Abstract
Tamoxifen is currently the standard hormonal treatment of breast cancer, both for metastatic disease and in the adjuvant setting. A new antiestrogen, toremifene, was approved recently for use in managing metastatic breast cancer in postmenopausal women. Toremifene is structurally similar to tamoxifen, differing only by a single chlorine atom, and has a similar pharmacologic profile. The major difference between the two compounds is in the preclinical activity; chronic, high-dose tamoxifen is hepatocarcinogenic in the rat, whereas toremifene is not. Neither agent is hepatocarcinogenic in mice, hamsters, or humans; therefore, clinical relevance of the rat data may not be significant. In a worldwide phase III trial, the two agents demonstrated comparable efficacy and safety against metastatic breast cancer. Both agents have shown a significant hypocholesterolemic effect after long-term administration. Due to the paucity of long-term clinical data on toremifene, important unresolved questions remain, which include its effects on bone mineral density, the frequency of cardiac events, and the risk for endometrial cancer. Tamoxifen has been associated with maintenance of bone mineral density, a reduction in cardiac events, and a sligh...Continue Reading
Citations
Jun 5, 1998·Journal of Women's Health·W D Schlaff
Jun 14, 2000·Breast Cancer Research and Treatment·U Hellmann-BlumbergM W DeGregorio
Mar 23, 2001·Breast Cancer Research and Treatment·A Milla-SantosV Solano
Apr 12, 2002·Acta Obstetricia Et Gynecologica Scandinavica·Oronzo CeciRaffaella Di Venere
Jan 25, 2002·Annals of the New York Academy of Sciences·B K Dunn, B Kramer
Nov 25, 2003·Pharmacology & Toxicology·Hanna MäenpääHanna Tähti
Nov 30, 2004·Clinical Journal of Oncology Nursing·Patty Gerken
Apr 9, 2005·Cancer Investigation·Nigel Bundred
Jun 1, 2006·Cancer Science·Masamichi HashibaMasakuni Degawa
Apr 24, 2009·Climacteric : the Journal of the International Menopause Society·A Nath, R Sitruk-Ware
Jan 15, 2010·International Journal of Cancer. Journal International Du Cancer·Y R Santosh LaxmiShinya Shibutani
Sep 9, 2010·International Journal of Cancer. Journal International Du Cancer·Naomi SuzukiShinya Shibutani
Jul 23, 2013·PloS One·Karin Tamm-RosensteinMadis Metsis
Apr 27, 2019·Frontiers in Surgery·Hakan Kulacoglu, Ferdinand Köckerling
Nov 13, 2002·Pharmacology & Toxicology·Hanna MäenpääHanna Tähti
Dec 7, 2000·Clinical Pharmacokinetics·T L TarasM W DeGregorio
Jul 20, 1999·Current Opinion in Rheumatology·G WeryhaJ Leclère
Mar 7, 2014·Cytotechnology·Serkan YilmazEbru Yilmaz
Feb 24, 2000·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·A Gadducci, A R Genazzani
Nov 15, 2007·Reproductive Sciences·Sussane C J P GielenCurt W Burger
Apr 20, 2004·British Journal of Cancer·I Vergote, J F R Robertson
Jul 9, 2004·Drug Metabolism Reviews·Sung Yeon KimShinya Shibutani
Dec 22, 1999·Acta Oncologica·A BoströmJ Bergh
Nov 5, 1999·Current Opinion in Oncology·A C Wolff
Sep 13, 2012·Breast Cancer : the Journal of the Japanese Breast Cancer Society·Morihiko KimuraNobuoki Eshima
Jun 10, 2016·Molecular Diversity·M S R MurtyR S Prakasham
Mar 22, 2012·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Vineetha Koroth EdavanaSusan Kadlubar
Jan 25, 2002·Annals of the New York Academy of Sciences·M AnthonyB K Dunn
Nov 23, 2006·Journal of Interferon & Cytokine Research : the Official Journal of the International Society for Interferon and Cytokine Research·Snehal G ThakkarErnest C Borden
Sep 27, 2000·Annals of Surgical Oncology·L A NewmanS E Singletary
Feb 7, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Basappa BasappaVijay Pandey
Nov 23, 2006·Arquivos brasileiros de endocrinologia e metabologia·Adolfo Diez-Perez
Mar 21, 2006·Chemical Research in Toxicology·Atsushi UmemotoShinya Shibutani
Jun 20, 2006·Chemical Research in Toxicology·Sung Yeon KimShinya Shibutani
Mar 25, 2000·Surgical Oncology·N K Ibrahim, G N Hortobagyi
Dec 18, 2001·Chemical Research in Toxicology·D YaoJ L Bolton
Feb 19, 2011·Critical Reviews in Oncology/hematology·Nagi S El SaghirAhmad Awada