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estradiol (Julina / estradiol, Bayer)

✓ Approved

Bayer AG · ESR1 · Small Molecule

What is estradiol?

estradiol is a small molecule developed by Bayer AG. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesJulina, estradiol, Bayer
CompanyBayer AG
Drug ClassSmall Molecule
Molecular TargetESR1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Bayer AG

Mechanism of Action

Molecular Targets

estradiol acts on 1 molecular target:

ESR1estrogen receptor 1 (ER, ESR)
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Therapeutic Indications

estradiol is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Surgical and medical proceduresHormone replacement therapy✓ Approved

Related Research Articles

PubMedArchives of sexual behavior2026-10-16

"There's No Magic Pill to Help Me, Right?": Sex After Early Midlife Bilateral Salpingo-Oophorectomy.

Amarakoon Anuki A, Galley Jana J, Perović Mateja M, Karkaby Laurice L et al.

Women with risk-reducing bilateral salpingo-oophorectomy (RRBSO) report poorer sexual health than women of a similar age with intact ovaries. Since women with RRBSO lose the ability to make endogenous 17-β-estradiol (E2), open questions include whether: (1) poorer sexual function is associated with E2 loss and (2) exogenous estradiol therapy (ETBSO) is related to amelioration of objective decrements and subjective experiences. We combined online questionnaires with qualitative interviews to explore the sexual function of women with pathogenic variants in the BRCA1/2 genes and RRBSO not taking ETBSO (RRBSO) and those taking ETBSO (RRBSO + ETBSO). We compared their quantitative responses to those of age-matched women with intact ovaries (AMC) and women in spontaneous menopause (SM). RRBSO had lower total sexual function scores than AMC and more sexually related distress than AMC than SM. In terms of lived experience with RRBSO + /-ETBSO, qualitative interviews mirrored the quantitative data with reports of pain, loss of sexual desire, and dryness, in addition to concerns about identity, relational challenges, and lacking crucial information regarding sexual response after RRBSO. The combination of the objective and subjective reports details worse sexual function and experience of younger women with RRBSO regardless of ETBSO. Since ETBSO does not appear to ameliorate all aspects of sexual function and distress for many women with RRBSO, it is critical to consider other interventions including fully informed consent prior to RRBSO.

PMID 42881326
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PubMedInternational journal of molecular sciences2026-10-16

Eating Behavior in Menopausal Women: From Molecular to Clinical Aspects-What Changes?

La Vignera Sandro S, Calogero Aldo E AE, Cannarella Rossella R, Crafa Andrea A et al.

The menopausal transition represents a critical period in women's lives characterized by profound hormonal, metabolic, and behavioral changes. Estrogen deficiency during menopause triggers complex alterations in eating behavior through multiple molecular mechanisms involving hypothalamic neuropeptide systems, neurotransmitter pathways, and peripheral hormonal signals. This narrative review examines the molecular basis of eating behavior changes in menopausal women, integrating evidence from basic science and clinical research. At the molecular level, declining estradiol disrupts the hypothalamic regulation of appetite through estrogen receptors ERα and ERβ, leading to dysregulation of key neuropeptides including neuropeptide Y (NPY), agouti-related peptide (AgRP), and proopiomelanocortin (POMC). Peripheral signals such as leptin, ghrelin, and insulin show altered secretion and sensitivity patterns. Clinically, postmenopausal women experience increased appetite, heightened food reward sensitivity, carbohydrate cravings, and elevated risk of binge eating behaviors. These changes contribute to weight gain averaging 2-3 kg during the menopausal transition, with preferential visceral fat accumulation increasing metabolic syndrome risk. Body composition shifts include 44% increases in visceral adiposity and concurrent sarcopenia. Emerging evidence highlights the role of gut microbiota alterations in mediating metabolic dysfunction. Therapeutic strategies including hormone replacement therapy, targeted nutritional interventions, and lifestyle modifications show promise in mitigating these changes. Understanding the molecular-to-clinical continuum of eating behavior changes in menopause is essential for developing evidence-based preventive and therapeutic approaches to improve metabolic health and quality of life in postmenopausal women.

PMID 42883785
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PubMedCells2026-10-16

Heat-Inactivated Lactiplantibacillus plantarum (RSB11) as a Multifunctional Postbiotic: Anti-Inflammatory Effects Compared with Live RSB11 Across Multiple Human Cell Models.

Nicola Teodora T, Madhvacharyula Tanmaya T, Ashok Ajay A, Mandot Aryan A et al.

The clinical potential of probiotics is increasingly recognized; however, dependence on microbial viability, formulation and storage constraints, and safety considerations in vulnerable populations can limit their broader application. Postbiotics offer an alternative by providing inanimate microbial preparations with retained biological activity, yet whether heat inactivation preserves the functional effects of probiotic-derived candidates remains an important question. Here, we compare Lactiplantibacillus plantarum RSB11 in its live (RSB11 life) and heat-inactivated (RSB11-HI) forms across human cell models representing the gut, lung, ovary, bone, kidney, and liver. Following inflammatory challenge with lipopolysaccharide or Escherichia coli, we assessed MMP-9 expression and the pro-inflammatory cytokines TNF-α, IL-6, and IL-1β. Both RSB11 life and RSB11-HI broadly suppressed inflammatory responses, with RSB11-HI maintaining effects comparable to the live preparation across the MMP-9 and cytokine endpoints, where the two forms were tested side by side, and demonstrating greater suppression in selected experimental contexts. Additionally, RSB11-HI increased β-glucuronidase and estradiol levels relative to untreated controls in a gut-ovarian conditioned-medium model, suggesting effects extending beyond inflammatory modulation; a live comparator was not included in the β-glucuronidase measurements, so this effect is not established as specific to the inactivated form. Collectively, these findings demonstrate that heat inactivation preserves key biological functions of RSB11 and support RSB11-HI as a multifunctional candidate postbiotic with potential for expanded formulation and application.

PMID 42882434
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PubMedInternational journal of molecular sciences2026-10-16

The Role of Amh in Gonadal Development and Its Response to Exogenous Hormones in Blotched Snakehead (Channa maculata).

Qin Junqi J, Deng Yueying Y, Lu Yuntao Y, Zhang Yang Y et al.

Anti-Müllerian hormone (Amh) is a key regulator of sex determination and differentiation in fish. In this study, we identified and characterized a single-copy Amh ortholog, designated CmAmh, in blotched snakehead (Channa maculata), an economically important species in China. The cDNA spans 2340 bp and encodes a 545-amino-acid protein with conserved AMH-N and TGF-β domains. CmAmh exhibited pronounced male-biased gonadal expression, with transcript levels in testes markedly exceeding those in ovaries across all developmental stages (45~365 days post-hatching (dph)). Cellular localization revealed CmAmh transcripts in the Sertoli cells and spermatogonia of the testis and, more weakly, in the oogonia and primary oocytes of the ovary, suggesting a primary role in spermatogenesis and a potential modulatory function in early oogenesis. A strong inverse correlation between promoter CpG methylation and transcriptional activity, hypermethylation in ovaries (82.5~89.7%) versus hypomethylation (15.8~19.1%) in testes, indicated epigenetic regulation, which functionally integrates with hormonal signaling: 17β-estradiol (E2) suppressed, whereas methyltestosterone (MT) upregulated CmAmh expression. Long-term E2 exposure induced male-to-female secondary sex reversal (SSR) in 26.7% of XY individuals, whereas MT failed to reverse XX fish, indicating that CmAmh modulation alone is insufficient to override ovarian fate. Furthermore, CRISPR/Cas9-mediated mutagenesis achieved 40~45% editing efficiency, predominantly generating frameshift alleles, providing a platform for future functional studies. Collectively, these findings position CmAmh as a hormone-responsive nodal point within a broader sex-differentiation network. This work provides a theoretical foundation for sex-control strategies in C. maculata aquaculture, while future studies should focus on homozygous mutant generation to definitively establish its loss-of-function phenotype and regulatory networks.

PMID 42883834
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PubMedNutrients2026-10-16

Sex-Stratified Characterization of Behavioral, Hippocampal, and Microglial Androgen Responses to Adolescent High-Fat Diet Consumption in Mice.

Wang Conghui C, Li Hong H, Yu Zhehao Z, Xie Bingjie B et al.

Background: Adolescence is a vulnerable developmental period during which dietary exposure and psychosocial stressors may have lasting effects on higher-order brain functions. Depression often emerges during adolescence, at which time a female preponderance in prevalence becomes apparent. Consumption of a high-fat diet (HFD) is common during adolescence and has been associated with adverse emotional and neurobiological outcomes; however, its consequences have not been systematically characterized in both sexes. Methods: Male and female mice were fed a HFD from postnatal days 28 to 56 (spanning most of adolescence), with chronic unpredictable mild stress (CUMS) used as a challenge to assess stress responsiveness. Results: Sex-stratified analyses revealed that HFD consumption induced anhedonia-like behavior in both sexes, whereas additional behavioral impairments were detected in females. Additionally, HFD consumption amplified the behavioral response to CUMS in females. HFD feeding altered the ventral hippocampal neurostructure and microglial status in both sexes; however, dendritic and spine deficits and microglial activation-like changes were detected across more ventral hippocampal subregions in females, together with increased synaptic engulfment in the vDG. HFD consumption increased circulating leptin and estradiol levels in both sexes, and higher free fatty acid levels were detected in nonstressed HFD-fed mice of both sexes. In females, HFD consumption increased circulating testosterone levels, which was accompanied by increased androgen receptor (AR) nuclear localization and TNF-α expression in hippocampal microglia. Serum from HFD-fed females significantly increased AR nuclear localization (p = 0.0008) and phagocytic activity (p = 0.0038) in primary female microglia. Enzalutamide abolished the serum-induced increase in AR nuclear localization (p < 0.0001), reduced the corresponding increase in phagocytic activity (p = 0.0335), and attenuated the associated induction of TNF-α at both the protein (p = 0.0057) and mRNA (p = 0.0003) levels. Conclusions: These findings characterize sex-stratified behavioral and hippocampal neurobiological consequences of adolescent HFD consumption and suggest a previously underrecognized association between androgen-responsive microglial signaling and the broader hippocampal alterations observed in females. Although the causal contribution of this signaling pathway to the in vivo phenotypes remains to be established, this work provides a framework for further investigating sex-related differences in the neurobiological consequences of adolescent HFD consumption and the potential contribution of endocrine-microglial signaling.

PMID 42884680
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PubMedCureus2026-10-15

The Impact of Assisted Reproduction Technology on Breast Cancer Risk for Women With Infertility: Current Insights and Future Perspectives.

Bimpa Kanelina K, Xydias Emmanouil M EM, Varvaras Dimitrios D, Koronarchis Dimitrios N DN et al.

Breast cancer is the most frequently diagnosed malignancy among women worldwide. Because assisted reproduction technology (ART) commonly involves controlled ovarian stimulation (COS) and temporary increases in circulating estradiol and progesterone, its possible effect on long-term breast cancer risk remains an important clinical question. This narrative review, supported by a structured literature search of MEDLINE/PubMed, Scopus, and Web of Science from January 2003 to March 2026, summarizes 31 primary observational studies with a cumulative reported sample exceeding 7.1 million participants, with follow-up extending beyond three decades in some cohorts. Most studies found no significant association between ART and breast cancer incidence. Signals of increased risk were reported in selected subgroups, including women undergoing multiple stimulation cycles, women starting treatment at younger or older ages, and some women with prolonged clomiphene citrate (CC) exposure. The review also considers evidence concerning letrozole, postpartum breast cancer risk, tumor subtype, and fertility preservation in women with breast cancer. Overall, the available evidence does not demonstrate a meaningful increase in breast cancer risk attributable to ART itself. However, substantial heterogeneity, the predominance of older treatment protocols, and the lack of long-term incidence data for contemporary letrozole-based treatment limit definitive conclusions. Prospective studies using current ART protocols and long-term, subtype-specific follow-up are needed.

PMID 42877633
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