Drug Database
ES

estradiol (EstroGel)

✓ Approved

Ascend Therapeutics · ESR1 · Small Molecule

What is estradiol?

estradiol is a small molecule developed by Ascend Therapeutics. It is approved for therapeutic indications via topical or transdermal.

Drug Profile

Brand NamesEstroGel
CompanyAscend Therapeutics
Drug ClassSmall Molecule
Molecular TargetESR1
RouteTopical, Transdermal
StatusApproved
Sources: ClinicalTrials.gov, Ascend Therapeutics

Mechanism of Action

Molecular Targets

estradiol acts on 1 molecular target:

ESR1estrogen receptor 1 (ER, ESR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

estradiol is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Reproductive system and breast disordersAtrophic vulvovaginitis✓ Approved
Surgical and medical proceduresHormone replacement therapy✓ Approved

Related Research Articles

PubMedFood research international (Ottawa, Ont.)2026-08-24

Evaluating the potential of foodborne chemicals to modulate intestinal barrier function: a combined in vitro/in silico toolbox to study the effects on tight junction protein claudin-4.

Bergen Janice J, Fellinger Christian C, Weinstabl Magdalena M, Jobst Maximilian M et al.

Intestinal barrier integrity is of paramount importance for our health. Several food constituents and contaminants have been described for positive or detrimental effects, however, a correlation between gut associated disorders and xenobiotics exposures remains challenging and modeling options limited. This study presents a NAMs-based hybrid in vitro/in silico workflow to investigate, and eventually prioritize, foodborne xenobiotics for their effect on gut barrier homeostasis. Model compounds comprised endocrine-active chemicals, such as plastic components (bisphenol A, bisphenol F), phytoestrogens (chrysin, daidzein, genistein), mycotoxins (alternariol, zearalenone), and natural/synthetic steroids (17-β-estradiol, cholesterol, levonorgestrel). Plasticizer diisodecyl phthalate was included as foodborne, non-endocrine active substance. The Caco-2/HT29-MTX-E12 intestinal epithelial co-culture was used to design a workflow capable of grasping discrete alterations in tight junction organization. The protein claudin-4 was taken as reference to study the structural organization along cell-cell contacts. Complementarily, docking and molecular dynamics simulations were applied to explore ligand-claudin-4 interactions, providing a pipeline which is potentially suitable to screen larger compounds libraries. Finally, proof-of-principle experiments including repeated exposures to reference compound 17-β-estradiol and plasticizer diisodecyl phthalate, supported the plausibility of a functional impairment of claudin-4. Both compounds significantly increased epithelial permeability without altering cell viability, indicating selective modulation of mechanical barrier properties. Together, this work outlines a mechanistic toolbox for the study of the potential of orally derived xenobiotics in modulating intestinal homeostasis.

PMID 42637315
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PubMedAnimal reproduction science2026-08-24

miR-130a-5p regulates steroid hormone synthesis in porcine ovarian granulosa cells by targeting APOE and modulating cholesterol metabolism.

Chen Xiaochen X, Zhou Mingshuo M, Hao Honglei H, Chang Minwen M et al.

The function of ovarian granulosa cells is central to follicular development and hormone production. To identify miRNAs associated with estrous status, we performed miRNA sequencing on ovaries from gilts that displayed estrus (ES) or remained non‑estrus (NES). miR‑130a‑5p was significantly upregulated in NES ovarian follicular tissues. In primary porcine granulosa cells, miR-130a-5p overexpression reduced estradiol(E2) secretion and decreased the abundance of key steroidogenic proteins, whereas miR-130a-5p inhibition increased E2 and progesterone(P4) secretion. miR-130a-5p also altered lipid droplet accumulation and the abundance of cholesterol metabolism-related proteins, including HMGCR and LDLR. Integrative target prediction combined with transcriptomic filtering identified apolipoprotein E (APOE) as a candidate target. A dual‑luciferase reporter assay confirmed direct binding of miR‑130a‑5p to the APOE 3'UTR. Functionally, APOE overexpression enhanced E₂ and P₄ secretion and increased lipid accumulation and HMGCR/LDLR expression, whereas APOE knockdown exerted opposite effects. Moreover, APOE overexpression attenuated the inhibitory effects of miR-130a-5p on steroid hormone production and steroidogenesis-related gene expression. Together, these findings identify a miR-130a-5p/APOE axis that links cholesterol metabolism-related processes to steroid hormone synthesis in porcine granulosa cells and provides a candidate pathway for further investigation of endocrine regulation in gilts.

PMID 42636602
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PubMedClimacteric : the journal of the International Menopause Society2026-08-24

Perimenopause and metabolic vulnerability: hormones, body composition and lifestyle changes.

Lobato Vanessa Alves VA, Minari Tatiana Palotta TP, Pisani Luciana Pellegrini LP

Perimenopause is a transitional phase characterized by substantial hormonal fluctuations, particularly declining estradiol levels, accompanied by age-related metabolic changes. Increasing evidence suggests that this period constitutes a critical window of metabolic vulnerability, marked by adverse alterations in body composition, energy metabolism and cardiometabolic health. Notably, these changes may develop even without significant increases in body weight, potentially delaying their recognition in clinical settings. A narrative review was conducted using the PubMed/MEDLINE, Scopus, Web of Science and SciELO databases. Studies involving perimenopausal women, plus relevant animal models, were included. Search terms covered estrogen deficiency, body composition, metabolism, insulin resistance, inflammation, physical activity and nutrition. Fifty-six studies published between 2000 and 2026 were analyzed. Evidence shows that perimenopause is characterized by increased visceral fat, loss of lean mass, reduced fat oxidation and impaired metabolic flexibility, even without major weight changes. Declining estrogen drives adipose redistribution, muscle dysfunction, hepatic insulin resistance and chronic low-grade inflammation. These changes heighten risk for metabolic syndrome, type 2 diabetes and cardiovascular events. Lifestyle interventions, particularly resistance training and Mediterranean diet adherence, demonstrate strong potential to preserve muscle, improve insulin sensitivity and reduce inflammation. In conclusion, perimenopause should be recognized as a pivotal stage for early detection and prevention of metabolic dysfunction. Lifestyle-based interventions during this phase may reduce long-term cardiometabolic risk and improve women's health.

PMID 42634879
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PubMedPediatric allergy and immunology : official publication of the European Society of Pediatric Allergy and Immunology2026-08-24

Salivary OMICS factors associated with atopic dermatitis in early infancy.

Alomeir Nora N, Chinchilli Ellen E, Terio Chloe C, Zhang Lanxin L et al.

Atopic dermatitis (AD) often develops in early childhood and may persist into adulthood. Noninvasive measures to identify infants at risk for AD are limited. We investigated whether oral biomarkers and oral microbiota are associated with AD onset within the first 2 years of life. In this prospective cohort study, we followed 119 infants residing in Upstate New York from birth to 24 months (2018-2023). AD diagnoses were obtained from electronic health records. Saliva samples were collected at seven time points (1, 2, 4, 6, 12, 18, and 24 months) and analyzed for 5 hormones and 23 cytokines using multiplex immunoassays. Salivary microbiome profiles were characterized via metagenomic sequencing. Nearly half (48%) of infants developed AD by age 2, with most cases manifesting by 12 months (42%) and peak incidence occurring between months 2-4. Infants who developed AD by 1 year demonstrated significantly elevated estradiol (p = .007) and progesterone (p = .046) at 1 month, and a significantly lower salivary cortisol level (p = .019) at 6 months. Additionally, these infants exhibited higher sIL-1ra (p = .024) and IL-9 (p = .034) in saliva at 4 months and lower IL-1α (p = .038) at 6 months. Salivary microbiome beta diversity differed significantly at 2 months between infants with and without AD by 1 year (p = .038), with lower differential abundances of Bifidobacterium breve and Veillonella atypica in early infancy prior to AD onset. Early-life salivary biomarkers, including hormonal, cytokine, and microbiome signatures, may serve as noninvasive indicators of infants at risk for early AD onset.

PMID 42634387
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PubMedReproduction in domestic animals = Zuchthygiene2026-08-24

A Comparison of Long-Acting Progesterone and Intravaginal Device Priming Protocols for Inducing Ovarian Activity in Dromedary Camels.

Moussa Mahmoud M, Ahmed Salahaddin S, Elbaz Mohamed M, Pasha Kamaal K

The objectives of this study were to evaluate the efficacy of long-acting progesterone (P4) versus a P4-releasing intravaginal device (PRID) in restoring ovarian activity in dromedary camels with inactive ovaries, and to determine whether P4 priming is necessary before eCG administration. Seventy-five camels were equally assigned to three groups: a control group receiving only 1500 IU eCG; a PRID group treated with a 12-day PRIDΔ followed by eCG; and a P4 long-acting (P4 LA) group administered 1500 mg P4 LA followed by eCG on Day 12. Serum P4 and estradiol (E2) levels were measured on Days 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, and 20, and reproductive outcomes were recorded. Results showed that the P4 LA group exhibited a rapid increase followed by a sharp decline in P4 levels, whereas the PRID group maintained more stable P4 levels, with a gradual decrease by Day 12. Moreover, from Day 16 onward, primed groups had significantly higher E2 levels than controls (p < 0.05). The response rate was 100% in the primed groups versus 60% in controls (p < 0.05), and the interval from eCG injection to ovulatory follicle development was shorter in primed groups (p < 0.05). The 18-day conception rate was highest in the PRID group (100%), followed by P4 LA (84%) and controls (53.3%). However, the pregnancy rate at Day 60 did not differ between PRID (84%) and P4 LA (80%) groups, both of which were significantly higher than controls (13.3%) (p < 0.05). In conclusion, P4 priming is essential before eCG administration, and LA P4 offers practical advantages for field veterinarians.

PMID 42635096
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PubMedJournal of reproduction & infertility2026-08-23

Successful Intrauterine Insemination Following Estradiol Pretreatment in a Patient with Primary Ovarian Insufficiency: A Case Report.

Huynh Trang Nguyen Khanh TNK, Huynh Minh Phuc Khanh MPK, Ly Loc Thai LT

Premature ovarian insufficiency (POI) is a clinical condition characterized by impaired ovarian function to secrete gonadal hormones, leading to hypoestrogenism and amenorrhea before the age of 40. Oocyte depletion in POI significantly reduces the chance of spontaneous conception, making infertility a key concern. Various in vitro fertilization (IVF) stimulation protocols, including estrogen pretreatment, have been investigated to facilitate conception with autologous oocytes in patients with POI. The principle of estrogen pretreatment involves administering exogenous estrogen to suppress elevated pituitary gonadotropins (FSH and LH), thereby restoring normal follicular development. This article presents a case of a 32-year-old patient with POI, characterized by severely diminished ovarian reserve, as evidenced by an AMH level of 0.03 ng/ml and an antral follicle count (AFC) of 1. Our patient had been attempting to conceive for 14 months and reported shortened menstrual cycles. Hysterosalpingography revealed bilaterally patent fallopian tubes, and the patient's partner demonstrated normozoospermia. The patient was initially scheduled for IVF with controlled ovarian stimulation and estrogen pretreatment. However, a spontaneously matured follicle was detected during the course of estrogen therapy. Consequently, the patient was advised to undergo intrauterine insemination (IUI) following ovulation triggering with human chorionic gonadotropin (hCG). The procedure resulted in a clinical pregnancy and culminated in a term live birth. In POI patients using for estrogen pretreatment autologous oocytes, may enhance ovarian responsiveness. If a mature follicle emerges during estrogen pretreatment, ovulation induction with IUI offers a viable path to natural conception.

PMID 42633041
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