TAK-700 (Orteronel) selectively inhibits the enzyme CYP17A1 which is expressed in testicular, adrenal, and prostatic tumor tissues. 17,20-Lyase inhibition by orteronel was tolerable and results in declines in PSA and testosterone, with evidence of radiographic responses.
|Animal models||Adult male cynomolgus monkeys.|
|Formulation||TAK-700 is dissolved in 0.5% methylcellulose.|
|Administration||Administered via p.o.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥60 mg/mL
Ethanol ≥60 mg/mL
Phase I/II trial of orteronel (TAK-700)--an investigational 17,20-lyase inhibitor--in patients with metastatic castration-resistant prostate cancer.
Dreicer R, et al. Clin Cancer Res. 2014 Mar 1;20(5):1335-44. PMID: 24418642.
|Related Androgen Receptor Products|
MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
Dehydroepiandrosterone is an effective antiapoptotic factor.
ASC-J9, also known as GO-Y025 and Dimethylcurcumin, suppressesing castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia. GSK 2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.
Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.