药品详细

Trilostane(曲洛司坦)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

曲洛司坦

英文名

Trilostane

分子式

C₂₀H₂₇NO₃

化学名

(1S,2R,6R,8S,11S,12S,15S,16S)-5,15-dihydroxy-2,16-dimethyl-7-oxapentacyclo[9.7.0.0^{2,8}.0^{6,8}.0^{12,16}]octadec-4-ene-4-carbonitrile

分子量

Average: 329.4333
Monoisotopic: 329.199093735

CAS号

13647-35-3

ATC分类

H02C 未知

药物类型

small molecule

阶段

approved, withdrawn

商品名

同义名

基本介绍

Trilostane is an inhibitor of 3 beta-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome. It was withdrawn from the United States market in April 1994. [Wikipedia]

生产厂家

Bioenvision inc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Komanicky P, Spark RF, Melby JC: Treatment of Cushing’s syndrome with trilostane (WIN 24,540), an inhibitor of adrenal steroid biosynthesis. J Clin Endocrinol Metab. 1978 Nov;47(5):1042-51. Pubmed

剂型

规格

化合物类型

Type	small molecule

Classes

Steroids and Steroid Derivatives

Substructures

Glycerol and Derivatives
Hydroxy Compounds
Nitriles and Derivatives
Ethers
Cyanides
Heterocyclic compounds
Steroids and Steroid Derivatives
Alcohols and Polyols
Cyclohexenes and Derivatives
Epoxides
Enols

适应症

药理

Indication	Used in the treatment of Cushing's syndrome. It is normally used in short-term treatment until permanent therapy is possible.
Pharmacodynamics	Trilostane blocks an enzyme involved in the production of several steroids including cortisol. Inhibiting this enzyme inhibits the production of cortisol. In Cushing's syndrome, the adrenal gland overproduces steroids. Although steroids are important for various functions of the body, too much can cause problems. Trilostane reduces the amount of steroids produced by the adrenal gland. This product was withdrawn from the U.S. market in April 1994.
Mechanism of action	Trilostane produces suppression of the adrenal cortex by inhibiting enzymatic conversion of steroids by 3-beta-hydroxysteroid dehydrogenase/delta 5,4 ketosteroid isomerase, thus blocking synthesis of adrenal steroids.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Hepatic.
Route of elimination	Not Available
Half life	8 hours.
Clearance	Not Available
Toxicity	Symptoms of overdose include darkening of skin, drowsiness or tiredness, loss of appetite, mental depression, skin rash, and/or vomiting.
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	264 dec °C	PhysProp
logP	3	Not Available

Predicted Properties

Property	Value	Source
water solubility	5.93e-02 g/l	ALOGPS
logP	2.41	ALOGPS
logP	2.3	ChemAxon
logS	-3.8	ALOGPS
pKa (strongest acidic)	5.23	ChemAxon
pKa (strongest basic)	-0.88	ChemAxon
physiological charge	-1	ChemAxon
hydrogen acceptor count	4	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	76.78	ChemAxon
rotatable bond count	0	ChemAxon
refractivity	90.17	ChemAxon
polarizability	36.96	ChemAxon

药物相互作用

食物相互作用

Not Available

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