For research use only.
CAS No. 426219-18-3
TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.
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Choose Selective P450 (e.g. CYP17) Inhibitors
|Description||TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.|
In vitro, TAK-700 shows the potent inhibitory activity against rat and human steroid 17,20-lyase with IC50 of 54 nM and 38 nM, respectively. While other CYP isoforms including 11-hydroxylase and CYP3A4 are not significantly affected by TAK-700.  In microsomes expressing human CYP isoforms, TAK-700 exhibit greater inhibitory effects on 17,20-lyase with IC50 of 19 nM compared to the other CYP isoforms.  TAK-700 shows the inhibitory activity against monkey 17,20-lyase and 17-hydroxylase with IC50 of 27 nM and 38 nM, respectively.  In monkey adrenal cells, TAK-700 inhibits the ACTH stimulated production of DHEA and androstenedione with IC50 of 110 nM and 130 nM, respectively. Moreover, TAK-700 also potently inhibits DHEA production in human adrenocortical tumor line H295R cells with IC50 of 37 nM. 
|In vivo||In cynomolgus monkeys, oral treatment of TAK-700 at a dose of 1 mg/kg markedly reduces serum testosterone and dehydroepiandrosterone (DHEA) levels.  Oral treatment of TAK-700 at a dose of 1 mg/kg results in favorable pharmacokinetic parameters with Tmax, Cmax, t1/2 and AUC0-24 hours of 1.7 hours, 0.147 μg/mL, 3.8 hours and 0.727 μg h/mL, respectively. |
|In vitro||DMSO||61 mg/mL (198.47 mM)|
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|% DMSO % % Tween 80 % ddH2O|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01808040||Completed||Drug: TAK700||Post Menopausal Hormone Receptor Positive Breast Cancer||University of Wisconsin Madison|Millennium Pharmaceuticals Inc.||November 2012||Phase 1|
|NCT01666314||Completed||Drug: Orteronel|Drug: Orteronel Placebo|Drug: Prednisone||Prostate Cancer||Millennium Pharmaceuticals Inc.|Takeda||August 20 2012||Phase 1|Phase 2|
|NCT01549951||Completed||Drug: Orteronel+Prednisone||Prostate Cancer||Millennium Pharmaceuticals Inc.||May 2012||Phase 2|
|NCT01084655||Completed||Drug: TAK-700|Drug: Docetaxel|Drug: Prednisone||Prostate Cancer||Millennium Pharmaceuticals Inc.|Takeda||July 2010||Phase 1|Phase 2|
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