Tìm theo
Arsenic trioxide
Các tên gọi khác (11 ) :
  • Acide Arsenieux
  • Anhydride Arsenieux
  • Arseni Trioxydum
  • Arsenic Blanc
  • Arsenic Oxidearsenous Trioxide
  • Arsenigen Saure
  • Arsenious Acid
  • Arsenious Acid Anhydride
  • Arsenious Trioxide
  • Arsentrioxide
  • Oxyde Arsenieux
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 1327-53-3
ATC: L01XX27
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: As2O3
PTK: 197.8414
Arsenic trioxide is a chemotheraputic agent of idiopathic function used to treat leukemia that is unresponsive to first line agents. It is suspected that arsenic trisulfide induces cancer cells to undergo apoptosis. Due to the toxic nature of arsenic, this drug carries significant health risks. The enzyme thioredoxin reductase has recently been identified as a target for arsenic trioxide.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
As2O3
Phân tử khối
197.8414
Monoisotopic mass
197.8279367
InChI
InChI=1S/As2O3/c3-1-4-2(3)5-1
InChI Key
InChIKey=GOLCXWYRSKYTSP-UHFFFAOYSA-N
IUPAC Name
bicyclo[1.1.1]diarsoxane
Traditional IUPAC Name
arsenic trioxide
SMILES
O1[As]2O[As]1O2
Độ hòa tan
1.7E+004 mg/L (at 16 °C)
logP
2.31
pKa (Strongest Basic)
-5.2
PSA
27.69 Å2
Refractivity
4.05 m3·mol-1
Polarizability
7.14 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Arsenic Trioxide is indicated for induction of remission and consolidation in patients with acute promyelocytic leukemia (APL) who are refractory to, or have relapsed from, retinoid and anthracycline chemotherapy.
Cơ Chế Tác Dụng : Arsenic trioxide is a chemotheraputic agent of idiopathic function used to treat leukemia that is unresponsive to first line agents. It is suspected that arsenic trisulfide induces cancer cells to undergo apoptosis. Due to the toxic nature of arsenic, this drug carries significant health risks. The enzyme thioredoxin reductase has recently been identified as a target for arsenic trioxide. The mechanism of action of Arsenic Trioxide is not completely understood. Arsenic trioxide causes morphological changes and DNA fragmentation characteristic of apoptosis in NB4 human promyelocytic leukemia cells in vitro. Arsenic trioxide also causes damage or degradation of the fusion protein PML/RAR-alpha. It is suspected that arsenic trioxide induces cancer cells to undergo apoptosis.
Dược Động Học :

▧ Protein binding :
75% bound
▧ Metabolism :
The metabolism of arsenic trioxide involves reduction of pentavalent arsenic to trivalent arsenic by arsenate reductase and methylation of trivalent arsenic to monomethylarsonic acid and monomethylarsonic acid to dimethylarsinic acid by methyltransferases. The main site of methylation reactions appears to be the liver. Arsenic is stored mainly in liver, kidney, heart, lung, hair and nails.
▧ Route of Elimination :
Trivalent arsenic is mostly methylated in humans and excreted in urine.
Độc Tính : Symptoms of overdose include convulsions, muscle weakness and confusion.
Chỉ Định : For induction of remission and consolidation in patients with acute promyelocytic leukemia (APL), and whose APL is characterized by the presence of the t(15;17) translocation or PML/RAR-alpha gene expression
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Quinupristin This combination presents an increased risk of toxicity
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Trisenox
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01169
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=518740
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506448
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02106
ChemSpider
http://www.chemspider.com/Chemical-Structure.452539.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/63459-600-10
PharmGKB
http://www.pharmgkb.org/drug/PA448486
Wikipedia
http://en.wikipedia.org/wiki/Arsenic_trioxide
RxList
http://www.rxlist.com/cgi/generic2/arsenic.htm
Drugs.com
http://www.drugs.com/cdi/arsenic.html
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