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)
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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

PubMedAnalytical chemistry2026-10-20

Subpicogram-Level Quantification of Trace Biomarkers Using an Automated High-Sensitivity Chemiluminescence Immunoassay Technology Based on a Novel Substrate Enhancement Strategy.

Li Kexin K, Duan Zhuonan Z, Li Ke K, Wang Yanzhong Y et al.

Trace biomarkers showed great potential for improving the diagnosis and monitoring of various diseases. However, the sensitivity of the current high-throughput detection platforms is limited, posing a significant challenge for the reliable measurement and clinical application of trace biomarkers. We developed an automated high-sensitivity chemiluminescence immunoassay (CLIA) technology with subpicogram-level sensitivity based on the modification of the substrate molecular structure and the synergy of surfactant and fluorescein. Using this technology, we constructed assay kits for five trace biomarkers: leukemia inhibitory factor (LIF), high-sensitivity cardiac troponin I (hs-cTnI) and T (hs-cTnT), phosphorylated tau-217 (p-tau217), and estradiol (E2). The analytical and clinical performance was evaluated by examining the precision, linearity, limits of detection, and methodological comparison. The high-sensitivity chemiluminescent substrate demonstrated approximately 7-fold higher sensitivity and 2.5-fold greater luminescence efficiency compared to those of the traditional substrate, with a linear range exceeding 160 million relative light units (RLUs). The five trace biomarker assays exhibited excellent analytical sensitivity, with the LoD values of 0.070 pg/mL (LIF), 0.18 pg/mL (hs-cTnI), 1.1 pg/mL (hs-cTnT), 0.007 pg/mL (p-tau217), and 0.113 pg/mL (E2 II). Compared with other high-sensitivity detection methods, the Passing-Bablok linear correlation coefficients (r) ranged from 0.9767 to 0.9974. The proportions of cTnI, cTnT, and E2 II concentrations above the LoD in healthy populations exceeded 98%. We established an automated high-sensitivity CLIA technology based on a novel substrate enhancement strategy, improving the analytical sensitivity to the subpicogram level. An automated high-throughput detection method of various trace biomarkers was realized that may have broad application in the clinic.

PMID 42899535
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PubMedFrontiers in endocrinology2026-10-20

Integrated pituitary adaptations to the low estrogen state.

Miles Tiffany K TK, Odle Angela K AK, Herdman Ashley K AK, Clark Lillian G LG et al.

Estrogen's broad trophic effects on anterior pituitary function are not fully understood. The compound 4-vinyl cyclohexene diepoxide (VCD) induces early ovarian failure and reduced E2 production, which may differentially affect anterior pituitary cells. We recently identified transcriptomic changes in pituitary gonadotropes at the single-cell level in females treated with VCD for 20 days, which were acyclic, with low serum estradiol (E2) levels and 8-12-fold increases in gonadotropins 138 days later. We tested vehicle-control and VCD-treated female mice in metabolic cages and assayed serum hormone levels by EIA, and pituitary cell transcripts by qRT-PCR and single-cell RNA-seq. VCD-treated mice showed normal metabolic health. Compared with controls, VCD-treated females exhibited a 5-fold elevation in serum pituitary thyroid-stimulating hormone (TSH) levels and near-normal thyroid hormone levels. Pituitary Tshb mRNA levels were reduced, and pituitary Gh, Prl, and Pomc mRNA levels were unchanged. Serum growth hormone (GH) levels were higher in VCD-treated mice than in controls 62 days after the start of treatment (perimenopause) and then reduced to control levels after 118-138 days. Ingenuity Pathway Analyses (IPA) of upregulated differentially expressed gene (DEG) transcripts predicted activation of G protein-mediated signaling pathways in one scRNA-seq somatotrope subcluster and in the thyrotrope and lactotrope clusters. In contrast, downregulated DEGs in corticotropes and the remaining two somatotrope clusters predicted downregulation of critical signaling pathways. The unchanged pituitary Gh, Prl, and Pomc mRNA levels correlated with unchanged serum levels. The interim rise in serum GH 62 days after treatment agrees with reports of perimenopausal responses due to estrogen spikes. Reduced pituitary Tshb correlates with the recently reported reduced expression in gonadotropes. IPA analysis of upregulated DEGs in thyrotrope clusters predicted the activation of canonical signaling pathways that support elevated serum TSH levels. The near-normal thyroid hormone levels suggest subclinical hypothyroidism in menopausal women. Downregulated DEGs in corticotropes and in two somatotrope subclusters predicted compromised stress and metabolic responses. Finally, reduced multihormone gene expression suggested compromised plasticity in a low-estrogen environment. These different responses to a sustained low-estrogen state, such as that seen in menopause, reflect the diversity of estrogen's trophic actions.

PMID 42898303
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PubMedEuropean journal of endocrinology2026-10-19

BMI as a partitioning factor for estradiol and estrone reference intervals in middle-aged men and postmenopausal women.

Kruijt M M, de Mutsert R R, van Hylckama Vlieg A A, Rosendaal F R FR et al.

Estrogens play a large role in female and male physiology and are routinely determined in the clinical setting. For interpretation, distinct reference intervals are applied for men, pre---, and postmenopausal women. Adipose tissue is a potent producer of estrogens and influences the circulating estrogen concentrations, although its impact on estrogen reference intervals is currently unknown. We determined estradiol and estrone concentrations in 6,671 middle-aged participants of a large cohort oversampled for persons with BMI >27 kg/m2. We investigated partitioning based on sex, age, menopausal status, and BMI by assessing the proportion of subgroups outside each limit of a shared 95% reference interval (ideally 2.5%) and calculating reference intervals for justified subgroups according to CLSI EP28-A3c. As expected, the strongest partitioning factor was sex, followed by menopausal status for women. When using a shared reference interval for all BMI categories, 4.9% and 5.2% of values in men with obesity and 11.4% and 7.7% of values in postmenopausal women with obesity fell above the reference interval for estradiol and estrone, respectively. Within postmenopausal women differences in the upper reference limit were found, being 138, 157, and 210 pmol/L for estradiol and 32, 41, and 74 pmol/L for estrone for normal weight, overweight, and obesity, respectively. Laboratory professionals and clinicians should be aware that BMI affects estrogen concentrations to such extent that it may influence clinical interpretation. Ideally their reference intervals should be stratified by BMI category to reflect the increased estrogen concentrations associated with higher BMI.

PMID 42895437
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PubMedEcotoxicology and environmental safety2026-10-19

Tebuconazole-induced ferroptosis impairs human trophoblast function via GPX4: A multi-omics study on unexplained recurrent pregnancy loss.

Wang Shaowei S, Che Huiyi H, Ren Xiya X, Lin Zi Z et al.

Tebuconazole (TEB) is a widely used triazole fungicide with suspected endocrine-disrupting and reproductive toxicity. However, its effects on human placental trophoblasts and its association with unexplained recurrent pregnancy loss (RPL) remain poorly defined. Chorionic villi from 27 women with unexplained RPL and 25 women with normal pregnancies were analyzed by HPLC-MS/MS, and TEB effects were examined in BeWo and HTR-8/SVneo trophoblasts. Villus TEB residues were 1.82-fold higher in the RPL group (mean 0.0356 versus 0.0196 ng/g; P < 0.001), whereas TEB-OH did not differ significantly. In HTR-8/SVneo cells, 48-h TEB exposure reduced estradiol secretion at 20-80 µM and impaired migration at 40-80 µM without a significant loss of CCK-8 viability, and increased intracellular labile Fe2 +. Transcriptome profiling at 80 µM identified 1680 differentially expressed genes (797 up-regulated, 883 down-regulated), and the downregulation of GPX4, TFRC, and SLC40A1 was confirmed by RT-qPCR and Western blotting. Network toxicology identified 72 core targets shared with RPL and fetal growth restriction, and docking predicted GPX4 as a candidate binding target of TEB (Ki= 44.74 µM). Consistent with a ferroptotic mechanism, ferrostatin-1 (2 µM) attenuated TEB-induced lipid peroxidation and Fe2+accumulation and partially restored GPX4, SLC40A1, and TFRC abundance, trophoblast migration, and estradiol secretion. These findings suggest that ferroptosis-related lipid peroxidation contributes to TEB-induced trophoblast dysfunction and links chorionic villus TEB residues to unexplained RPL. Because the effective in vitro concentrations exceed typical human exposure levels, the results provide mechanistic evidence of hazard and warrant further risk assessment.

PMID 42896376
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PubMedCureus2026-10-19

Efficacy and Safety of Vitex Extract on Menopausal Symptoms and Quality of Life in Postmenopausal Women: A Randomized Placebo-Controlled Trial.

Reddy Prasanna A PA, Aluri Srilakshmi S, Ca Anzar A, Mv Joseph J et al.

Postmenopausal women often experience vasomotor and hormonal symptoms due to a decline in estradiol levels, which affects their quality of life (QOL). Botanical extracts like Vitexextract, known for their estrogen- and progesterone-like actions, may offer a safe and effective approach for alleviating postmenopausal symptoms and improving overall quality of life. The current study was a prospective, randomized, double-blind, placebo-controlled, monocenter clinical study to evaluate the safety and efficacy of Vitex extract in postmenopausal women aged 40-65 years. Sixty eligible participants were randomized to either the Vitex extract or placebo group equally and instructed to take one capsule daily after breakfast for 60 days. The primary endpoints included changes in the Blatt-Kupperman Index (BKI), Menopause-Specific Quality of Life Questionnaire (MENQOL), Menopause Rating Scale (MRS), and overall QOL scores. The study was prospectively registered with the Clinical Trials Registry of India (CTRI/2025/03/082025). After 60 days, Vitex extract supplementation led to clinically and statistically significant improvements compared with placebo in all primary outcomes. Notable reductions were observed in BKI, MENQOL, and MRS scores, reflecting better control of vasomotor, psychosocial, physical, and sexual symptoms. Improvements were also seen in the reduction in joint and muscle pain, stress levels, and serum cortisol. Hormonal regulation of luteinizing hormone (LH), follicle-stimulating hormone (FSH), estradiol, and thyroid function, along with reduced rheumatoid factor, indicated anti-inflammatory and endocrine benefits. No adverse effects or lab abnormalities were reported. In this single-center study, Vitex extract appeared effective and was well tolerated, suggesting its potential as a safe, non-hormonal option for relieving menopausal symptoms and improving quality of life in postmenopausal women. However, these findings should be confirmed in larger, multi-center trials before broader clinical recommendations can be made.

PMID 42894752
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PubMediScience2026-10-19

LncRNA Arsa-DT is required for spermatogenesis and male fertility by regulating G2/M progression.

Choi Haena H, Kim Ji-Eun JE, Kim Ju-Yeon JY, Lee Ho H et al.

Male infertility is a major reproductive health burden worldwide, yet its molecular etiology remains largely unknown. The testis expresses numerous long non-coding RNAs (lncRNAs), although their involvement in the pathophysiology of male infertility remains unexplored. Here, we identified Arsa-DT, a testis-predominant divergent lncRNA of Arsa, and demonstrated its essential role in maintaining male fertility. Loss of Arsa-DT leads to subfertility, characterized by reduced sperm production, increased sperm abnormalities, and decreased serum testosterone levels. Notably, Arsa-DT deficiency alters the testosterone-to-estradiol ratio through upregulation of aromatase expression. Specifically expressed in the nuclei of spermatogonia and spermatocytes, Arsa-DT regulates spermatogenesis in the seminiferous tubules. Mechanistically, Arsa-DT regulates G2/M phase progression and chromosome segregation in male germ cells. Collectively, our findings identify Arsa-DT, a testis-predominant lncRNA, as a regulator of spermatogenesis by controlling G2/M phase progression of male germ cells. This study provides mechanistic insights into the pathogenesis of male infertility.

PMID 42894537
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