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DRUG CLASS:

Estrogen receptor antagonist

19h
Apurinic/apyrimidinic endonuclease 1 prevents oxidative DNA damage in intestinal epithelial cells induced by genotoxic Escherichia coli NC101. (PubMed, Redox Biol)
APE1 protects epithelial cells by inhibiting the accumulation of ROS and oxidative DNA damage induced by intestinal bacteria, including the colibactin produced by E. coli NC101.
Journal
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APEX1 (Apurinic/Apyrimidinic Endodeoxyribonuclease 1)
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tamoxifen
19h
Comprehensive CYP2D6 genotyping improves phenotype classification and highlights methodological pitfalls in tamoxifen-treated breast cancer. (PubMed, BMC Cancer)
Comprehensive CYP2D6 profiling improves phenotype assignment and highlights methodological pitfalls that may contribute to inconsistencies in pharmacogenetic studies. While no definitive association with clinical outcomes was observed in the overall cohort, these findings underscore the importance of analytically robust genotyping strategies and warrant validation in larger, prospectively designed cohorts, and highlight the importance of comprehensive genotyping strategies in resolving inconsistencies across pharmacogenetic studies.
Journal
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ER (Estrogen receptor)
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ER positive
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tamoxifen
22h
Proximal Tubule-Derived Semaphorin 3C Promotes Fibrosis in Adenine-Induced Tubulointerstitial Nephritis. (PubMed, Kidney360)
PT-derived SEMA3C promotes inflammation and fibrosis in adenine-induced tubulointerstitial nephritis.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • NDRG1 (N-Myc Downstream Regulated 1)
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tamoxifen
22h
Glucagon-Like Peptide-1 Receptor Agonists in Breast Cancer: Metabolic, Clinical, and Survivorship Implications. (PubMed, JCO Oncol Pract)
Available breast cancer-specific data are largely retrospective and suggest clinically meaningful but attenuated weight loss compared with pivotal obesity trials, with concurrent aromatase inhibitor or tamoxifen use associated with smaller reductions...Studies also suggest potential survivorship benefits relevant to lymphedema and cardio-oncology, although causality is unproven. Prospective cancer-specific trials and implementation studies are needed to define safety; optimal timing; patient selection; and effects on oncologic outcomes, function, and quality of life.
Journal
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ER (Estrogen receptor) • IGF1 (Insulin-like growth factor 1) • LEP (Leptin)
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ER positive
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tamoxifen
22h
The antiproliferative and antimigratory properties of the 3-biotin-B-norcholesteryl benzimidazole derivative in MCF-7 cells are mediated through G1 phase arrest and apoptosis. (PubMed, Steroids)
MTT and colony formation assays identified compound 1 as the most potent antiproliferative agent, with an IC50 of 6.53 μM in MCF-7 cells, which outperformed tamoxifen under identical experimental conditions...Taken together, these observations establish compound 1 as a promising antitumor lead scaffold for subsequent structural modification. Further investigations regarding its selectivity profile, systemic toxicity, pharmacokinetic properties, and in vivo therapeutic efficacy are therefore warranted.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MDM2 (E3 ubiquitin protein ligase) • ANXA5 (Annexin A5)
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tamoxifen
2d
Drug-Conjugated Tam-NHC-Gold(I) Complexes Overcome ESR1 Mutant Breast Cancer Resistance and Downregulate the RAMP3/CALCR Signaling Pathway. (PubMed, J Med Chem)
Herein, we developed drug-conjugated Tam-NHC-gold(I) complexes that can target breast cancer cells by the binding of tamoxifen (Tam) to the G protein-coupled estrogen receptor (GPER) present on cell membranes...Moreover, 7b exhibited potent antiproliferative activity on both wild-type and mutant MCF-7Y537S in xenograft mouse models with low toxicity. This study verified that 7b may offer a new approach for the treatment of endocrine-resistant breast cancer.
Journal
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ER (Estrogen receptor) • CALCR (Calcitonin Receptor 2)
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HR positive • ESR1 mutation
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tamoxifen
5d
Tailoring Oncofertility to Breast Cancer Subtype: A Systematic Review of Fertility Preservation Strategies in Premenopausal Women. (PubMed, Cancers (Basel))
Among studies with medium-term follow-up (3-5.5 years), no significant increase in recurrence or mortality attributable to FP was identified; long-term data beyond 5 years remain sparse. Substantial heterogeneity precluded meta-analysis; all synthesis is narrative. Standardized outco reporting and larger prospective subtype-stratified studies are required to establish precision oncofertility recommendations.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
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HER-2 positive • HR positive • HR negative
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tamoxifen • letrozole
6d
When Breast Cancer Meets the Uterus: A Quantitative Review of 105 Cases Spanning Four Decades. (PubMed, Medicina (Kaunas))
Invasive lobular carcinoma (ILC) demonstrates a documented predilection for unusual metastatic patterns including the female genital tract, while tamoxifen-associated endometrial pathology may complicate diagnosis in breast cancer survivors...Endometrial sampling should be considered with a low threshold in breast cancer survivors with abnormal uterine bleeding, and breast imaging is warranted when discohesive cells are encountered without a known breast primary. These proportions describe the published case literature rather than population-based prevalence; because the evidence is limited to case reports and small series, they should not be read as the true frequency of uterine involvement among women with breast cancer.
Review • Journal
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CDH1 (Cadherin 1) • GATA3 (GATA binding protein 3) • PAX8 (Paired box 8) • TRPS1 (Transcriptional Repressor GATA Binding 1)
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tamoxifen
7d
A novel ERα-targeted hydrophobic tag degrader, overcomes tamoxifen resistance via unfolded protein response-induced apoptosis and homologous recombination repair inhibition in breast cancer. (PubMed, Bioorg Chem)
We designed 20a, a novel ERα degrader based on the OBHSA scaffold with a hydrophobic amantadine tag. The latter effect creates synthetic lethality with Olaparib. Our findings elucidate the multi-mechanistic antitumor profile of 20a, highlighting its potential as a next-generation therapeutic for endocrine-resistant ERα-positive BC.
Journal
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • RAD51 (RAD51 Homolog A) • ATF4 (Activating Transcription Factor 4)
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ER positive
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Lynparza (olaparib) • tamoxifen
7d
The ESR1-MYH14 axis functions as a critical driver of cervical cancer progression and metastasis. (PubMed, Transl Oncol)
The ESR1-MYH14 signaling axis drives cervical cancer growth and metastasis. Targeting this pathway may represent a promising therapeutic strategy for cervical cancer management.
Journal
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ER (Estrogen receptor) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MMP9 (Matrix metallopeptidase 9)
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Etcamah (camizestrant)
10d
Evaluating the synergistic effects of cisplatin and tamoxifen in canine osteosarcoma cells. (PubMed, Front Vet Sci)
These findings suggest that tamoxifen enhances cisplatin-based combination therapy by promoting cell death in canine osteosarcoma at reduced drug concentrations. Combination therapies targeting estrogen-independent pathways may represent a promising strategy for improving treatment response in metastatic canine osteosarcoma and warrant further investigation.
Journal
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CCND1 (Cyclin D1)
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cisplatin • tamoxifen
14d
Does Next Generation Sequencing (NGS)-Based CYP2D6 Sequencing Improve Genotype-Phenotype Concordance in Tamoxifen-Treated Patients? (PubMed, Clin Pharmacol Ther)
and p.Pro264Thr) were identified and further evaluated using adapted in silico prediction strategies, compared with patients' phenotypes and published in vitro data. Comprehensive CYP2D6 sequencing improved gene profiling accuracy in our preselected cohort, while highlighting the remaining challenges of rare variant interpretation in pharmacogenetics-guided therapeutic drug monitoring.
Journal • Next-generation sequencing
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CYP2D6 (Cytochrome P450 Family 2 Subfamily D Member 6)
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tamoxifen