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DRUG CLASS:

Estrogen receptor antagonist

1d
TAM-01 L_FU: Long-term Follow-up of the TAM-01 Study (clinicaltrials.gov)
P=N/A, N=500, Not yet recruiting, Ente Ospedaliero Ospedali Galliera | Initiation date: Oct 2025 --> Jun 2026
Trial initiation date
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tamoxifen
1d
Pharmacodynamics of Camizestrant Treatment in Postmenopausal Women With Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Primary Breast Cancer: Results From the Randomized, Presurgical SERENA-3 Study. (PubMed, J Clin Oncol)
SERENA-3 demonstrates that camizestrant 75 mg once daily (Phase III dose) is well-tolerated and achieves maximal reduction in ER through known mechanisms, that is, antagonism and degradation, by 5-7 days, and proliferation suppression determined by Ki67 expression, by 12-15 days. These data support camizestrant 75 mg once daily as the preferred dose for ongoing clinical development and highlight the importance of presurgical WOO studies in guiding dose selection.
PK/PD data • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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ER positive • HER-2 negative • EGFR positive
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camizestrant (AZD9833)
1d
Pharmacotherapeutic considerations of selective estrogen receptor modulators for vascular protection. (PubMed, Front Pharmacol)
Among the most studied SERMs are Tamoxifen and Raloxifene. The pharmacological profile of SERMs therefore reflects a delicate equilibrium between receptor-mediated vascular protection and thrombotic liability. Indeed, their raison d'être increasingly extends beyond oncology into cardiovascular endocrine pharmacology, where they serve as prototypes for designing next-generation agents with optimized receptor selectivity and safer vascular outcomes.
Review • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • NOS3 (Nitric oxide synthase 3)
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tamoxifen • raloxifene hydrochloride
5d
Integrative analysis of EMT-driving genes identifies a prognostic signature and GJB2 as a potential biomarker in glioblastoma. (PubMed, Front Cell Dev Biol)
Drug sensitivity analyses suggested that high-risk GBM may respond better to paclitaxel and tamoxifen. Random Forest modeling and in vitro experiments identified GJB2 as an oncogenic driver that promotes GBM cell proliferation and migration. Our findings provide a clinically applicable EMT-based prognostic framework that links transcriptional plasticity to patient outcomes in GBM and identify GJB2 as a promising therapeutic target.
Journal
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MGMT (6-O-methylguanine-DNA methyltransferase)
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MGMT promoter methylation
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paclitaxel • tamoxifen
5d
Prospective Single-Arm Study of Endocrine Therapies With Ovarian Function Suppression in Premenopausal Node-Positive Early Breast Cancer Patients With Low Genomic Risk (INTERSTELLAR Trial, KBCSG-25). (PubMed, J Breast Cancer)
Our results may establish evidence supporting the omission of adjuvant chemotherapy in premenopausal women with low genomic risk scores and limited nodal involvement (p-N1), potentially reducing treatment-related morbidity while preserving comparable oncologic outcomes.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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tamoxifen
5d
Optimizing dose selection in oncology: the rationale for the clinical dose selection of giredestrant, an oral selective estrogen receptor degrader. (PubMed, Expert Opin Investig Drugs)
Data were leveraged from preclinical and phase I/II studies in metastatic and early breast cancer, as a single agent and with palbociclib, to inform giredestrant dose selection. Our learnings challenge the MTD paradigm in drug development, particularly in targeted therapies, and demonstrate the importance of basing dose selection on the totality of evidence, including preclinical data, and may help inform the clinical development of future targeted therapies.
Journal
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ER (Estrogen receptor)
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ER positive
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Ibrance (palbociclib) • giredestrant (RG6171)
6d
DHCR7 drives AML development through the IL6/JAK2/STAT3 signalling pathway. (PubMed, Br J Haematol)
In vitro functional assays demonstrated that either DHCR7 knockdown or treatment with the targeted inhibitor tamoxifen significantly suppressed AML cell proliferation...Mechanistic investigations further revealed that DHCR7 exerts pro-leukaemic effects through activation of the IL-6/JAK2/STAT3 signalling axis. Collectively, this study establishes the novel function of DHCR7 in AML pathogenesis and provides robust evidence supporting its potential as a therapeutic target for AML.
Journal
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IL6 (Interleukin 6) • DHCR7 (7-Dehydrocholesterol Reductase)
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tamoxifen
6d
Early Diagnosis of Male Breast Cancer: A Case Report and Literature Review. (PubMed, Cureus)
Oncotype diagnosis (DX) testing indicated a low chemotherapy benefit, leading to adjuvant therapy with tamoxifen...The prompt detection of the suspicious mass, culminating in effective early-stage treatment, proved crucial to this patient's favorable prognosis, in contrast to the common trend of delayed diagnoses and their less promising outcomes. Accordingly, strengthening public awareness and professional training is essential to optimize management and improve outcomes in men with breast cancer.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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Oncotype DX Breast Recurrence Score®Test
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tamoxifen
6d
SERENA-1: Study of AZD9833 Alone or in Combination in Women With Advanced Breast Cancer. (clinicaltrials.gov)
P1, N=396, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2026 --> Jun 2027
Trial completion date • First-in-human
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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HER-2 negative
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Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • Truqap (capivasertib) • anastrozole • camizestrant (AZD9833)
6d
EZH2 directs HER2+ breast cancer progression through the modulation of epithelial plasticity. (PubMed, EMBO Rep)
Further, inhibition of EZH2 in vitro resulted in increased expression of ER in HER2+ human breast cancer cell lines and conferred sensitivity to Tamoxifen. These findings demonstrate that EZH2 dictates cancer plasticity and provides rationale for combining EZH2 inhibitors with endocrine therapies to improve HER2+ breast cancer outcomes.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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HER-2 expression
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tamoxifen
7d
The Crosstalk Mechanism of EGFR and ER in EGFR-Mutant Lung Adenocarcinoma. (PubMed, Cells)
Furthermore, coadministration of tamoxifen and the EGFR TKI gefitinib potentially inhibited p-EGFR expression in EGFR-mutant lung adenocarcinoma. Regular follow-up with chest computed tomography is recommended for patients with breast cancer. For those diagnosed with both ER-positive breast cancer and EGFR-mutant lung adenocarcinoma, combined tamoxifen and EGFR TKI therapy may offer an effective targeted treatment strategy.
Journal
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EGFR (Epidermal growth factor receptor) • ER (Estrogen receptor)
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ER positive • EGFR mutation
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gefitinib • tamoxifen
7d
Real-World Clinical Experience of First-Line Ribociclib Combined with an Aromatase Inhibitor in Metastatic Breast Cancer. (PubMed, Cancers (Basel))
The results in terms of PFS and AEs are consistent with those of pivotal studies and real clinical practice data, but a direct comparison is not possible due to differences in patient populations. Ribociclib once again demonstrated efficacy in all patient subgroups and remains the gold standard, alongside ET, for first-line HR+/HER2-negative mBC.
Journal • Real-world evidence
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HER-2 (Human epidermal growth factor receptor 2) • CDK4 (Cyclin-dependent kinase 4)
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HER-2 negative
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tamoxifen • Kisqali (ribociclib)