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DRUG CLASS:

Estrogen receptor agonist

21h
MAP4 phosphorylation induced by ARID1A loss sensitizes colorectal cancer cells to EMP. (PubMed, Cell Death Dis)
Here, we performed a synthetic lethal drug screening in an approved drug library with ARID1A isogenic CRC cell lines and identified estramustine phosphate sodium (EMP), an FDA approved antimicrotubule chemotherapy drug, as a synthetic lethal partner of ARID1A...Furthermore, we identified that MAP4 is phosphorylated by PI3K, which is activated by ARID1A loss. These findings highlight MAP4 as a key regulator of microtubule dynamics in ARID1A-deficient cells and unveil a novel synthetic lethality relationship between ARID1A and EMP.
Journal
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ARID1A (AT-rich interaction domain 1A) • MAP4 (Microtubule Associated Protein 4) • PI3K (Phosphoinositide 3-kinases)
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ARID1A mutation
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Emcyt (estramustine)
24h
An Ethno-bridging Study of Pergoveris in Healthy Premenopausal Participants of Japanese or Caucasian Origin (clinicaltrials.gov)
P1, N=24, Recruiting, Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany
New P1 trial
5d
Estradiol in Treating Patients With ER Beta Positive, Triple Negative Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
P2, N=5, Active, not recruiting, Mayo Clinic | Trial completion date: Jul 2026 --> Dec 2026
Trial completion date
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HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • PGR (Progesterone receptor)
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HER-2 negative
18d
Enrollment change
25d
Estrogen Supplementation and Bone Health in Women With CF (clinicaltrials.gov)
P4, N=75, Recruiting, Johns Hopkins University | Trial completion date: Dec 2025 --> Jan 2027 | Trial primary completion date: Dec 2025 --> Jan 2027
Trial completion date • Trial primary completion date
29d
Estrogen Hormone Products (clinicaltrials.gov)
P1, N=8, Completed, University of Maryland, Baltimore | Recruiting --> Completed | N=12 --> 8
Trial completion • Enrollment change
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Divigel (estradiol)
1m
Hormonal Status on Blood Flow and Tissue in Pelvic Organ Prolapse (clinicaltrials.gov)
P4, N=7, Terminated, The University of Texas Medical Branch, Galveston | N=10 --> 7
Enrollment change
2ms
Clinical outcomes of different 17β-estradiol drug regimens and their impact on endometrial receptivity. (PubMed, Front Endocrinol (Lausanne))
Subjects were divided into three groups based on different estrogen formulations and administration routes: Group A [oral Estradiol Valerate Tablets (Progynova)], Group B (oral M17EH), and Group C (oral combined with vaginal M17EH)...For Groups B and C, endometrial tissue samples were collected five days after progesterone conversion...In FET cycles, a HRT regimen combining oral and vaginal administration of Micronized 17-beta estradiol hemihydrate is more conducive to endometrial growth. Although vaginal administration results in higher estrogen levels, it does not appear to compromise endometrial receptivity.
Clinical data • Retrospective data • Journal
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MUC1 (Mucin 1) • LIF (LIF Interleukin 6 Family Cytokine)
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estradiol valerate
2ms
Surgical Myomectomy Followed by Oral Myfembree Versus Standard of Care Trial (SOUL) (clinicaltrials.gov)
P4, N=0, Withdrawn, University of Chicago | N=136 --> 0 | Terminated --> Withdrawn
Enrollment change • Trial withdrawal
2ms
Mechanism of Tiaogeng decoction in a cognitive dysfunction mouse model. (PubMed, J Tradit Chin Med)
TG may improve memory ability while reducing oxidative stress and apoptosis. It also reduces Aβ protein deposition in the hippocampus, protecting the central nervous system and improving memory function. TG may reduce the risk of AD.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2) • HMOX1 (Heme Oxygenase 1) • APP (Amyloid Beta Precursor Protein) • CASP9 (Caspase 9) • MAPK8 (Mitogen-activated protein kinase 8)
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estradiol valerate
3ms
Trial initiation date
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CCL3 (C-C Motif Chemokine Ligand 3)
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Orgovyx (relugolix)
3ms
Enrollment change • Trial withdrawal