酢酸アビラテロン

化学名:酢酸アビラテロン

英語名:Abiraterone acetate

CBNumberCB81396153

MFC26H33NO2

MW391.55

别名

酢酸アビラテロン

3β-17-(3-ピリジル)アンドロスタ-5,16-ジエン-3-オールアセタート

アビラテロンアセタート

酢酸アビラテロン物理性質

安全性情報

危険有害性情報のコード(GHS)

外観
白色～うすい黄色～うすい黄赤色粉末～結晶
効能
抗悪性腫瘍薬, アンドロゲン合成阻害薬
商品名
ザイティガ (ヤンセンファーマ)
説明
In April 2011, the United States FDA approved abiraterone acetate (CB7630) in combination with the steroid prednisone for the treatment of metastatic castration-resistant prostate cancer (mCRPC) for patients who were previously treated with a docetaxel containing regimen for late-stage disease. Abiraterone acetate affects prostate, testicular, and adrenal androgens by irreversibly inhibiting both the lyase and hydroxylase activity of cytochrome P450 17A (CYP17) signaling pathways (IC_50's of 2.9 and 4 nM, respectively) thereby decreasing testosterone levels.Most common serious adverse events for abiraterone acetate versus placebo included fluid retention (30.5% vs. 22.3%), hypokalemia (17.1% vs. 8.4%), hypertension (9.7% vs. 7.9%), hepatic transaminase abnormalities (10.4% vs. 8.1%), and cardiac abnormalities (13.3% vs. 10.4%).
化学的特性
Off-White Solid
使用
Abiraterone acetate is a novel steroidal inhibitor of human Cytochrome P450 (17α-Hydroxylase-C17,20-lyase): potential agent for the treatment of prostatic cancer.
定義
ChEBI: A sterol ester obtained by formal condensation of the 3-hydroxy group of abiraterone with the carboxy group of acetic acid. A prodrug that is converted in vivo to abiraterone. Used for treatment of metastatic castrate-resistant prostate cance .