SR appears to be a potential therapeutic agent for endometriosis by suppressing inflammatory and pain-related factor expressions by inhibiting the nuclear factor-kappa B pathway.

ERβ activation was found to reduce the expression of GULP1 as a direct downstream target in bladder cancer cells, resulting in the induction of cisplatin resistance.

Current Protocols published by Wiley Periodicals LLC. Basic Protocol 1: Establishment of a high-throughput ERα reporter gene assay with luminescence readout to identify activators and inhibitors of estrogen receptor α Basic Protocol 2: Use of an orthogonal assay with fluorescence readout to confirm potential estrogen receptor activators or inhibitors.

Adding the CDK4/6 inhibitor palbociclib enhanced the antitumor activity of EP0062 or fulvestrant in ESR1-mutant models but not in HER2-enriched or PTEN-mutant PDX models...EP0062 triggers an E2F1 downmodulation which mediates a potent antiproliferative activity. For EP0062-resistant tumors that remain ER-driven, the addition of palbociclib displays a potent antitumor effect.

P2, N=37, Active, not recruiting, Medical College of Wisconsin | Trial completion date: Jul 2024 --> Mar 2025

These findings underscore the influence of tamoxifen derivatives on DNA methylation patterns, particularly through modulating TET3 expression, which appears to be contingent on the presence of estrogen receptors. This study highlights the potential of targeting epigenetic modifications for personalized anti-cancer therapy, offering a novel avenue to improve treatment outcomes.

P=N/A, N=100, Not yet recruiting, Assiut University

P4, N=21, Not yet recruiting, McGill University Health Centre/Research Institute of the McGill University Health Centre | Trial primary completion date: Jul 2026 --> Oct 2026

P2, N=19, Active, not recruiting, Stanford University | Recruiting --> Active, not recruiting | N=150 --> 19

P1, N=15, Not yet recruiting, University of Nebraska | Initiation date: May 2024 --> Sep 2024

P4, N=21, Not yet recruiting, McGill University Health Centre/Research Institute of the McGill University Health Centre | Trial completion date: Aug 2026 --> Dec 2026 | Trial primary completion date: Feb 2026 --> Jul 2026

Resveratrol increasead the in vitro cytotoxic effect of conventional therapy in breast cancer cells. However, it was necessary to block resveratrol-induced autophagy to improve the therapeutic response.

No abstract available

P2, N=30, Completed, Johns Hopkins University | Active, not recruiting --> Completed

P2, N=74, Not yet recruiting, University of Chicago

The lead compound was found to have a significant effect on the signaling pathways in parental and 4-hydroxytamoxifen-resistant cells...Accumulation of cleaved poly(ADP-ribose) polymerase in cells treated with compound 2f indicated induction of apoptosis. The selectivity analysis showed that lead compound 2f produces no significant effects on cytochromes P450, CYP19A1, CYP21A2, and CYP7B1.

P4, N=120, Completed, University of Palermo

P1, N=15, Not yet recruiting, University of Nebraska

P4, N=103, Completed, University of Palermo

XAV-939, Fulvestrant, and SR16157 may have potential value in the clinical use of LUAD. We revealed the potential linkage between PRGs and LUAD prognosis, and the application of these prognostic factors in risk stratification and prognosis prediction of LUAD patients may be of great significance.

BZA treatment alone led to a tenfold reduction in cellular proliferation compared to estrogen-treated cells, suggesting antiproliferative effects. Understanding BZA's modulation of BRCA1 and ERα, along with their mechanistic interactions, is vital for comprehending its impact on breast cancer tumor suppressors and hormone receptors.

P2, N=31, Completed, National Institute of Allergy and Infectious Diseases (NIAID) | Active, not recruiting --> Completed | Trial completion date: Oct 2023 --> Jul 2023

This study highlights the potential of SERMs as inhibitory ligands for immune checkpoint proteins, emphasizing the importance of considering PD-1 and CTLA-4 inhibition when evaluating SERMs as therapeutic agents. Our findings open new avenues for cancer immunotherapy by exploring the interaction between various SERMs and immune checkpoint pathways.

P4, N=21, Not yet recruiting, McGill University Health Centre/Research Institute of the McGill University Health Centre | Phase classification: P=N/A --> P4 | Trial completion date: Nov 2025 --> Aug 2026 | Initiation date: Nov 2023 --> Feb 2024 | Trial primary completion date: Nov 2025 --> Feb 2026

P4, N=160, Recruiting, The Alfred | Trial completion date: Dec 2023 --> Dec 2025 | Trial primary completion date: Dec 2022 --> Dec 2025

P4, N=13, Completed, The Alfred | Unknown status --> Completed | N=180 --> 13

The levels of liver injury serum biomarkers, liver content of interleukin-6 (IL-6), relative liver weight and distortion of liver histological pictures were significantly increased in ovariectomized (OVX) rats and SHAM rats that received DEN alone and were further exaggerated when DEN was combined with fulvestrant (F) compared to non-DEN treated rats...The tapering impact on these parameters was clear in OVX rats that received estradiol benzoate (EB), silymarin (S) or orlistat (ORS)...In addition, ORS induced similar mitigating effect against DEN-induced HCC which could be attributed to FASN inhibition and anti-inflammatory effect. Furthermore, S alleviated DEN-induced HCC, independent of its estrogenic effect.

P2, N=60, Recruiting, Jose Pablo Leone | Not yet recruiting --> Recruiting

Associations between 27-HC and breast cancer prognosis varied by circulating estradiol levels and endocrine therapy. Less consistent results were observed for 25-HC.

P2, N=37, Active, not recruiting, Medical College of Wisconsin | Trial completion date: Jul 2023 --> Jul 2024

Tamoxifen, a popular selective estrogen receptor modulator, can treat breast cancer but also has unfavourable side effects due to its estrogenic activity in other tissues...Moreover, several of these compounds speed up cell death by supressing estrogen receptor gene expression. This opens wide avenue to introduce number of natural medicines with a revolutionary therapeutic impact and few side effects.

UA is safe to consume and is very well tolerated. This study further opens up the potential of UA as ER modulator and its benefits in estrogen-dependent tissues.

P2, N=60, Not yet recruiting, Jose Pablo Leone | Initiation date: Feb 2023 --> Oct 2023

When facing moderate-severe GSM, the options for BCS are limited: local estrogen therapy, considered the 'gold standard' but with concerns about safety; vaginal androgens and prasterone, which seem to trigger an activation of estrogen and androgen receptors of the vaginal epithelium layers, without activating estrogen receptors on other tissues, being potentially safe but still without strong evidence in favor of BCS; vaginal lasers, which appear to improve vascularization of vaginal mucosa by stimulating the remodeling of the underlying connective tissue, but with contradictory results of efficacy in recent randomized clinical trials; and ospemifene, an oral selective estrogen receptor modulator presenting mild vaginal estrogenic potency and anti-estrogenic effect at the endometrial and breast level, but still not recommended for use in BCS in recent North American Menopause Society guidelines...On the other hand, sexuality must be seen as a multifactorial issue, where GSM is only part of the problem; evidence shows that sexual counseling improves the quality of life of BCS. Finally, there is a need to limit the underdiagnosis and undertreatment of GSM in BCS; the primary goal of physicians treating BCS regarding this issue has to be the provision of information of what to expect regarding genital and sexual symptoms to BCS and to counsel on early first-line treatments that may help prevent more severe GSM.

P2, N=150, Recruiting, Stanford University | Not yet recruiting --> Recruiting

P2, N=150, Not yet recruiting, Stanford University | N=100 --> 150

Subjects will be followed yearly for 10 years post-surgery for recurrence free survival and overall survival. Initial results are expected 2024. Conclusion(s): This trial will assess the potential feasibility of lasofoxifene as NET among women with HR+, HER2-, locally advanced breast cancer.

P3; N=10000 --> 5083 | Trial completion date: Feb 2023 --> Mar 2024

This study demonstrates that ormeloxifene promoted pulmonary 17β-estradiol synthesis, alleviated inflammation, improved the NOX4/HO1/Nrf/PPARγ/PGC-1α axis, and attenuated pulmonary hypertension. It is evidently safe at tested concentrations and may be effectively repurposed for pulmonary hypertension treatment.

Since the introduction of tamoxifen for adjuvant endocrine therapy in women with non-metastatic ER+ breast cancer, subsequent trials have demonstrated an oncologic benefit with the addition of ovarian function suppression (OFS) to adjuvant endocrine therapy...The long-term sequelae of bilateral oophorectomy include cardiovascular and bone density morbidity along with sexual dysfunction, negatively impacting overall quality of life. As gynecologists are the providers consulted to perform bilateral oophorectomies in this population, careful consideration of each patient's oncologic prognosis, cardiovascular risk, and psychosocial factors should be included in the preoperative assessment to assist in shared decision-making and prevent the lifelong adverse effects that may result from overtreatment.

In an in-vivo mice model, treatment with CANN14 and low doses of tamoxifen reduced tumor volumes and weights. Treatment with 373.15b by itself reduced tumor volumes and weights, but the effect was more profound when combined with tamoxifen.

The stability of the Tc(IV)-genistein complex was confirmed by DFT calculations at a value of 99.0822. As a result, [Tc]Tc-genistein could be a potential radiotracer kit for SPECT imaging of breast cancer.