Affiliation: Pharmaceutical Research Division
- Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeysMasuo Yamaoka
Oncology Drug Discovery Unit, Takeda Pharmaceutical Company Limited, Fujisawa, Japan
J Steroid Biochem Mol Biol 129:115-28. 2012..These findings suggest that orteronel may be an effective therapeutic option for diseases where androgen suppression is critical, such as androgen sensitive and CRPC...
- Overcoming persistent dependency on androgen signaling after progression to castration-resistant prostate cancerMasuo Yamaoka
Takeda Pharmaceutical Company Limited, Tsukuba, Japan
Clin Cancer Res 16:4319-24. 2010..The study of circulating tumor cells will likely be important not only to identify patients likely to receive benefit from this therapeutic approach, but also to further understand the molecular mechanisms of resistance...
- Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancerTomohiro Kaku
CNS Drug Discovery Unit, Takeda Pharmaceutical Company, Ltd, Shonan Research Center, 26 1, Muraoka Higashi 2 chome, Fujisawa, Kanagawa 251 0012, Japan
Bioorg Med Chem 19:6383-99. 2011..Therefore, (+)-3c (termed orteronel [TAK-700]) was selected as a candidate for clinical evaluation and is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer...
- Effect of a novel 17,20-lyase inhibitor, orteronel (TAK-700), on androgen synthesis in male ratsTakahito Hara
Oncology Drug Discovery Unit, Takeda Pharmaceutical Company Ltd, Fujisawa, Japan
J Steroid Biochem Mol Biol 134:80-91. 2013..Our data suggests that orteronel would therefore be effective for androgen-dependent disorders such as PC...
- Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonistsSatoshi Yamamoto
Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, 26 1, Muraokahigashi 2 Chome, Fujisawa, Kanagawa 251 8555, Japan
Bioorg Med Chem 20:2338-52. 2012..These results suggest that the novel pyrazole derivatives are new-generation AR antagonists, different from the 'first-generation' antagonists such as bicalutamide in a CRPC treatment model...
- Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonistsSatoshi Yamamoto
Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, 26 1 Muraokahigashi 2 chome, Fujisawa, Kanagawa 251 8555, Japan
Bioorg Med Chem 20:422-34. 2012....
- A mutation in beta-tubulin and a sustained dependence on androgen receptor signalling in a newly established docetaxel-resistant prostate cancer cell lineTakahito Hara
Pharmacology Research Laboratories, Takeda Pharmaceutical Company Limited, Tsukuba, Japan
Cell Biol Int 34:177-84. 2010..These results suggest that an acquired mutation in beta-tubulin is associated with docetaxel resistance in PC and that a novel AR-targeted therapy is effective for docetaxel-resistant PC...
- C(17,20)-lyase inhibitors. Part 2: design, synthesis and structure-activity relationships of (2-naphthylmethyl)-1H-imidazoles as novel C(17,20)-lyase inhibitorsNobuyuki Matsunaga
Medicinal Chemistry Research Laboratories, Pharmaceutical Research Division Takeda Chemical Industries Ltd, 17 85, Jusohonmachi 2 chome, Yodogawa ku, Osaka 532 8686, Japan
Bioorg Med Chem 12:4313-36. 2004..Furthermore, (S)-42 showed a potent suppression of testosterone biosynthesis after a single oral administration in monkeys. These data suggest that (S)-42 may be a promising agent for the treatment of androgen-dependent prostate cancer...
- Enhanced androgen receptor signaling correlates with the androgen-refractory growth in a newly established MDA PCa 2b-hr human prostate cancer cell sublineTakahito Hara
Pharmacology Research Laboratories I, Takeda Chemical Industries, Ltd, Osaka 532 8686, Japan
Cancer Res 63:5622-8. 2003....
- Possible role of adaptive mutation in resistance to antiandrogen in prostate cancer cellsTakahito Hara
Pharmacology Research Laboratories I, Takeda Pharmaceutical Company Limited, 17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka, Japan
Prostate 65:268-75. 2005..CONCLUSIONS: These results suggest the hypermutational state might occur in LNCaP-FGC cells during bicalutamide-treatment, which might create the W741C/L mutant AR leading to bicalutamide-resistance...