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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

PubMedJAMA network open2026-08-04

Racial Differences in Sonographic Evaluation in Suspected Cases of Endometrial Neoplasia.

Rotenberg Ohad O, Fridman Dmitry D, Goldstein Steven S, Leone Francesco Paolo Giuseppe FPG et al.

Black women have twice the endometrial cancer mortality of White women, and studies suggest that differences in ultrasound diagnostic accuracy partially contribute to this disparity. To evaluate racial and ethnic differences in the diagnostic performance of transvaginal ultrasound for detecting endometrial neoplasia. A prospective cohort study of 1833 women aged 50 years or older at risk of endometrial neoplasia, conducted at a large urban academic medical center from February 2014 to August 2022, with follow-up through March 2023. The statistical analyses were conducted from March 2024 to December 2025. Women underwent endometrial assessment via transvaginal ultrasound followed by sonohysterogram-directed biopsy and follow-up observation to establish final outcome. Assessment of transvaginal ultrasound diagnostic performance for detecting endometrial cancer and hyperplasia across racial and ethnic groups, measured by: (1) completion rate (endometrial accessibility) and (2) accuracy of completed scans. To assess any association with fibroids, analyses were repeated after excluding women with fibroids. Subgroup analyses were conducted among women with endometrial cancer, those with postmenopausal bleeding, and those without prior exposure to estrogen or tamoxifen. A total of 1833 women met inclusion criteria (mean [SD] age, 60.3 [8.1] years). Most were postmenopausal (1218 women [87.4%]), and 832 (45.4%) were Black, 705 (38.5%) were Hispanic, and 253 (13.8%) were White. Black women had significantly lower completion rates (adequate endometrial visibility) for transvaginal ultrasound compared with White women (75.7% vs 88.9%; relative risk, 0.85; 95% CI, 0.80-0.90; P < .001). Accuracy of completed transvaginal ultrasound was slightly lower among Black women compared with White women (sensitivity, 96.3%; 95% CI, 91.3%-100% vs 100%; negative predictive value, 97.9%; 95% CI, 95.0%-100% vs 100%). After excluding women with fibroids, differences in completion and accuracy between Black and White women disappeared. Similar findings were observed in subgroup analyses of women with a final diagnosis of endometrial cancer, those presenting with postmenopausal bleeding, and those without prior exposure to estrogen or tamoxifen. In this cohort study of a diverse population of women, ultrasound completion rates were lower among Black women, primarily due to fibroids impairing endometrial visibility. Nevertheless, transvaginal sonography demonstrated a 76% completion rate and retained excellent ability to exclude cancer in Black women, regardless of fibroid presence.

PMID 42550505
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PubMedRevue medicale de Liege2026-08-03

[Retinal intoxication with tamoxifen treatment for breast cancer].

Pegolotti Marine M, Locht Bénédicte B, Rakic Jean-Marie JM

Breast cancer is often treated with tamoxifen, a drug that can cause ocular side effects, including toxic retinopathy. Multimodal imaging, particularly optical coherence tomography (OCT), has improved the detection of early lesions such as foveal pseudocysts, thus increasing the prevalence of this complication. We present a case of tamoxifen-induced retinopathy in a patient treated for four years who developed decreased visual acuity with irreversible retinal lesions in the right eye despite discontinuation of the treatment. OCT was essential in characterizing the lesions. The pathophysiology remains poorly understood, but involvement of Müller cells and glutamate accumulation in the retinal pigment epithelium are suspected. Toxicity depends on cumulative dose, duration of treatment, and individual factors. Initial ophthalmologic screening and regular OCT monitoring are recommended to detect retinal damage early. In case of lesions, substitution with an aromatase inhibitor is often considered to limit lesion progression and preserve vision.

PMID 42544074
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PubMedBone & joint research2026-08-01

Phenotypic divergence in rotator cuff tear and volumetric muscle loss mouse models following fibroadipogenic progenitor depletion.

Wang Zili Z, Sang Luke L, Youn Alex A, Liu Mengyao M et al.

Fibroadipogenic progenitors (FAPs) are a group of resident muscle stem cells capable of differentiating into fibroblasts and adipocytes, contributing to intramuscular fibrotic and fatty degeneration after injury. However, FAPs are also thought to play a crucial role in muscle regeneration by facilitating satellite cell myogenesis. Despite this dual role, the precise functions of FAPs in muscle degeneration and regeneration remain unclear. This study aimed to utilize a FAP depletion mouse model to define the role of FAPs in two distinct, clinically relevant injury models of rotator cuff tears (RCTs) and tibialis anterior (TA) volumetric muscle loss (VML). Six PDGFRα-CreERT/DTA mice were applied for fluorescence-activated cell sorting (FACS) evaluation of FAP depletion efficiency with tamoxifen induction. Then, two groups of ten PDGFRα-CreERT/DTA mice and five DTA mice underwent either unilateral supraspinatus and infraspinatus tendons and suprascapular nerve transection (RCT model) or the creation of a 4 mm diameter defect in the unilateral TA (VML model). To induce FAP depletion, tamoxifen or corn oil (control) was administered daily for two weeks before surgery. Gait analysis was conducted at six weeks post-surgery to evaluate shoulder or hindlimb function. Supraspinatus or TA muscles were harvested to assess muscle atrophy and for histological analysis. FACS analysis confirmed a 50% reduction in FAPs following tamoxifen administration in PDGFRα-CreERT/DTA mice. In the RCT model, FAP depletion significantly attenuated muscle atrophy and improved fibrosis, fatty infiltration (FI), and global shoulder function. Conversely, in the VML model, FAP depletion significantly decreased muscle fibrosis but had no effect on FI and functional outcomes. Our results suggest that FAPs play distinct roles in muscle regeneration depending on the specific clinical context. These models can be used to further understand the different injury mechanisms and muscle-specific properties influencing FAP roles in musculoskeletal pathology.

PMID 42538008
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PubMedCureus2026-07-30

Single-Cell Profiling Identifies the SPDEF/GAS5 Axis as a Potential Driver of Tamoxifen Resistance in Estrogen Receptor-Positive Breast Cancer.

Jin Wen W, Chen Claire C, Zhou Yanling Y, Wang Jing J et al.

Background Estrogen receptor-positive (ER+) breast cancer is the most prevalent breast cancer subtype, and tamoxifen remains the cornerstone of adjuvant endocrine therapy. However, a significant proportion of patients eventually develop acquired tamoxifen resistance, leading to disease recurrence and progression. Methodology To characterize the cellular and molecular mechanisms underlying this resistance at single-cell resolution, we performed an integrative analysis of publicly available single-cell RNA sequencing data from 16 ER+ breast cancer specimens, comprising 13 treatment-naive primary tumors and three tamoxifen-resistant recurrent tumors. Following rigorous quality control, batch correction, and dimensionality reduction, we identified 11 major cell populations in the tumor microenvironment. Copy number variation inference using InferCNV was utilized to confirm the malignant identity of the epithelial cells. Results Gene Ontology Biological Process enrichment analysis revealed that recurrent malignant cells were significantly enriched for pathways associated with translation, chromatin remodeling, and cell division compared with primary tumor cells. Sub-clustering of malignant epithelial cells resolved nine distinct subpopulations, among which a GAS5+ (growth arrest-specific 5-positive) subpopulation was markedly expanded in tamoxifen-resistant recurrent tumors. This subpopulation exhibited distinctive metabolic reprogramming characterized by enhanced aerobic respiration and energy metabolism. Monocle2-based pseudotemporal trajectory analysis positioned GAS5+ cells at a terminally differentiated state, likely derived from CLDN3+ and CEACAM6+ tumor progenitor cells. Single-cell regulatory network inference using SCENIC identified SPDEF (SAM pointed domain-containing ETS transcription factor) as a putative key transcription factor specifically active in GAS5+ tumor cells, and SPDEF expression was highly enriched in this subcluster. Validation in The Cancer Genome Atlas breast cancer cohort demonstrated that high SPDEF expression was significantly associated with worse overall survival (log-rank p = 0.011). Conclusions These findings implicate the SPDEF-GAS5+ regulatory axis as a potential driver of tamoxifen resistance and a compelling candidate for future therapeutic targeting in ER+ breast cancer.

PMID 42528776
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PubMedJournal of affective disorders2026-07-30

Efficacy, acceptability, and related outcomes of pharmacological interventions for acute bipolar mania: a systematic review and dose-related network meta-analysis across different age groups.

Fornaro Michele M, Di Lorenzo Chiara C, Kishi Taro T, Daray Federico Manuel FM

Acute bipolar mania carries negative social and economic consequences. We investigated the comparative efficacy/response/acceptability of pharmacological interventions for acute bipolar mania, considering dose effects across different age groups. We conducted a network meta-analysis (NMA) to search for randomized controlled trials (RCTs) comparing pharmacological interventions with one another or placebo in acute bipolar mania patients, indexed in PubMed/MEDLINE, Embase, Web of Science, and Scopus (from inception through 2025.12.24). Co-primary outcomes were change in manic symptoms/response/and acceptability. Tolerability/remission and rate of adverse events were secondary outcomes. Confidence-In-Network-Meta-Analysis was likewise appraised. 113 RCTs, encompassing 49 distinct treatment combinations, included 20,666 participants. Sensitivity analysis retaining only low-risk-of-bias studies and excluding outliers for possible effect modifiers indicated that risperidone 3 mg/day(SMD = -7.57;95%C.I. = -8.25;-5.85); tamoxifen 160 mg/day(SMD = -1.73;95%C.I. = -2.32;-1.13); rivastigmine 3 mg/day(SMD = -1.13;95%C.I. = -1.06;-0.58); haloperidol 30 mg/day(SMD = -0.96;95%C.I. = -1.25;-0.75); valproate 750 mg/day(SMD = -0.76;95%C.I. = -1.48;-0.58); tamoxifen 40 mg/day(SMD = -0.75;95%C.I. = -1.41;-0.59); celecoxib 400 mg/day(SMD = -0.74;95%C.I. = -1.20;-0.38); paliperidone extended-release 12 mg/day(SMD = -0.62; 95%C.I. = -0.91;-0.32); olanzapine 15 mg/day(SMD = -0.59;95%C.I. = -0.60;-0.38); olanzapine 20 mg/day(SMD = -0.52;95%C.I. = -0.66;-0.38); risperidone 4 mg/day(SMD = -0.53;95%C.I. = -0.76;-0.29); allopurinol 600 mg/day(SMD = -0.54;95%C.I. = -0.67;-0.22); cariprazine 12 mg/day(SMD = -0.49;95%C.I. = -0.66;-0.33); risperidone 4.2 mg/day(SMD = -0.46;95%C.I. = -0.75;-0.17); lithium 1500 mg/day(SMD = -0.42;95%C.I. = -0.57;-0.28); ziprasidone 160 mg/day(SMD = -0.49;95%C.I. = -0.68;-0.31); asenapine 20 mg/day(SMD = -0.38;95%C.I. = -0.53;-0.22); haloperidol 8 mg/day(SMD = -0.34;95%C.I. = -0.63;-0.05); aripiprazole 15 mg/day(SMD = -0.33;95%C.I. = -0.61;-0.06) outperformed placebo. Ziprasidone 160 mg/day, celecoxib 200 mg/day, asenapine 20 mg/day, and asenapine 10 mg/day proved more efficacious than placebo in children. No statistically significant differences were reported between treatments and placebo for response/remission/acceptability/tolerability, and manic/hypomanic switch. A meta-regression of efficacy effect sizes against the adapted AMSTAR-Plus content scores showed that larger SMDs were associated with lower AMSTAR scores, indicating lower study quality, warranting further caution for such large efficacy estimates. Our findings are consistent with previous NMAs and current guidelines, expanding the current knowledge base while concurrently appraising different drugs, doses, and age groups.

PMID 42526603
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PubMedJAMA network open2026-07-30

Adiposity Excess and Vertebral Fractures in Patients With Breast Cancer Taking Aromatase Inhibitors.

Schivardi Greta G, Cosentini Deborah D, Scartabellati Giulia G, Ravanelli Marco M et al.

Aromatase inhibitors (AIs) profoundly suppress estrogen synthesis and accelerate bone loss in postmenopausal women with early breast cancer (EBC). Although body mass index (BMI)-defined obesity has been considered protective for skeletal health, emerging evidence suggests a paradoxical association with fracture risk. To evaluate whether fat mass percentage (FM%) greater than 40.8%, measured by dual-energy x-ray absorptiometry (DXA), is associated with vertebral fracture (VF) progression in patients with EBC receiving AIs. This retrospective cohort study included consecutive postmenopausal women with EBC (stages I-III) recruited in a single referral center between September 2014 and June 2024. All patients received adjuvant endocrine therapy and underwent serial DXA assessments. Patients treated with tamoxifen or with major comorbidities affecting skeletal fragility were excluded. Body composition and bone fragility parameters evaluated by DXA at baseline and at 18, 24, and 30 months. Adiposity excess was defined as FM% greater than 40.8%, and VF progression was defined as new incident fractures and/or worsening by at least 1 Genant grade at a previously fractured vertebral level. Their association was evaluated using a joint model; time-dependent associations were evaluated using extended Cox regression. Secondary analyses explored associations with bone mineral density, trabecular bone score (TBS), appendicular lean mass index (ALMI), and traditional fracture risk factors. A total of 769 White women (median [range] age, 63 [30-87] years; median [range] BMI, 24.6 [15.6-46.1]) entered the study. During follow-up, 69 patients (9.0%) experienced VF progression. FM% greater than 40.8% was independently associated with increased VF progression (adjusted hazard ratio [HR], 2.00; 95% CI, 1.44-2.82; P < .001). Higher ALMI (HR, 0.38; 95% CI, 0.22-0.65; P < .001) and BMD (HR, 0.79; 95% CI, 0.66-0.94; P = .01) were associated with lower risk of VF progression. In this retrospective cohort study of patients with EBC receiving AIs, adiposity excess was identified as a novel fracture risk factor, whereas higher muscle mass was protective. These findings support incorporating body-composition assessment into fracture-risk evaluation and preventive strategies for patients undergoing AI therapy.

PMID 42530924
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