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Xenobiotica
the fate of foreign compounds in biological systems
Volume 14, 1984 - Issue 11
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Original Article

Disposition and metabolism of a new benzothiophene antiestrogen in rats, dogs and monkeys

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Pages 841-847 | Received 26 Jul 1983, Published online: 30 Sep 2009

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Khaled Greish, Hayley Nehoff, Fatemah Bahman, Tara Pritchard & Sebastien Taurin. (2019) Raloxifene nano-micelles effect on triple-negative breast cancer is mediated through estrogen receptor-β and epidermal growth factor receptor. Journal of Drug Targeting 27:8, pages 903-916.
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Takako Furukawa, Yoichi Naritomi, Kazuhiro Tetsuka, Fumihiro Nakamori, Hiroyuki Moriguchi, Katsuhiro Yamano, Shigeyuki Terashita, Kenji Tabata & Toshio Teramura. (2014) Species differences in intestinal glucuronidation activities between humans, rats, dogs and monkeys. Xenobiotica 44:3, pages 205-216.
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Satya Prakash Tripathi, Anuseema Bhadauriya, Abhijeet Patil & Abhay T. Sangamwar. (2013) Substrate selectivity of human intestinal UDP-glucuronosyltransferases (UGTs): in silico and in vitro insights. Drug Metabolism Reviews 45:2, pages 231-252.
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Takako Furukawa, Katsuhiro Yamano, Yoichi Naritomi, Kohichiro Tanaka, Shigeyuki Terashita & Toshio Teramura. (2012) Method for predicting human intestinal first-pass metabolism of UGT substrate compounds. Xenobiotica 42:10, pages 980-988.
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A. Chandrasekaran, S. Ahmad, L. Shen, W. DeMaio, T. Hultin & J. Scatina. (2010) Disposition of bazedoxifene in rats. Xenobiotica 40:8, pages 578-585.
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Muhammad Mohsin Ansari, Dang-Khoa Vo, Ho-Ik Choi, Jeong-Su Ryu, Yumi Bae, Nadeem Irfan Bukhari, Alam Zeb, Jin-Ki Kim & Han-Joo Maeng. (2023) Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability. Pharmaceutics 15:8, pages 2073.
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Ting Du, Rongjin Sun, Imoh Etim, Zicong Zheng, Dong Liang, Ming Hu & Song Gao. (2021) Age-and Region-Dependent Disposition of Raloxifene in Rats. Pharmaceutical Research 38:8, pages 1357-1367.
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Rašković Aleksandar, Paut Kusturica Milica, Mitić Gorana, Milijašević Boris, Stojšić-Milosavljević Anastazija, Lalić-Popović Mladena, Stević Snežana, Stilinović Nebojša & Gigov Slobodan. (2021) Interaction between apigenin and sodium deoxycholate with raloxifene: A potential risk for clinical practice. European Journal of Pharmaceutical Sciences 161, pages 105809.
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Shiyan Chen, Karl Austin-Muttitt, Linghua Harris Zhang, Jonathan G. L. Mullins & Aik Jiang Lau. (2019) In Vitro and In Silico Analyses of the Inhibition of Human Aldehyde Oxidase by Bazedoxifene, Lasofoxifene, and Structural Analogues. Journal of Pharmacology and Experimental Therapeutics 371:1, pages 75-86.
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Robyn Meech, Dong Gui Hu, Ross A. McKinnon, Siti Nurul Mubarokah, Alex Z. Haines, Pramod C. Nair, Andrew Rowland & Peter I. Mackenzie. (2019) The UDP-Glycosyltransferase (UGT) Superfamily: New Members, New Functions, and Novel Paradigms. Physiological Reviews 99:2, pages 1153-1222.
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Punna Rao Ravi, N. Aditya, Himanshu Kathuria, Srinivas Malekar & Rahul Vats. (2014) Lipid nanoparticles for oral delivery of raloxifene: Optimization, stability, in vivo evaluation and uptake mechanism. European Journal of Pharmaceutics and Biopharmaceutics 87:1, pages 114-124.
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Angela Wehr. 2014. Handbook of Metabolic Pathways of Xenobiotics. Handbook of Metabolic Pathways of Xenobiotics 1 4 .
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Takako Furukawa, Fumihiro Nakamori, Kazuhiro Tetsuka, Yoichi Naritomi, Hiroyuki Moriguchi, Katsuhiro Yamano, Shigeyuki Terashita & Toshio Teramura. (2012) Quantitative Prediction of Intestinal Glucuronidation of Drugs in Rats Using In Vitro Metabolic Clearance Data. Drug Metabolism and Pharmacokinetics 27:2, pages 171-180.
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Kim Henriksen, Claus Christiansen & Morten Asser Karsdal. (2011) Serological biochemical markers of surrogate efficacy and safety as a novel approach to drug repositioning. Drug Discovery Today 16:21-22, pages 967-975.
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Keigo Kosaka, Norifumi Sakai, Yuya Endo, Yuga Fukuhara, Minoru Tsuda-Tsukimoto, Tatsuyuki Ohtsuka, Ichiro Kino, Tomohiko Tanimoto, Naomi Takeba, Masakatsu Takahashi & Toshiyuki Kume. (2011) Impact of Intestinal Glucuronidation on the Pharmacokinetics of Raloxifene. Drug Metabolism and Disposition 39:9, pages 1495-1502.
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Yan Chen, Xiaobin Jia, Jian Chen, Jinyan Wang & Ming Hu. (2010) The Pharmacokinetics of Raloxifene and Its Interaction with Apigenin in Rat. Molecules 15:11, pages 8478-8487.
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Ae Ra Kim, Soo-Jeong Lim & Beom-Jin Lee. (2009) Metabolic inhibition and kinetics of raloxifene by pharmaceutical excipients in human liver microsomes. International Journal of Pharmaceutics 368:1-2, pages 37-44.
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Deepak Dalvie, Ping Kang, Michael Zientek, Cathie Xiang, Sue Zhou & R. Scott Obach. (2008) Effect of Intestinal Glucuronidation in Limiting Hepatic Exposure and Bioactivation of Raloxifene in Humans and Rats. Chemical Research in Toxicology 21:12, pages 2260-2271.
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Susie Y. Dai, Michael J. Chalmers, John Bruning, Kelli S. Bramlett, Harold E. Osborne, Chahrzad Montrose-Rafizadeh, Robert J. Barr, Yong Wang, Minmin Wang, Thomas P. Burris, Jeffrey A. Dodge & Patrick R. Griffin. (2008) Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method. Proceedings of the National Academy of Sciences 105:20, pages 7171-7176.
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Zhaoyong Yang, Xiaobo He & Yueqin Zhang. (2007) The determination of raloxifene in rat tissue using HPLC. Biomedical Chromatography 21:3, pages 229-233.
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Zh. Y. Yang, Zh. F. Zhang, X. B. He, G. Y. Zhao & Y. Q. Zhang. (2006) Validation of a Novel HPLC Method for the Determination of Raloxifene and Its Pharmacokinetics in Rat Plasma. Chromatographia 65:3-4, pages 197-201.
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Gregory T. Wurz, Karla C. Read, Cristina Marchisano-Karpman, Jeffrey P. Gregg, Laurel A. Beckett, Qilu Yu & Michael W. DeGregorio. (2005) Ospemifene inhibits the growth of dimethylbenzanthracene-induced mammary tumors in Sencar mice. The Journal of Steroid Biochemistry and Molecular Biology 97:3, pages 230-240.
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Eun Ju Jeong, Yong Liu, Huimin Lin & Ming Hu. (2005) SPECIES- AND DISPOSITION MODEL-DEPENDENT METABOLISM OF RALOXIFENE IN GUT AND LIVER: ROLE OF UGT1A10. Drug Metabolism and Disposition 33:6, pages 785-794.
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David Czock, Frieder Keller, Mette Heringa & Franz Maximilian Rasche. (2005) Raloxifene pharmacokinetics in males with normal and impaired renal function. British Journal of Clinical Pharmacology 59:4, pages 479-482.
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E. J. Jeong. (2004) Disposition Mechanisms of Raloxifene in the Human Intestinal Caco-2 Model. Journal of Pharmacology and Experimental Therapeutics 310:1, pages 376-385.
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Valeria N Rubin, Peter C Ruenitz, F.Douglas Boudinot & Jason L Boyd. (2001) Identification of new triarylethylene oxyalkanoic acid analogues as bone selective estrogen mimetics. Bioorganic & Medicinal Chemistry 9:6, pages 1579-1587.
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Antonino Saitta, Nunziate Morabito, Nicola Frisina, Domenico Cucinotte, Francesco Corrado, Rosario D'Anna, Domenica Altavilla, Giovanni Squadrito, Letteria Minutoli, Vincenzo Arcoraci, Francesco Cancellieri & Francesco Squadrito. (2006) Cardiovascular Effects of Raloxifene Hydrochloride. Cardiovascular Drug Reviews 19:1, pages 57-74.
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E.A. Lien & P.E. Lønning. (2000) Selective oestrogen receptor modifiers (SERMs) and breast cancer therapy. Cancer Treatment Reviews 26:3, pages 205-227.
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Jeffrey A. Dodge, Charles W. Lugar, Stephen Cho, John J. Osborne, David L. Phillips, Andrew L. Glasebrook & Charles A. Frolik. (1997) Synthesis and estrogen receptor binding affinities of the major human metabolites of raloxifene (LY139481). Bioorganic & Medicinal Chemistry Letters 7:8, pages 993-996.
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Jeffrey A. Dodge, Charles W. Lugar, Stephen Cho, Lorri L. Short, Masahiko Sato, Na N. Yang, Larry A. Spangle, Michael J. Martin, David L. Phillips, Andrew L. Glasebrook, John J. Osborne, Charles A. Frolik & Henry U. Bryant. (1997) Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity. The Journal of Steroid Biochemistry and Molecular Biology 61:1-2, pages 97-106.
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Michael J. Martin, Timothy A. Grese, Andrew L. Glasebrook, Ken Matsumoto, Lewis D. Pennington, D.Lynn Phillips & Lorri L. Short. (1997) Versatile raloxifene triflates. Bioorganic & Medicinal Chemistry Letters 7:7, pages 887-892.
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