Please use this identifier to cite or link to this item: https://doi.org/10.1002/ijc.26279
Title: Inecalcitol, an analog of 1α,25(OH) 2D 3, induces growth arrest of androgen-dependent prostate cancer cells
Authors: Okamoto, R.
Delansorne, R.
Wakimoto, N.
Doan, N.B.
Akagi, T.
Shen, M.
Ho, Q.H.
Said, J.W.
Koeffler, H.P. 
Keywords: antiproliferative effects
inecalcitol
prostate cancer
vitamin D
Issue Date: 15-May-2012
Citation: Okamoto, R., Delansorne, R., Wakimoto, N., Doan, N.B., Akagi, T., Shen, M., Ho, Q.H., Said, J.W., Koeffler, H.P. (2012-05-15). Inecalcitol, an analog of 1α,25(OH) 2D 3, induces growth arrest of androgen-dependent prostate cancer cells. International Journal of Cancer 130 (10) : 2464-2473. ScholarBank@NUS Repository. https://doi.org/10.1002/ijc.26279
Abstract: 19-nor-14-epi-23-yne-1,25(OH) 2D 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) 2D 3 in causing 50% clonal growth inhibition of androgen-sensitive human prostate cancer LNCaP cells. Inecalcitol, more than 1,25(OH) 2D 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) 2D 3 is 0.0625 μg/mouse; therefore, inecalcitol is 480 times less hypercalcemic than 1,25(OH) 2D 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. © 2011 UICC.
Source Title: International Journal of Cancer
URI: http://scholarbank.nus.edu.sg/handle/10635/125405
ISSN: 00207136
DOI: 10.1002/ijc.26279
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.

SCOPUSTM   
Citations

45
checked on Oct 15, 2021

WEB OF SCIENCETM
Citations

37
checked on Oct 15, 2021

Page view(s)

68
checked on Oct 14, 2021

Google ScholarTM

Check

Altmetric


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.