Tìm theo
Nilutamide
Các tên gọi khác (5 ) :
  • 5,5-Dimethyl-3-(alpha,alpha,alpha-trifluoro-4-nitro-m-tolyl)hydantoin
  • Nilandron
  • Nilutamida
  • Nilutamide
  • Nilutamidum
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 63612-50-0
ATC: L02BB02
ĐG : Sanofi-Aventis Inc. , http://www.sanofi-aventis.com
CTHH: C12H10F3N3O4
PTK: 317.2207
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H10F3N3O4
Phân tử khối
317.2207
Monoisotopic mass
317.062340438
InChI
InChI=1S/C12H10F3N3O4/c1-11(2)9(19)17(10(20)16-11)6-3-4-8(18(21)22)7(5-6)12(13,14)15/h3-5H,1-2H3,(H,16,20)
InChI Key
InChIKey=XWXYUMMDTVBTOU-UHFFFAOYSA-N
IUPAC Name
5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]imidazolidine-2,4-dione
Traditional IUPAC Name
nilutamide
SMILES
CC1(C)NC(=O)N(C1=O)C1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F
Độ hòa tan
4.19e-03 g/l
logP
1.8
logS
-4.9
pKa (strongest acidic)
15.01
pKa (Strongest Basic)
-4.4
PSA
95.23 Å2
Refractivity
68.23 m3·mol-1
Polarizability
25.88 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ Absorption :
Rapidly and completely absorbed, yielding high and persistent plasma concentrations.
▧ 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
Độc Tính : Symptoms of overdose include dizziness, general discomfort, headache, nausea, and vomiting.
Chỉ Định : For use in combination with surgical castration for the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (Stage D2).
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Anandron
  • Công ty :
    Sản phẩm biệt dược : Nilandron
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00665
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4493
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505381
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08164
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00965
ChemSpider
http://www.chemspider.com/Chemical-Structure.4337.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0088-1111-14
PharmGKB
http://www.pharmgkb.org/drug/PA450632
Wikipedia
http://en.wikipedia.org/wiki/Nilutamide
RxList
http://www.rxlist.com/cgi/generic2/nilutam.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/nil1294.shtml
Drugs.com
http://www.drugs.com/cdi/nilutamide.html
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