Tìm theo
Anastrozole
Các tên gọi khác (2) :
  • alpha,alpha,Alpha',alpha'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-m-benzenediacetonitrile
  • Anastrozol
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 120511-73-1
ATC: L02BG03
ĐG : Accord Healthcare , http://www.accord-healthcare.com
CTHH: C17H19N5
PTK: 293.3663
Anastrozole is a drug indicated in the treatment of breast cancer in post-menopausal women. It is used both in adjuvant therapy (i.e. following surgery) and in metastatic breast cancer. It decreases the amount of estrogens that the body makes. Anastrozole belongs in the class of drugs known as aromatase inhibitors. It inhibits the enzyme aromatase, which is responsible for converting androgens (produced by women in the adrenal glands) to estrogens.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19N5
Phân tử khối
293.3663
Monoisotopic mass
293.164045633
InChI
InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3
InChI Key
InChIKey=YBBLVLTVTVSKRW-UHFFFAOYSA-N
IUPAC Name
2-[3-(1-cyano-1-methylethyl)-5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile
Traditional IUPAC Name
anastrozole
SMILES
CC(C)(C#N)C1=CC(=CC(CN2C=NC=N2)=C1)C(C)(C)C#N
Độ tan chảy
130.14 °C
Độ hòa tan
0.5 mg/mL
logP
2.4
logS
-3.6
pKa (Strongest Basic)
2.25
PSA
78.29 Å2
Refractivity
97.47 m3·mol-1
Polarizability
31.97 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Anastrozole is a potent and selective non-steroidal aromatase inhibitor indicated for the treatment of advanced breast cancer in post-menopausal women with disease progression following tamoxifen therapy. Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogens. In post-menopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues, such as adipose tissue, with further conversion of estrone to estradiol. Many breast cancers also contain aromatase; the importance of tumor-generated estrogens is uncertain. Treatment of breast cancer has included efforts to decrease estrogen levels by ovariectomy premenopausally and by use of anti-estrogens and progestational agents both pre- and post-menopausally, and these interventions lead to decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
Cơ Chế Tác Dụng : Anastrozole is a drug indicated in the treatment of breast cancer in post-menopausal women. It is used both in adjuvant therapy (i.e. following surgery) and in metastatic breast cancer. It decreases the amount of estrogens that the body makes. Anastrozole belongs in the class of drugs known as aromatase inhibitors. It inhibits the enzyme aromatase, which is responsible for converting androgens (produced by women in the adrenal glands) to estrogens. Anastrozole selectively inhibits aromatase. The principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues. Therefore, aromatase inhibition leads to a decrease in serum and tumor concentration of estrogen, leading to a decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole has no detectable effect on synthesis of adrenal corticosteroids, aldosterone, and thyroid hormone.
Dược Động Học :
▧ Absorption :
Rapidly absorbed into the systemic cirulation following oral administration. Peak plasma concentrations are usually attained within 2 hours under fasting conditions, with steady-state plasma concentrations attained in approximately 7 days.
▧ Protein binding :
40%
▧ Metabolism :
Hepatic. Metabolized mainly by N-dealkylation, hydroxylation, and glucuronidation to inactive metabolites. Primary metabolite is an inactive triazole.
▧ Route of Elimination :
Hepatic metabolism accounts for approximately 85% of anastrozole elimination. Renal elimination accounts for approximately 10% of total clearance.
▧ Half Life :
50 hours
Độc Tính : In rats, lethality is greater than 100 mg/kg.
Chỉ Định : For adjuvant treatment of hormone receptor positive breast cancer , as well as hormonal treatment of advanced breast cancer in post-menopausal women. Has also been used to treat pubertal gynecomastia and McCune-Albright syndrome; however, manufacturer states that efficacy for these indications have not been established.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Aromasin 25 mg tablet
    Giá bán buôn : USD >14.04
    Đơn vị tính : tablet
  • Biệt dược thương mại : Arimidex 1 mg tablet
    Giá bán buôn : USD >15.3
    Đơn vị tính : tablet
  • Biệt dược thương mại : Anastrozole 100% powder
    Giá bán buôn : USD >1326.52
    Đơn vị tính : g
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Anastrole
  • Công ty :
    Sản phẩm biệt dược : Arimidex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01217
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2187
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504987
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08159
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00960
ChemSpider
http://www.chemspider.com/Chemical-Structure.2102.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10015
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0310-0201-30
PharmGKB
http://www.pharmgkb.org/drug/PA448432
Wikipedia
http://en.wikipedia.org/wiki/Anastrozole
RxList
http://www.rxlist.com/cgi/generic2/anastr.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ari1028.shtml
Drugs.com
http://www.drugs.com/cdi/anastrozole.html
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