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DRUG:

ormeloxifene

Associations
Trials
Company:
Generic mfg.
Drug class:
Selective estrogen receptor modulator
Associations
Trials
4ms
Evaluation of molecular effects associated with apoptosis, tumour progression, angiogenesis and metastasis by a novel combination of drugs with ormeloxifene in triple negative breast cancer cells. (PubMed, Explor Target Antitumor Ther)
To investigate the molecular effects of a novel combination [sertraline and plumbagin (comb) with ormeloxifene (Orm)] for anticancer activity in triple negative breast cancer cell line "MDA-MB-231". Collectively this study reveals the efficacy of Orm + comb as more significant than the clinically used tamoxifen (Tam). The study elucidates the promising novelty of the combination as a potential chemotherapeutic intervention for mitigating the aggressiveness of triple negative breast cancer and it addresses the intrinsic resistance caused by single drug treatments.
Journal
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TP53 (Tumor protein P53) • CASP3 (Caspase 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • ZEB1 (Zinc Finger E-box Binding Homeobox 1) • ANXA5 (Annexin A5)
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tamoxifen • ormeloxifene
1year
Synthesis and Antitumor Activity of Brominated-Ormeloxifene (Br-ORM) against Cervical Cancer. (PubMed, ACS Omega)
Consequently, Br-ORM treatment effectively inhibited tumor growth in an orthotopic cervical cancer xenograft mouse model along with EMT associated changes as compared to vehicle control-treated mice. Altogether, experimental findings suggest that Br-ORM is a novel, promising β-catenin inhibitor and therefore can be harnessed as a potent anticancer small molecule for cervical cancer treatment.
Journal • PARP Biomarker
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CDH1 (Cadherin 1) • MMP2 (Matrix metallopeptidase 2) • VIM (Vimentin) • CDH2 (Cadherin 2) • MMP9 (Matrix metallopeptidase 9)
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VIM expression
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ormeloxifene
over1year
Ormeloxifene, a nonsteroidal antifertility drug promotes megakaryocyte differentiation in leukemia cell line K562. (PubMed, Cell Biol Int)
Because induction of megakaryocytic differentiation in K562 involves growth arrest and exit from cell cycle, we also observed an increase in levels of p21 and p27 with decrease in c-Myc protein levels in K562 cells treated with 7.5 µM ORM for 24 and 48 h, respectively. Taken together, these findings indicate that ORM can markedly induce megakaryocytic differentiation in K562 cells.
Preclinical • Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • GATA1 (GATA Binding Protein 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • ITGA2B (Integrin Subunit Alpha 2b)
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ormeloxifene
over1year
Molecular mechanism of ormeloxifene mediated chemo-sensitivity in hepatocellular carcinoma (AACR 2023)
Background: Hepatocellular carcinoma (HCC) is a lethal cancer with a dismal 5-year survival rate as the standard therapy available Sorafenib (SRB), is only effective in extending survival for a subset of patients. Taken together, ORM displayed an effective chemo-therapeutic and chemo-sensitizing agents in treatment of hepatocellular carcinoma.
IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • MCL1 (Myeloid cell leukemia 1) • BCL2L1 (BCL2-like 1) • VIM (Vimentin) • CDH2 (Cadherin 2) • ANXA5 (Annexin A5)
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MCL1 expression • CDH1 expression • VIM expression
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sorafenib • ormeloxifene