ArticleInternational journal of cancer2012
Inecalcitol, an analog of 1α,25(OH)(2) D(3) , induces growth arrest of androgen-dependent prostate cancer cells.
Article in International journal of cancer, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 53 citations in OpenAlex.
- Synthetic Modulators of the Vitamin D Receptor: From Structural Innovation to Disease-Specific Applications.Biomolecules · 2026Review
- Regulation of infant gut microbiota and metabolic pathways by human milk oligosaccharides: a multi-omics investigation.RSC advances · 2026Article
- Exploring the Molecular Mechanism of 1,25(OH)Current issues in molecular biology · 2025Article
- Vitamin D in Cancer Prevention and Treatment: A Review of Epidemiological, Preclinical, and Cellular Studies.Cancers · 2024Review
- Biological evaluation of combinations of tyrosine kinase inhibitors with Inecalcitol as novel treatments for human chronic myeloid leukemia.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Article
- First Experimental Quantitative Charge Density Studies of Advanced Intermediate of Vitamin D Analogues.Molecules (Basel, Switzerland) · 2022Article
- Differential Response of Lung Cancer Cells, with Various Driver Mutations, to Plant Polyphenol Resveratrol and Vitamin D Active Metabolite PRI-2191.International journal of molecular sciences · 2021Article
- New Roles for Vitamin D Superagonists: From COVID to Cancer.Frontiers in endocrinology · 2021Review
- Vitamin D Signaling in Inflammation and Cancer: Molecular Mechanisms and Therapeutic Implications.Molecules (Basel, Switzerland) · 2020Review
- 1,25(OH)2D3 Attenuates IL-1β-Induced Epithelial-to-Mesenchymal Transition Through Inhibiting the Expression of lncTCF7.Oncology research · 2019Article
- Repurposing vitamin D for treatment of human malignanciesActa pharmaceutica Sinica. B · 2019Review
- Calcitriol and cancer therapy: A missed opportunity.Bone reports · 2018Article
- Article
- Antiangiogenic cancer treatment: The great discovery and greater complexity (Review).International journal of oncology · 2016Review
- The Use of 1α,25-Dihydroxyvitamin D₃ as an Anticancer Agent.International journal of molecular sciences · 2016Review
- Vitamin D and urological cancers.Central European journal of urology · 2016Review
- [Prostate cancer prophylaxis by dietary supplements: more than just an illusion?].Der Urologe. Ausg. A · 2014Review
- The future of vitamin D analogs.Frontiers in physiology · 2014Review
- Vitamin D and cancer.Cell cycle (Georgetown, Tex.) · 2013Article
- Inecalcitol, an analog of 1,25D3, displays enhanced antitumor activity through the induction of apoptosis in a squamous cell carcinoma model system.Cell cycle (Georgetown, Tex.) · 2013Article
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
Abstract
19-nor-14-epi-23-yne-1,25(OH)(2) D(3) (inecalcitol) is a unique vitamin D(3) analog. We evaluated the activity of inecalcitol in a human prostate cancer model system. The analog was 11-fold more potent than 1,25(OH)(2) D(3) in causing 50% clonal growth inhibition of androgen-sensitive human prostate cancer LNCaP cells. Inecalcitol, more than 1,25(OH)(2) D(3) , reduced in a dose-dependent manner the expression levels of the transcription factor ETS variant 1 and the serine/threonine protein kinase Pim-1, both of which are upregulated in prostate cancer. Remarkably, dose challenge experiments revealed that inecalcitol maximal tolerated dose (MTD) by intraperitoneal (i.p.) administration was 30 μg/mouse (1,300 μg/kg) three times per week, while we previously found that the MTD of 1,25(OH)(2) D(3) is 0.0625 μg/mouse; therefore, inecalcitol is 480 times less hypercalcemic than 1,25(OH)(2) D(3) . Pharmacokinetic studies showed that plasma half-life of inecalcitol were 18.3 min in mice. A xenograft model of LNCaP cells was developed in immunodeficient mice treated with inecalcitol. The tumors of the diluent-treated control mice increased in size but those in the inecalcitol treatment group did not grow. Our data suggest that inecalcitol inhibits androgen-responsive prostate cancer growth in vivo and should be examined either alone or with other chemotherapy in clinical trials in individuals with rising serum prostate-specific antigen after receiving either surgery or irradiation therapy with curative intent.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.