomitantly, AMH, SHBG, and free testosterone were also favorably modulated. Blood biochemistry, liver function tests, and vital signs confirmed the broad-spectrum safety of SheVari4®. SheVari4® significantly improved menopause-specific QOL and endocrine parameters in peri- and post-menopausal women, with a well-established safety profile.

PMID 42571384
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PubMedFrontiers in endocrinology2026-08-08

Estetrol/drospirenone for combined oral contraception: a systematic review of efficacy, cycle control, and safety.

Sánchez-Prieto Manuel M, Coll Sandra S, Romero-Domínguez Marina M, Avella-Marcos Marta M et al.

To systematically evaluate the evidence on the contraceptive efficacy, cycle control, safety, and selected noncontraceptive effects of estetrol 15 mg/drospirenone 3 mg (E4/DRSP) and to assess certainty of evidence by outcome using the GRADE approach. A systematic review was conducted in accordance with PRISMA 2020. PubMed/MEDLINE, Scopus, and Google Scholar were searched for eligible studies published through February 2026. Clinical trials and comparative studies evaluating E4/DRSP in women of reproductive age were included. Outcomes were grouped into contraceptive efficacy, bleeding/cycle control, safety and tolerability, hemostatic and endocrine-metabolic effects, ovarian suppression, and noncontraceptive clinical outcomes. Risk of bias was assessed using design-specific tools, and certainty of evidence was graded by outcome. A total of 25 eligible publications/study reports were included, comprising phase 2 dose-finding studies, pivotal phase 3 contraceptive trials, pooled analyses, mechanistic comparator studies, adolescent data, and indication-specific studies. E4/DRSP demonstrated robust contraceptive efficacy, predictable bleeding patterns, and an acceptable tolerability profile. Across mechanistic studies, E4/DRSP showed less pronounced hemostatic and endocrine-metabolic effects than ethinyl estradiol-containing comparators. The most consistent biological differentiation of E4/DRSP was observed for APC resistance and thrombin-generation endpoints, which were less affected than with EE-containing comparators. The strongest noncontraceptive evidence was observed for dysmenorrhea, supported by a randomized, double-blind, placebo-controlled trial. Certainty of evidence was moderate for contraceptive efficacy, cycle control, common adverse events, and surrogate hemostatic/metabolic outcomes; high for dysmenorrhea versus placebo; low for endometriosis-related and menstrual symptom outcomes; and very low for clinical thromboembolic risk. E4/DRSP is an effective combined oral contraceptive with favorable cycle control and a consistent biologic profile suggesting lower hepatic/hemostatic impact than ethinyl estradiol-containing formulations. However, current evidence does not establish comparative thromboembolic safety, which requires dedicated postauthorization and real-world comparative studies.

PMID 42568434
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PubMedNeurochemical research2026-08-08

Δ9-Tetrahydrocannabinol Modulates Hippocampal Neurogenesis in Female Wistar Rats: Interaction with Estradiol.

Carvalhinho Duarte R DR, Marques Sandra I SI, Leal Sandra S, Fonseca Bruno M BM et al.

The endocannabinoid system (ECS) plays a key role in regulating neurogenesis and inflammatory processes in the brain. The increasing prevalence of Cannabis use among women highlights the importance of understanding sex-specific effects of cannabinoids, particularly in the context of hormonal interactions. This study aimed to investigate the effects of delta-9-tetrahydrocannabinol (THC) and estradiol benzoate (EB) on adult hippocampal neurogenesis (AHN) and inflammation in ovariectomized female Wistar rats. Sixteen rats were allocated to four experimental groups receiving THC, EB, both treatments, and vehicle. Immunohistochemical analyses were conducted to evaluate markers of proliferation (Ki-67), neurogenesis (doublecortin and PSA-NCAM), cannabinoid receptor expression (CB1), and inflammation (COX-2 and TNF-α) in the hippocampal formation. The administration of THC significantly increased Ki-67 immunoreactivity, suggesting enhanced cell proliferation. A trend toward increased doublecortin expression was observed, particularly in EB-treated animals. THC also modulated CB1 receptor expression, with significant increases in the dentate gyrus and hilus following combined THC and EB treatment. Furthermore, THC reduced inflammatory markers, with region-dependent decreases in COX-2 and TNF-α expression. These findings indicate that THC influences markers associated with hippocampal cell proliferation, neurogenesis, cannabinoid signaling and inflammation in female rats, and that some of these effects depend on estradiol status. The interaction between cannabinoids and gonadal hormones may represent an important mechanism underlying sex-specific neurobiological responses and suggests potential targets for therapeutic intervention in neuropsychiatric disorders.

PMID 42570151
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PubMedTheriogenology2026-08-08

Exploring the postpartum period in mares: hormonal dynamics and ovarian activity under physiological and pathological conditions.

Perina Francesca F, Lanci Aliai A, Fanelli Diana D, Maltinti Saverio S et al.

The aims of the study were to evaluate factors influencing the resumption of postpartum ovarian activity and to compare hormone concentrations among mares with physiological/pathological postpartum period and cyclic non-lactating mares. Follicular dynamics were monitored ultrasonographically in 38 postpartum mares from foaling or admission (Tpp/Ta) every other day until the emergence of a dominant follicle (Td), then daily until ovulation (To). Blood samples were collected at Tpp/Ta, Td, and To in postpartum mares and at Td and To in cyclic mares to determine serum estradiol, progesterone, leptin and cortisol concentrations. Ovulation occurred in 34/38 (90%) mares. The χ2 test showed that ovulation was significantly more frequent in mares with physiological postpartum (p = 0.005), in multiparous (p = 0.03) and in lactating mares (p = 0.00011). Age and foaling month were not associated with ovulation. In physiological postpartum mares, estradiol and progesterone concentrations decreased significantly over time (p = 0.002; p = 0.004 respectively), whereas leptin and cortisol remained unchanged. No significant temporal changes were observed for any hormone in mares with pathological postpartum or in cyclic mares. Hormone concentrations did not differ significantly among groups at any time point. Progesterone concentrations at Tpp/Ta were lower in primiparous mares (p = 0.048). Overall, parity, type of postpartum and lactation status influenced the likelihood of postpartum ovulation. Although hormone concentrations were largely comparable among groups, pathological postpartum mares exhibited delayed or absent ovulation, suggesting that postpartum disorders may affect the resumption of ovarian activity.

PMID 42567120
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