药品详细

Bicalutamide(比卡鲁胺)

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

比卡鲁胺

英文名

Bicalutamide

分子式

C₁₈H₁₄F₄N₂O₄S

化学名

N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorobenzene)sulfonyl]-2-hydroxy-2-methylpropanamide

分子量

Average: 430.373
Monoisotopic: 430.061040456

CAS号

90357-06-5

ATC分类

L02B 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

Bicalutamide is an oral non-steroidal anti-androgen for prostate cancer. It binds to the androgen receptor.

生产厂家

Accord healthcare inc usa
Actavis totowa llc
Astrazeneca uk ltd
Fresenius kabi oncology plc
Kudco ireland ltd
Mylan pharmaceuticals inc
Sandoz inc
Sun pharma global inc
Synthon pharmaceuticals inc
Teva pharmaceuticals usa inc
Zydus pharmaceuticals usa inc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Acetanilides

Substructures

Hydroxy Compounds
Amino Ketones
Nitriles and Derivatives
Sulfonyls
Benzene and Derivatives
Acetanilides
Carboxylic Acids and Derivatives
Cyanides
Alcohols and Polyols
Sulfones
Halobenzenes
Aromatic compounds
Carboxamides and Derivatives
Aryl Halides
Anilines
Sulfoxides

适应症

药理

Indication	For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer.
Pharmacodynamics	Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration.
Mechanism of action	Bicalutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.
Absorption	Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown.
Volume of distribution	Not Available
Protein binding	96%
Metabolism	Bicalutamide undergoes stereo specific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation.
Route of elimination	Not Available
Half life	5.9 days
Clearance	Apparent oral cl=0.32 L/h [Normal Males]
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	191-193 °C	Not Available
water solubility	5 mg/L	Not Available
logP	2.5	Not Available
pKa	12.0	Not Available

Predicted Properties

Property	Value	Source
water solubility	9.28e-03 g/l	ALOGPS
logP	2.7	ALOGPS
logP	2.71	ChemAxon
logS	-4.7	ALOGPS
pKa (strongest acidic)	11.95	ChemAxon
pKa (strongest basic)	-4	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	5	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	107.26	ChemAxon
rotatable bond count	6	ChemAxon
refractivity	96.59	ChemAxon
polarizability	36.68	ChemAxon

药物相互作用

Drug	Interaction
Budesonide	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of budesonide. The clinical significance of this interaction is greater for oral budesonide than for orally inhaled budesonide. Consider reducing the oral budesonide dose when used together with a CYP3A4 inhibitor.
Colchicine	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of colchicine. Increase monitoring for colchicine-related toxicity when using such combinations. Use extra caution in patients with impaired renal and/or hepatic function.
Eplerenone	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of eplerenone. A lower starting dose of eplerenone (25 mg once daily) is recommended in patients with hypertension who are also taking drugs that are moderate inhibitors of CYP3A4.
Everolimus	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of everolimus. Consider therapy modification. Recommendations regarding optimal management of this interaction vary according to specific indication and product used.
Fentanyl	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of fentanyl. The risk of prolonged adverse effects, including potentially fatal respiratory depression is increased. Consider therapy modification.
Halofantrine	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of halofantrine. Extreme caution, with possibly increased monitoring of cardiac status (e.g., ECG), should be used with concurrent use of halofantrine with any moderate CYP3A4 inhibitor(s).
Lurasidone	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of lurasidone. Limit adult lurasidone dose to 40 mg/day in patients receiving a moderate CYP3A4 inhibitor.
Ranolazine	CYP3A4 inhibitors like ranolazine may increase the serum concentration of ranolazine. Consider therapy modification.
Tolvaptan	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of tolvaptan. This combination is contraindicated.

食物相互作用

Take without regard to meals, at the same time everyday.

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