Land: Taiwan
Sprog: kinesisk
Kilde: 衛生福利部食品藥物管理署 (Ministry of Health and Welfare, Food And Drug Administration)
VORINOSTAT
美商默沙東藥廠股份有限公司台灣分公司 台北市信義區信義路五段106號12樓 (86683720)
L01XH01
膠囊劑
VORINOSTAT (1000000400) MG
塑膠瓶裝
製 劑
須由醫師處方使用
MERCK SHARP & DOHME CORP 4633 MERCK ROAD, WILSON, NORTH CAROLINA 27893, U.S.A. US
vorinostat
經兩種全身性治療後仍出現進行性、持續性或復發性疾病表現之皮膚T細胞淋巴瘤(CTCL)患者的皮膚病灶(cutaneous manifestations)
註銷日期: 2018/05/02; 註銷理由: 自請註銷; 有效日期: 2020/07/06; 英文品名: ZOLINZA Capsules
已註銷
2010-07-06
CAPSULES ZOLINZA™ (VORINOSTAT, MSD) DESCRIPTION ZOLINZA 1 contains vorinostat, which is described chemically as _N-_hydroxy-_N'-_phenyloctanediamide. The empirical formula is C 14 H 20 N 2 O 3 . The molecular weight is 264.32 and the structural formula is: N H H N O O OH Vorinostat is a white to light orange powder. It is very slightly soluble in water, slightly soluble in ethanol, isopropanol and acetone, freely soluble in dimethyl sulfoxide and insoluble in methylene chloride. It has no chiral centers and is non-hygroscopic. The differential scanning calorimetry ranged from 161.7 (endotherm) to 163.9°C. The pH of saturated water solutions of vorinostat drug substance was 6.6. The pKa of vorinostat was determined to be 9.2. Each 100 mg ZOLINZA capsule for oral administration contains 100 mg vorinostat and the following inactive ingredients: microcrystalline cellulose, sodium croscarmellose and magnesium stearate. The capsule shell excipients are titanium dioxide, gelatin and sodium lauryl sulfate. CLINICAL PHARMACOLOGY MECHANISM OF ACTION Vorinostat inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II) at nanomolar concentrations (IC 50 <86 nM). These enzymes catalyze the removal of acetyl groups from the lysine residues of proteins, including histones and transcription factors. In some cancer cells, there is an overexpression of HDACs, or an aberrant recruitment of HDACs to oncogenic transcription factors causing hypoacetylation of core nucleosomal histones. Hypoacetylation of histones is associated with a condensed chromatin structure and repression of gene transcription. Inhibition of HDAC activity allows for the accumulation of acetyl groups on the histone lysine residues resulting in an open chromatin structure and transcriptional activation. _In vitro_, vorinostat causes the accumulation of acetylated histones and induces cell cycle arrest and/or apoptosis of some transformed cells. The mechanism of the antineoplastic effect of vorinostat has not b Læs hele dokumentet