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tamoxifen (tamoxifen, Douglas)

✓ Approved

Douglas Pharmaceuticals Limited · ESR1 · 小分子

什么是 tamoxifen？

tamoxifen 是一种小分子，由Douglas Pharmaceuticals Limited研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名tamoxifen, Douglas
公司Douglas Pharmaceuticals Limited
药物类别小分子
分子靶点ESR1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Douglas Pharmaceuticals Limited

作用机制

分子靶点

tamoxifen 作用于 1 个分子靶点：

ESR1estrogen receptor 1 (ER, ESR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

tamoxifen 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Breast cancer✓ Approved

相关研究文献

PubMedJournal of the National Cancer Institute2026-09-10

Endocrine Biomarker Changes in a Randomised Low-Dose Tamoxifen Trial for Breast Cancer Prevention.

Nash Stephen S, Hammarström Mattias M, Thörngen John-Olof JO, Winqvist Ola O et al.

Tamoxifen reduces breast cancer incidence and recurrence, but uptake for primary prevention remains limited, largely because of concerns regarding adverse effects at the standard 20 mg dose. Understanding systemic endocrine effects of lower tamoxifen doses may help improve future prevention strategies. We analysed data from 1,055 healthy women enrolled in the randomised, double-blind, placebo-controlled KARISMA trial, assigned to placebo or tamoxifen 1, 2.5, 5, 10, or 20 mg daily for 6 months. Plasma concentrations of endocrine biomarkers and tamoxifen metabolites were measured at study end. Associations between randomised tamoxifen dose, circulating metabolite concentrations, and endocrine biomarker plasma concentration (estrogens, androgens, progestogens, cortisol, prolactin, and sex hormone-binding globulin (SHBG)), were evaluated. Tamoxifen dose was associated with measurable endocrine changes after six months, most consistently increased SHBG levels, with additional associations observed for cortisol and hydroxyprogesterone. SHBG demonstrated the clearest dose-response relationship, with increasing levels across tamoxifen dose groups and evidence of attenuated increase at intermediate doses. Large relative differences between placebo and 20 mg tamoxifen were additionally observed for estrone, estrone sulphate and estradiol. Unadjusted analyses of circulating endoxifen showed broadly similar endocrine patterns; however, these associations were substantially attenuated after adjustment for randomised tamoxifen dose. Circulating tamoxifen metabolites were strongly correlated with administered dose and with one another. Low-dose tamoxifen was associated with measurable endocrine changes, particularly in SHBG, cortisol, and hydroxyprogesterone. These findings show endocrine pharmacodynamic responses during low-dose tamoxifen therapy warrants further investigation as a potential component of future individualised prevention and adjuvant endocrine therapy strategies. ClinicalTrials.gov ID: NCT03346200.

PMID 42720596
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PubMedClinical radiology2026-09-09

Endometrial imaging.

Creaney K K, Ordidge K K, Sahdev A A

Imaging remains fundamental to the diagnosis and management of endometrial disorders. Recognition of the normal endometrium in premenarchal, menstruating, post-partum and post-menopausal patients, as well as patients taking medications such as hormone replacement therapy and tamoxifen, is essential to exclude endometrial pathology. In addition, endometrial cancer is now the most common gynaecological malignancy in the United Kingdom, and imaging remains central to the diagnosis and management of these patients. This paper explores multimodality imaging appearances of the endometrium, including normal appearances and abnormalities such as polypoid lesions, hyperplasia and endometrial cancer. Secondary endometrial tumours as well as infective/inflammatory endometrial pathologies are also considered. Transvaginal ultrasound (TVUS) is the first-line imaging for endometrial assessment, and the normal appearances vary according to menstrual cycle and menopausal status. Most endometrial pathologies are identified and characterised with TVUS. Further imaging with magnetic resonance imaging (MRI) is useful to stage endometrial cancer, while computed tomography (CT) is usually reserved for the staging and post treatment follow up of distant metastases. This review article provides a current summary of endometrial imaging in the United Kingdom, including normal endometrial appearances and endometrial disorders across the range of imaging modalities.

PMID 42716865
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PubMedThe Journal of neuroscience : the official journal of the Society for Neuroscience2026-09-09

Nestin-Cre Mouse Lines: A User Guide for CNS Genetics.

Thomas Maya M, Wei Pei-Chi PC

Nestin-Cre is the most widely used Cre driver for conditional genetic manipulation in the central nervous system (CNS), underpinning hundreds of studies in neurodevelopment, lineage tracing, brain tumor modeling, and circuit analysis. Despite its dominant role, divergent recombination outcomes-spanning developmental onset, penetrance, mosaicism, and ectopic activity-are frequently reported, creating substantial interpretive challenges across the field. Here we provide a practical guide to selecting and using Nestin-Cre and Nestin-CreER(T2) mouse lines for CNS research. We systematically examine 22 independently generated lines (1996-2025), synthesizing data from >400 published studies. Rather than cataloguing line histories, we organize this knowledge around the decisions experimentalists actually face: whether to use a constitutive or inducible system, which lines best target specific CNS compartments and developmental windows, and how to achieve uniform versus sparse recombination. We show that reported variability is not an intrinsic limitation of Nestin-based drivers but arises from definable, controllable factors-construct architecture, transgene integration context, reporter sensitivity, breeding configuration, and, for inducible systems, tamoxifen formulation and dosing. Each factor is addressed with specific guidance. For inducible lines, we provide a comparative ranking of recombination efficiency against background leakiness to inform line selection. We highlight breeding strategy as a critical and frequently mismanaged variable, discuss Cre-dosage effects on neural progenitor survival, and address reporter-dependent differences in apparent recombination efficiency. Together, this TechSight article offers a consolidated, decision-oriented framework for reproducible CNS-targeted genetic experiments, converts the thesis into bench practice, and reduces wasted cohorts.

PMID 42716801
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PubMedJournal of menopausal medicine2026-09-08

Endometrial Polyp and Vaginal Superficial Myofibroblastoma following Tamoxifen Use: A Case Study.

Kim Min-Sun MS, Lee Hae-Hyeog HH, Han Eunkyung E, Park Young-Ji YJ et al.

Tamoxifen, a selective estrogen receptor modulator, is the standard adjuvant therapy for hormone receptor-positive breast cancer. Although it acts as an estrogen receptor antagonist in breast tissue, it may exert agonistic effects on the endometrium, increasing the risk of endometrial polyps, hyperplasia, and malignancy. We report a rare case of a 51-year-old woman who developed both an endometrial polyp and a vaginal superficial myofibroblastoma after approximately 4 years of tamoxifen therapy. This case emphasizes the importance of long-term gynecologic surveillance in patients receiving tamoxifen treatment.

PMID 42711105
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PubMedCirculation2026-09-08

Impaired Glycolysis Leads to Defective Efferocytosis and Impaired Plaque Resolution in Tet2 Clonal Hematopoiesis.

Yalcinkaya Mustafa M, Hsu Cheng-Chieh CC, Li Linke L, Wang Ranran R et al.

Clonal hematopoiesis (CH) arising from mutations in hematopoietic genes has been identified as an important risk factor for atherosclerotic cardiovascular disease. Despite the established role of some CH mutations in promoting atherosclerosis progression, their role in clinically relevant LDL (low-density lipoprotein) lowering-induced plaque remodeling or regression has not been extensively studied. To assess the effects of TET2 (tet methylcytosine dioxygenase 2) CH on plaque resolution, we prepared control or chimeric Tet2+/- CH mice with conditional deletion of Tet2 in hematopoietic stem cells during LDL lowering-induced plaque remodeling. After establishing atherosclerosis by Western diet feeding for 12 weeks in Ldlr-/- mice, Tet2 was deleted by tamoxifen injection, and hypercholesterolemia was either normalized to simulate clinical lipid management, or mice were continued on the Western diet. Unlike control mice, Tet2+/- CH mice failed to significantly reduce necrotic core area or increase fibrous cap thickness and showed impaired macrophage efferocytosis during LDL lowering. Single-cell RNA sequencing and gene set enrichment analysis of aortic cell populations revealed that Tet2 deficient monocyte/macrophage populations were defective in glycolysis, phagocytosis, and actin polymerization. Tet2-deficient bone marrow-derived macrophages and Tet2+/- induced pluripotent stem cell-derived human macrophages showed defective ability to sustain continuing rounds of efferocytosis. Bone marrow-derived macrophages displayed reduced apoptotic cell binding and internalization and impaired activity of Wiskott-Aldrich syndrome protein and SCAR (suppressor of cyclic AMP receptor) homolog complex mediated actin polymerization. We linked these defects to reduced anaerobic glycolysis and lactate levels and rescued them by lactate supplementation or by treatment with the HIF-1α (hypoxia-inducible factor 1α) activator molidustat. Molidustat treatment reversed the defects in necrotic core and fibrous cap formation during LDL lowering-induced plaque remodeling in Tet2+/- CH mice. Reduced plasma lactate levels were also shown in TET2 clonal hematopoiesis of indeterminate potential carriers in the UK Biobank. Our data identify impaired efferocytosis and glycolysis-lactate-actin polymerization pathways in advanced atherosclerosis as potential therapeutic targets to induce proresolving restructuring of the plaque immune cells and to promote beneficial atherosclerosis remodeling in subjects with TET2 CH.

PMID 42708224
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PubMedSAR and QSAR in environmental research2026-09-07

Computer-aided drug design of quinoxaline based selective oestrogen receptor α modulators for breast cancer therapy: molecular docking, MD simulation, MM-PBSA and ADME/T analysis.

Sharma A A, Kumar D D, Narasimhan B B, Marwaha R K RK

Oestrogen receptor alpha (ERα) is a driver of hormone-dependent breast cancer, yet current therapies are often hindered by drug resistance and adverse effects. In this study, we developed a structure-based virtual screening workflow to identify novel quinoxaline derivatives as computationally prioritized potential ERα modulators. The quinoxaline analogues obtained from PubChem are screened through validated docking model of ERα. The top-ranked candidates were further refined by MD simulations in GROMACS for 300 ns to assess complex stability and interaction persistence, followed by MM-PBSA binding free energy calculations to quantify binding energetics. The prioritized quinoxaline hits exhibited more favourable predicted docking scores than reference ligand, tamoxifen, while MD trajectory analyses indicated stable complex formation with sustained predicted interactions involving key ERα binding site residues. MM-PBSA highlights LIG3 as the most promising lead with a favourable energy (ΔG = -34.15 kcal/mol). Complementary ADMET profiling predicted favourable pharmacokinetic behaviour and low toxicity for the prioritized compounds. This integrated in silico strategy demonstrates that quinoxaline scaffolds, specifically LIG3, represent promising computationally prioritized templates for the further development and experimental evaluation of ERα targeted ligands. These findings provide a reliable computational framework for the prioritization and structural optimization of next-generation anti-breast cancer agents.

PMID 42703730
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