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药品详细

Nilutamide(尼鲁米特)

化学结构式图
中文名
尼鲁米特
英文名
Nilutamide
分子式
C12H10F3N3O4
化学名
5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]imidazolidine-2,4-dione
分子量
Average: 317.2207
Monoisotopic: 317.062340438
CAS号
63612-50-0
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

Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin that 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.

生产厂家
  • Sanofi aventis us llc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Kassouf W, Tanguay S, Aprikian AG: Nilutamide as second line hormone therapy for prostate cancer after androgen ablation fails. J Urol. 2003 May;169(5):1742-4. Pubmed
  2. Lukka H, Waldron T, Klotz L, Winquist E, Trachtenberg J: Maximal androgen blockade for the treatment of metastatic prostate cancer—a systematic review. Curr Oncol. 2006 Jun;13(3):81-93. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Nitrobenzenes
Substructures
  • Nitrobenzenes
  • Oxoazaniums
  • Amino Ketones
  • Halogen Derivatives
  • Benzene and Derivatives
  • Ureas and Derivatives
  • Nitro compounds
  • Imidazolidines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Carboxylic Acids and Derivatives
  • Anilines
适应症
药理
Indication For use in combination with surgical castration for the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (Stage D2).
Pharmacodynamics Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin that 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. The relative binding affinity of nilutamide at the androgen receptor is less than that of bicalutamide, but similar to that of hydroxuflutamide.
Mechanism of action Nilutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin that stimulate the growth of normal and malignant prostatic tissue. This blockade of androgen receptors may result in growth arrest or transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis.
Absorption Rapidly and completely absorbed, yielding high and persistent plasma concentrations.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
The results of a human metabolism study using 14C-radiolabelled tablets show that nilutamide is extensively metabolized and less than 2% of the drug is excreted unchanged in urine after 5 days.
Route of elimination Nilutamide is extensively metabolized andless than 2% of the drug is excreted unchanged in urine after 5 days. Fecal elimination is negligible, ranging from 1.4% to 7% of the dose after 4 to 5 days.
Half life 38.0-59.1 hours
Clearance Not Available
Toxicity Symptoms of overdose include dizziness, general discomfort, headache, nausea, and vomiting.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 1.8 Not Available
Predicted Properties
Property Value Source
water solubility 4.19e-03 g/l ALOGPS
logP 1.74 ALOGPS
logP 2.25 ChemAxon
logS -4.9 ALOGPS
pKa (strongest acidic) 15.01 ChemAxon
pKa (strongest basic) -4.4 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 95.23 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 68.23 ChemAxon
polarizability 25.88 ChemAxon
药物相互作用
Drug Interaction
Ticlopidine Ticlopidine may decrease the metabolism and clearance of Nilutamide. Consider alternate therapy or monitor for adverse/toxic effects of Nilutamide if Ticlopidine is initiated, discontinued or dose changed.
食物相互作用
  • Avoid alcohol.
  • Take before breakfast.

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