Drug Database
ES

estradiol (Vagifem)

✓ Approved

Novo Nordisk A/S · ESR1 · Small Molecule

What is estradiol?

estradiol is a small molecule developed by Novo Nordisk A/S. It is approved for therapeutic indications via intravaginal.

Drug Profile

Brand NamesVagifem
CompanyNovo Nordisk A/S
Drug ClassSmall Molecule
Molecular TargetESR1
RouteIntravaginal
StatusApproved

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
Reproductive system and breast disordersAtrophic vulvovaginitis✓ Approved

Related Research Articles

PubMedClinical case reports2026-08-30

Synchronous Vaginal and Liver Metastases in Rectosigmoid Cancer: Case Report and Literature Review.

Alyaarabi Tamader T, Al-Dhaheri Mahmood M, Abdul-Hafez Hamza A HA, Aleter Ammar A et al.

Vaginal metastasis from colorectal cancer is extremely rare. We report the case of a 58-year-old postmenopausal woman with rectosigmoid adenocarcinoma and synchronous liver and vaginal metastases who initially presented with gastrointestinal symptoms followed by vaginal bleeding. The diagnosis was established through colonoscopy, biopsy, CT, MRI, and FDG PET-CT. After 6 cycles of FOLFOX chemotherapy, the liver metastases regressed, while the primary tumor and vaginal lesions progressed. She subsequently underwent pelvic exenteration with ileal conduit formation and right hepatectomy, followed by pulmonary metastasectomy and stereotactic body radiotherapy for subsequent lung metastases. At 41 months of follow-up from diagnosis, the patient remains alive with disease and has demonstrated a favorable response to multimodal therapy. This case highlights the importance of gynecological evaluation in female patients with colorectal cancer and demonstrates that aggressive multimodal management can achieve prolonged disease control.

PubMedDrug and alcohol dependence reports2026-08-30

Exploring hormonal influences on nicotine craving and use across the perinatal period: A prospective longitudinal study.

Allen Alicia M AM, Baurley James J, Linde-Krieger Linnea B LB, Chalke Arushi A et al.

Perinatal nicotine use is common despite well-documented adverse consequences. We examined associations between reproductive-related hormones with nicotine craving and use during the perinatal period to identify potential novel intervention points. All participants reported use of nicotine during the perinatal period. Participants were enrolled at gestational week ≥ 36 and followed to postpartum week 12 via daily surveys (i.e., nicotine craving via 100-point scale, dichotomous use) and weekly hormone measurement in saliva (cortisol, oxytocin) or dried blood spots (progesterone, estradiol, testosterone, dehydroepiandrosterone sulfate). Bayesian mixed-effects models accounted for within-person correlation while estimating hormone effects. Participants (n = 46) were 28.9 ± 4.9 years old. During follow-up, exclusive combustible cigarettes (n = 20), electronic nicotine delivery systems (ENDS; n = 13), or dual (n = 2) use was observed, with variability in use and craving across participants and over time. During pregnancy, higher oxytocin was linked to greater craving (β=16.31, 95% CI: 3.71, 28.83). Greater peripartum declines in oxytocin were associated with more craving (β=8.71, 95% CI: 0.75, 16.93) and use (β=1.13, 95% CI: 0.05, 2.43). During postpartum, lower estradiol was linked to more craving (β=-1.17, 95% CI: -2.15, -0.18) and use (β=-0.40, 95% CI: -0.76, -0.03). In models simultaneously evaluating all postpartum hormones, the lone meaningful association was between estradiol and craving (β=-1.66, 95% CI: -2.84, -0.48). The results of this study suggest that oxytocin and estradiol may contribute to the risk of perinatal nicotine use. Additional research is needed to replicate our observations in more diverse study samples and explore implications for clinical intervention.

PubMedSkeletal radiology2026-08-30

De novo osteosarcoma following prolonged denosumab treatment for giant cell tumor of bone at an anatomically distant site: a case report.

Burbank Katherine Elon KE, Henshaw Robert Mikael RM, Jelinek James Stephen JS, Murphey Mark D MD

Denosumab is a monoclonal antibody targeting RANKL, FDA-approved for the treatment of giant cell tumor of bone (GCTB). While it has shown efficacy in tumor regression and bone preservation, rare cases of malignant transformation to osteosarcoma have been associated with denosumab treatments. Previous literature has attributed such cases to either initial misdiagnosis of a malignant giant cell tumor at baseline presentation or, more rarely, transformation of previously histologically benign GCTB to a secondary malignant GCTB. To our knowledge, these cases involved or arose from an existing giant cell tumor neoplasm. We present a unique case of a patient who developed de novo osteosarcoma at a distant location from their original GCTB tumor following prolonged denosumab therapy, highlighting the clinical course, diagnostic challenges, and therapeutic considerations.

PubMedChemical communications (Cambridge, England)2026-08-30

Mapping conformational heterogeneity: 19F-Gd3+ ENDOR reveals otherwise hidden rotamer conformations.

Habel Edan E, Judd Martyna M, Huber Thomas T, Cox Nicholas N

19F-Gd3+ ENDOR is used to map the full conformational distribution of Trp42 in dihedral space in a de novo luminescent lanthanide-binding protein. By combining genetically encoded fluorination with regularisation modelling, we extract 19F-Gd3+ distance distributions, revealing a minor rotamer population proximal to the lanthanide, key for photoactivity.

PubMedBioinformatics and biology insights2026-08-30

De Novo Molecular Design and Bioactivity Prediction of Novel Hexahydroquinolines as Plasmodium falciparum Calcium-Dependent Protein Kinase 4 (CDPK4) Inhibitors.

Oduselu Gbolahan O GO, Bodun Damilola S DS, Ajani Olayinka O OO, Conway David J DJ et al.

Plasmodium falciparum Calcium-Dependent Protein Kinase 4 (PfCDPK4) is a validated target for malaria transmission-blocking interventions, as its inhibition disrupts male gametocyte exflagellation. Hexahydroquinolines (HHQs) have emerged as promising gametocytocidal agents. This study aimed to design novel HHQs as potential PfCDPK4 inhibitors with good binding affinity, favourable pharmacokinetics, and structural stability. A library of 20,000 novel HHQ analogs was generated using genetic algorithm-driven de novo molecular design in AlvaBuilder and systematically filtered through a pipeline comprising machine-learning-based bioactivity prediction, PAINS removal, pharmacophore modeling, ADMET screening, and structure-based virtual screening. Top-ranking compounds underwent bioisosteric optimization and were evaluated using 300 ns molecular dynamics simulations and density functional theory (DFT) calculations. Comparative in silico validation against known inhibitor Bumped Kinase Inhibitor-1 (BKI-1) and the co-crystallized ligand DXR as controls demonstrated that four HHQ analogs exhibited comparable binding affinities and stable interactions with key residues within the ATP-binding pocket. Favourable ADMET profiles, dynamic stability, and supportive electronic properties further reinforced their inhibition potential. These findings provide biologically meaningful computational evidence supporting HHQ scaffolds as potential PfCDPK4 inhibitors and demonstrate the utility of integrated bioinformatics approaches for malaria transmission-blocking drug discovery. Further experimental validation is required to confirm the inhibitory activities of the identified hexahydroquinoline compounds.

PubMedCureus2026-08-30

Effectiveness of Adherence to Antenatal Exercise on Labor Duration in Normal Vaginal Delivery.

Desai Sakshi S SS, S Anandh A

Prolonged labor during normal delivery is a common concern influenced by maternal factors such as age, fitness level, and pregnancy-related weight gain. Adherence to antenatal exercise programs, which often include breathing exercises, stretching, and pelvic floor components, is evidently related to enhanced labor outcomes. This study investigates the effectiveness of adherence to antenatal exercises in relation to the duration of labor in women planning to undergo normal delivery. The present study included 44 pregnant women in the third trimester (aged 20-30 years) planning normal vaginal delivery. Participants were randomly divided by sealed envelope method into Group A (control, n = 22) receiving conventional exercises and Group B (experimental, n = 22) receiving a structured antenatal exercise program including progressive yoga poses over 12 weeks. Outcome measures included the duration of labor, Numerical Pain Rating Scale (NPRS), and Borg Rating of Perceived Exertion (RPE) Scale. Following the 12-week intervention, women in the experimental group (Group B) demonstrated significantly shorter total labor duration (6.4 ± 1.2 hours) compared to the control group (Group A) (7.8 ± 1.4 hours, t = 3.56, p < 0.05). Group B also demonstrated significantly lower pain intensity on the NPRS (2.93 ± 0.73) compared to Group A (5.79 ± 1.36). Similarly, Group B reported significantly lower perceived exertion on the Borg RPE (7.5 ± 1.45) compared to Group A (12.5 ± 1.02). Within-group analysis confirmed that both groups showed significant improvement from pre- to post-intervention on the NPRS and Borg RPE Scale (labor duration, being a single delivery-time outcome, was not assessed pre-intervention), and the magnitude of improvement was markedly greater in Group B across all outcome measures. Mean session adherence was comparable between groups (91.3% in Group B vs. 88.6% in Group A, p = 0.32), indicating that the observed between-group differences were not attributable to differential compliance. The study suggests that among pregnant women planning to undergo normal delivery, structured antenatal exercises may be more effective than traditional exercises in decreasing duration of labor, pain, and physical exertion; given the modest sample size, these findings should be interpreted with caution and confirmed in larger trials.

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