Tìm theo
Deferasirox
Các tên gọi khác (4 ) :
  • Deferasiroxum
  • Exjade
  • ICL 670
  • ICL 670a
iron chelating agents
Thuốc Gốc
Small Molecule
CAS: 201530-41-8
ATC: V03AC03
ĐG : Novartis AG , http://www.novartis.com
CTHH: C21H15N3O4
PTK: 373.3615
Deferasirox is an oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved in the USA for this purpose.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H15N3O4
Phân tử khối
373.3615
Monoisotopic mass
373.106255983
InChI
InChI=1S/C21H15N3O4/c25-17-7-3-1-5-15(17)19-22-20(16-6-2-4-8-18(16)26)24(23-19)14-11-9-13(10-12-14)21(27)28/h1-12,25-26H,(H,27,28)
InChI Key
InChIKey=BOFQWVMAQOTZIW-UHFFFAOYSA-N
IUPAC Name
4-[bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid
Traditional IUPAC Name
exjade
SMILES
OC(=O)C1=CC=C(C=C1)N1N=C(N=C1C1=CC=CC=C1O)C1=CC=CC=C1O
Độ tan chảy
116-117 °C
Độ hòa tan
0.038 mg/mL at 37 °C
logP
3.52
logS
-4
pKa (strongest acidic)
4.55
pKa (Strongest Basic)
0.19
PSA
108.47 Å2
Refractivity
125.32 m3·mol-1
Polarizability
38.52 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
6
H Bond Donor Count
3
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Deferasirox is an orally active chelator that is selective for iron (as Fe3+). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain.
Cơ Chế Tác Dụng : Deferasirox is an oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved in the USA for this purpose. Two molecules of deferasirox are capable of binding to 1 atom of iron. Deferasirox works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming a stable complex which is eliminated via the kidneys.
Dược Động Học :
▧ Absorption :
The absolute bioavailability (AUC) of deferasirox tablets for oral suspension is 70% compared to an intravenous dose.
▧ Volume of Distribution :
* 14.37 ± 2.69 L
▧ Protein binding :
Deferasirox is highly (~99%) protein bound almost exclusively to serum albumin.
▧ Metabolism :
Hepatic. CYP450-catalyzed (oxidative) metabolism of deferasirox appears to be minor in humans (about 8%). Glucuronidation is the main metabolic pathway for deferasirox, with subsequent biliary excretion.
▧ Route of Elimination :
Deferasirox and metabolites are primarily (84% of the dose) excreted in the feces. Renal excretion of deferasirox and metabolites is minimal (8% of the administered dose).
▧ Half Life :
The mean elimination half-life ranged from 8 to 16 hours following oral administration.
Chỉ Định : For the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.
Tương Tác Thuốc :
  • Aluminium Possible physicochemical interaction
  • Bivalirudin Anticoagulants increase the risk for gastrointestinal ulceration/irritation and/or GI bleeding. If these two agents must be used, patients need to be closely monitored for signs and symptoms of GI toxicity.
  • Etravirine Etravirine, when administered concomitantly with deferasirox, may experience a decrease in serum concentration. It is recommended to monitor therapy.
  • Tofacitinib Tofacitinib (and other CYP3A4 substrates), when used in combination with deferasirox, may experience a decrease in concentration. It is recommended to monitor therapy.
Liều Lượng & Cách Dùng : Tablet, for suspension - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Exjade 125 mg tablet
    Giá bán buôn : USD >19.65
    Đơn vị tính : tablet
  • Biệt dược thương mại : Exjade 250 mg tablet
    Giá bán buôn : USD >39.3
    Đơn vị tính : tablet
  • Biệt dược thương mại : Exjade 500 mg tablet
    Giá bán buôn : USD >78.61
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Exjade
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01609
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5493381
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506791
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03669
ChemSpider
http://www.chemspider.com/Chemical-Structure.4591431.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0468-15
PharmGKB
http://www.pharmgkb.org/drug/PA164760843
Wikipedia
http://en.wikipedia.org/wiki/Deferasirox
RxList
http://www.rxlist.com/cgi/generic/exjade.htm
Drugs.com
http://www.drugs.com/cdi/deferasirox.html
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