容立莎膠囊

国家: 台湾

语言: 中文

来源: 衛生福利部食品藥物管理署 (Ministry of Health and Welfare, Food And Drug Administration)

有效成分:

VORINOSTAT

可用日期:

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)

ATC代码:

L01XH01

药物剂型:

膠囊劑

组成:

VORINOSTAT (1000000400) MG

每包单位数:

塑膠瓶裝

类:

製　劑

处方类型:

須由醫師處方使用

厂商:

MERCK SHARP & DOHME CORP 4633 MERCK ROAD, WILSON, NORTH CAROLINA 27893, U.S.A. US

治疗领域:

vorinostat

疗效迹象:

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）

產品總結:

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

授权状态:

已註銷

授权日期:

2010-07-06

资料单张

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