Safety, tolerability, and pharmacokinetics of TAS-108 in normal healthy post-menopausal female subjects: A phase I study on single oral dose

Journal of Clinical Pharmacy and Therapeutics

Volumn 30, Issue 5, 2005, Pages 459-470

  Yamaya, Hidetoshi ^a   Yoshida, K ^a   Kuritani, J ^a   Yonezawa, J I ^a   Tsuda, M ^a   Shindo, T ^a   Nagayama, S ^a   Buzdar, A U ^b  

^a TAIHO PHARMACEUTICAL CO LTD   (Japan)

^b UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

Author keywords

Anti oestrogen; Phase I pharmacokinetics; TAS 108

Indexed keywords

21 (4 DIETHYLAMINOMETHYL 2 METHOXYPHENOXY) 7ALPHA METHYL 19 NORPREGNA 1,3,5(10) TRIEN 3 OL; 7 ALPHA 21 [4 [(DIETHYLAMINO)METHYL] 2 METHOXYPHENOXY] 7 METHYL 19 NORPREGNA 1,3,5(10) TRIEN 3 OL 2 HYDROXY 1,2,3 PROPANETRICARBOXYLATE; STEROID; UNCLASSIFIED DRUG;

ADULT; AGED; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; FOOD INTAKE; HUMAN; LIPID DIET; MEAL; POSTMENOPAUSE;

ADULT; AGED; AREA UNDER CURVE; BLOOD SPECIMEN COLLECTION; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DOSE-RESPONSE RELATIONSHIP, DRUG; ESTRADIOL; FEMALE; FOOD-DRUG INTERACTIONS; HORMONES; HUMANS; MASS SPECTROMETRY; MIDDLE AGED; POSTMENOPAUSE; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 27744473143     PISSN: 02694727     EISSN: 13652710     Source Type: Journal    
DOI: 10.1111/j.1365-2710.2005.00673.x     Document Type: Article

References (26)

1. Jemal A, Murray T, Ward E et al. (2005) Cancer Statistics, 2005. CAA Cancer Journal for Clinicians, 55, 10-30.
2. Osbone CK, Elledge RM, Fuqua SAW (1996) Estrogen receptors in breast cancer therapy. Science and Medicine, 3, 32-41.
3. Early Breast Cancer Trialists' Collaborative Group (1992) Systemic treatment of early breast cancer by hormonal, cytotoxic, or immune therapy: 133 randomised trials involving 31000 recurrences and 24000 deaths among 75000 women. Lancet, 339, 71-85.
4. Early Breast Cancer Trialists' Collaborative Group (1998) Tamoxifen for early breast cancer: an overview of the randomised trials. Lancet, 351, 1451-1467.
5. Love RR, Mazess RB, Barden HS et al. (1992) Effects of tamoxifen on bone mineral density in postmenopausal women with breast cancer. New England Journal of Medicine, 326, 852-856.
6. Love RR, Newcomb PA, Wiebe DA, Surawicz TS, Jordan VC, Carbone PP, DeMets DL (1990) Effect of tamoxifen therapy on lipid and lipoprotein levels in postmenopausal patients with node-negative breast cancer. Journal of National Cancer Institute, 82, 1327-1332.
7. Bergman L, Beelen ML, Gallee MP, Hollema H, Benraadt J, van Leeuwen FE (2000) Risk and progression of endometrial cancer after tamoxifen for breast cancer. Lancet, 356, 881-887.
8. Lipton A, Harvey HA, Hamilton RW (1984) Venous thrombosis as a side effect of tamoxifen treatment. Cancer Treatment Reports, 68, 887-889.
9. Howell A, Dodwell DJ, Anderson H, Redford J (1992) Response after withdrawal of tamoxifen and progestogens in advanced breast cancer. Annals of Oncology, 3, 611-617.
10. Bonneterre J, Buzdar A, Nabholtz JM et al. (2001) Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor positive advanced breast carcinoma. Cancer, 92, 2247-2258.
11. Bonneterre J, Thurlimann B, Robertson JF et al. (2000) Anastrozole versus tamoxifen as first-line therapy for advanced breast cancer in 668 postmenopausal women: results of the Tamoxifen or Arimidex Randomized Group Efficacy and Tolerability Study. Journal of Clinical Oncology, 18, 3748-3757.
12. Nabholtz JM, Bonneterre J, Buzdar A, Robertson JF, Thurlimann B (2003) Anastrozole (Arimidex) versus tamoxifen as first-line therapy for advanced breast cancer in postmenopausal women: survival analysis and updated safety results. European Journal of Cancer, 39, 1684-1689.
13. Mouridsen H, Gershanovich M, Sun Y et al. (2003) Phase III study of letrozole versus tamoxifen as first-line therapy of advanced breast cancer in postmenopausal women: Analysis of survival and update of efficacy from the International Letrozole Breast Cancer Group. Journal of Clinical Oncology, 21, 2101-2109.
14. Mouridsen H, Gershanovich M, Sun Y et al. (2001) Superior efficacy of letrozole versus tamoxifen as first-line therapy for postmenopausal women with advanced breast cancer: results of a phase III study of the International Letrozole Breast Cancer Group. Journal of Clinical Oncology, 19, 2596-2606.
15. The ATAC Trialists' Group (2002) Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first results of the ATAC randomized trial. Lancet, 359, 2131-2139.
16. Goss PE, Ingle JN, Martino S et al. (2003) A randomized trial of letrozole in postmenopausal women after five years of tamoxifen therapy forearly-stage breast cancer. New England Journal of Medicine, 349, 1793-1802.
17. Coombes RC, Hall E, Gibson LJ et al. (2004) A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer. The New England Journal of Medicine, 350, 1081-1092.
18. Yamamoto Y, Wada O, Takada I et al. (2003) Both N- and C-terminal transactivation functions of DNA-bound ERalpha are blocked by a novel synthetic estrogen ligand. Biochemical and Biophysical Research Communications, 312, 656-662.
19. Yamamoto Y, Shibata J, Toko T et al. (2005) TAS-108, a novel steroidal anti-estrogenic agent, is a pure antagonist on ERα and a partial agonist on ERβ with low uterotrophic effect. Clinical Cancer Research, 11, 315-322.
20. Gibaldi M, Perrier D (1982) Pharmacokinetics, 2nd edn. New York: Marcel Dekker.
21. Snedecor GW, Cochran WG (1967) "One-way classifications. Analysis of variance," statistical methods, 6th edn. Ames, IA: The Iowa State University Press, 258-298.
22. Sokal RR, Rohlf FJ (1995) Biometry: the principles and practice of statistics in biological research, 3rd edn. San Francisco, CA: W.H. Freeman and Co., 440-444.
23. Blakely LJ, Buzdar A, Chang HY et al. (2004) A phase I and pharmacokinetic study of TAS-108 in post-menopausal female patients with locally advanced, locally recurrent inoperable, or progressive metastatic breast cancer. Clinical Cancer Research, 10, 5425-5431.
24. The ATAC Trialists' Group (2001) Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a subprotocol of the 'Arimidex™ and Tamoxifen Alone or in Combination' (ATAC) trial. British Journal of Cancer, 85, 317-324.
25. Evans TR, Di Salle E, Ornati G, Lassus M, Benedetti MS, Pianezzola E, Coombes RC (1992) Phase I and endocrine study of exemestane (FCE 24304), a new aromatase inhibitor, in postmenopausal women. Cancer Research, 52, 5933-5939.
26. Geisler J, Haynes B, Anker G, Dowsett M, Lonning PE (2002) Influence of letrozole and anastrozole on total Bbody aromatization and plasma estrogen levels in postmenopausal breast cancer patients evaluated in a randomized, cross-over study. Journal of Clinical Oncology, 20, 751-757.