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DRUG CLASS:

Estrogen receptor antagonist

14h
Desmoid Tumor of the Porta Hepatis: A Rare Location With Unusual Clinical Presentation. (PubMed, Case Reports Hepatol)
Adjuvant tamoxifen therapy was administered, and follow-up imaging showed no recurrence...This report highlights an extremely rare presentation of desmoid tumor in the hepatic hilum, mimicking malignancy. It underscores the importance of histopathological confirmation, multidisciplinary management, and individualized follow-up strategies, especially in women of reproductive age.
Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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tamoxifen
14h
Progress of estrogen receptor and splice variants in ovarian carcinoma. (PubMed, J Ovarian Res)
ERα promotes ovarian cancer cell proliferation and migration, and is linked to cisplatin resistance, while its splice variants modulate cancer cell sensitivity to tamoxifen. GPER1 may interact with ERα in ovarian cancer, yet the specific crosstalk mechanism remains unelucidated. Elucidating the complex functional crosstalk of estrogen and ERs, as well as the diverse roles of ER splice variants, is expected to provide novel insights for the early diagnosis and identification of therapeutic targets for ovarian cancer.
Review • Journal
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ER (Estrogen receptor) • GPER1 (G Protein-Coupled Estrogen Receptor 1)
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cisplatin • tamoxifen
3d
GO39932: A Study of GDC-9545 Alone or in Combination With Palbociclib and/or Luteinizing Hormone-Releasing Hormone (LHRH) Agonist in Locally Advanced or Metastatic Estrogen Receptor-Positive Breast Cancer (clinicaltrials.gov)
P1, N=181, Active, not recruiting, Genentech, Inc. | Trial completion date: Jul 2026 --> Jul 2027 | Trial primary completion date: Jul 2026 --> Jul 2027
Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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HER-2 positive • ER positive • HER-2 negative • ER positive + HER-2 negative • HER-2 negative + ER positive
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Ibrance (palbociclib) • triptorelin • goserelin acetate • giredestrant (RG6171)
6d
The EGR1/caspase-14/HIF-1α axis mediates tamoxifen resistance in MCF-7 breast cancer cells. (PubMed, Open Life Sci)
These data indicate that Caspase14 promotes survival, proliferation, and metabolic reprogramming in resistant MCF7 cells via the EGR1/HIF-1α pathway. Our findings reveal a mechanistic link between Caspase14 and endocrine therapy resistance and nominate Caspase14 as a therapeutic target to overcome tamoxifen resistance, with potential translational relevance.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • CASP4 (Caspase 4) • EGR1 (Early Growth Response 1) • CASP1 (Caspase 1)
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tamoxifen
7d
Endocrine therapy reprogramming of breast cancer facilitates metastatic escape via upregulation of P-Rex1/Rac1 signalling. (PubMed, Nat Commun)
Targeting the Rac1 pathway with small molecule inhibitors (NSC23766, R-ketorolac) reduces survival and motility in resistant cells, inhibits in vivo Rac1 activity, and reduces tumour burden when combined with tamoxifen in a drug-refractory patient derived xenograft model. This work identifies the P-Rex1/Rac1 axis as a potential therapeutic target for late recurring ER+ breast cancer.
Journal
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ER (Estrogen receptor)
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tamoxifen • NSC23766
10d
Novel Mechanism of and Therapeutic Approach for Anthracycline-Induced Cardiotoxicity (AIC). (PubMed, Cancer Res Commun)
The cardiomyocyte-specific, tamoxifen-inducible TOP2B transgenic mice exhibited pathophysiological features consistent with doxorubicin-induced cardiotoxicity, even without exposure to anthracyclines. Our findings reveal a novel role for TOP2B in AIC, demonstrating that its upregulation disrupts SMYD1 function in cardiomyocytes, contributing to cardiotoxicity. This study also highlights the therapeutic potential of targeting TOP2B using ASO for preventing AIC in cancer patients, offering new insights into cardioprotective strategies.
Journal
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TOP2A (DNA topoisomerase 2-alpha)
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tamoxifen • doxorubicin hydrochloride
10d
Mortality prediction with adjuvant tamoxifen in breast cancer: Machine learning-integrated explainable artificial intelligence and Bayesian model results. (PubMed, ADMET DMPK)
Integrating machine learning with XAI and Bayesian approaches effectively identified key predictors of mortality in tamoxifen-treated breast cancer patients. However, marked heterogeneity in model performance across subgroups highlights the critical need for external validation and careful evaluation of algorithmic fairness before clinical implementation.
Journal
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ER (Estrogen receptor)
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tamoxifen
14d
Trp53 loss drives the neoplastic transformation of Pik3caH1047R-induced vascular malformation in a mouse model. (PubMed, PLoS One)
Following tamoxifen induction, blood blister-like lesions developed on the tail, ear, and paw in 86.9% (53/61) of mice harboring at least one Pik3caH1047R allele, whereas no lesions were observed in mice lacking the mutant allele (0/13, P < 0.0001)...Together, these findings demonstrate that PIK3CA activation initiates highly penetrant vascular malformations, whereas p53 loss promotes their rare neoplastic transformation. This model provides mechanistic and translational insight into how benign PIK3CA-mutant vascular malformations may progress toward vascular malignancy and offers a platform for studying biomarkers and therapeutic strategies to prevent this transition.
Preclinical • Journal
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TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • FAP (Fibroblast activation protein, alpha) • CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1) • GFAP (Glial Fibrillary Acidic Protein) • PI3K (Phosphoinositide 3-kinases)
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TP53 mutation • PIK3CA mutation
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tamoxifen
14d
Extended Endocrine Therapy and Survival for Breast Cancer Subtypes in Premenopausal Patients. (PubMed, JAMA Netw Open)
EET (with tamoxifen monotherapy, LHRH agonist plus tamoxifen, or LHRH agonist plus aromatase inhibitor), irrespective of the duration of EET, measured at study baseline (defined as the first day of the sixth year after the initiation of adjuvant ET)...In this cohort study, a lower estimated risk with EET use was observed across all surrogate breast cancer subtypes. However, the lower estimated risk was greatest among patients with luminal A-like disease, a finding that warrants confirmation in larger, prospective cohorts.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HER-2 negative
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tamoxifen
14d
Protective Role of Adenosine Triphosphate Against Tamoxifen-Induced Retinal Toxicity in a Rat Model. (PubMed, Medicina (Kaunas))
These findings indicate that ATP attenuates tamoxifen-induced retinal toxicity by supporting mitochondrial energy balance and redox homeostasis. Accordingly, ATP administration may represent a promising protective approach for reducing retinal injury associated with long-term tamoxifen therapy.
Preclinical • Journal
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CAT (Catalase)
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tamoxifen
14d
Efficacy and Safety of Oral Progestogens (Megestrol Acetate and Medroxyprogesterone Acetate) in Heavily Pretreated Oestrogen Receptor-Positive Metastatic Breast Cancer: A 10-Year Multi-Site Study. (PubMed, Cancers (Basel))
Background: Oral progestogens, including megestrol acetate (MA) and medroxyprogesterone acetate (MPA), have largely been superseded by aromatase inhibitors, tamoxifen, and selective oestrogen receptor degraders (SERDs) in oestrogen receptor-positive (ER-positive) metastatic breast cancer. While prior exposure to CDK4/6 inhibitors was associated with shorter PFS, patients without liver metastases appeared to derive the greatest benefit. These findings support a role for oral progestogens in selected patients who have exhausted standard therapeutic options.
Journal
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ER (Estrogen receptor)
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ER positive
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tamoxifen • megestrol
15d
Endoxifen for mammographic density reduction-results from the KARISMA endoxifen trial. (PubMed, J Natl Cancer Inst)
Both 1 and 2 mg of (Z)-endoxifen significantly reduced MBD to a degree comparable to the established 20 mg dose of tamoxifen. The 1 mg dosage of (Z)-endoxifen indicated superior tolerability. Future studies are necessary to confirm impact on breast cancer incidence.
Journal
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ER (Estrogen receptor)
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tamoxifen