Tìm theo
Fludarabine
Các tên gọi khác (11 ) :
  • 2-Fluoro-ara AMP
  • 2-Fluoroadenine arabinoside 5'-monophosphate
  • 2F-Ara-AMP
  • 9-beta-Arabinofuranosyl-2-fluoroadenine-5'-phosphate
  • 9-beta-D-Arabinofuranosyl-2-fluoroadenine 5'-(dihydrogen phosphate)
  • 9-beta-D-Arabinofuranosyl-2-fluoroadenine 5'-monophosphate
  • FAMP
  • Fludara
  • Fludarabine 5'-monophosphate
  • Fludarabine monophosphate
  • Fludarabine phosphate
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 75607-67-9
ATC: L01BB05
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C10H13FN5O7P
PTK: 365.2117
Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a chemotherapy drug used in the treatment of hematological malignancies. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H13FN5O7P
Phân tử khối
365.2117
Monoisotopic mass
365.053662512
InChI
InChI=1S/C10H13FN5O7P/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(18)5(17)3(23-9)1-22-24(19,20)21/h2-3,5-6,9,17-18H,1H2,(H2,12,14,15)(H2,19,20,21)/t3-,5-,6+,9-/m1/s1
InChI Key
InChIKey=GIUYCYHIANZCFB-FJFJXFQQSA-N
IUPAC Name
{[(2R,3S,4S,5R)-5-(6-amino-2-fluoro-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}phosphonic acid
Traditional IUPAC Name
[(2R,3S,4S,5R)-5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxyphosphonic acid
SMILES
NC1=C2N=CN([C@@H]3O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]3O)C2=NC(F)=N1
Độ tan chảy
260 °C
Độ hòa tan
3.53 mg/ml
logP
-2.8
logS
-2.1
pKa (strongest acidic)
1.34
pKa (Strongest Basic)
0.6
PSA
186.07 Å2
Refractivity
74.93 m3·mol-1
Polarizability
28.88 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
10
H Bond Donor Count
5
Physiological Charge
-2
Number of Rings
3
Bioavailability
1
Rule of Five
true
Dược Lực Học : Fludarabine is a chemotherapy drug used in the treatment of chronic lymphocytic leukemia. It acts at DNA polymerase alpha, ribonucleotide reductase and DNA primase, results in the inhibition of DNA synthesis, and destroys the cancer cells.
Cơ Chế Tác Dụng : Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a chemotherapy drug used in the treatment of hematological malignancies. [Wikipedia] Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis. The mechanism of action of this antimetabolite is not completely characterized and may be multi-faceted.
Dược Động Học :
▧ Absorption :
Bioavailability is 55% following oral administration.
▧ Protein binding :
19-29%
▧ Half Life :
20 hours
▧ Clearance :
* 117-145 mL/min [patients with B-cell CLL receiving IV administration of a single dose of 40 mg/m2]
Chỉ Định : For the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to or whose disease has progressed during treatment with at least one standard alkylating-agent containing regimen
Tương Tác Thuốc :
  • Dipyridamole Dipyridamole may decrease the effect of fludarabine.
  • Pentostatin Unacceptable pulmonary toxicity
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Oforta 10 mg tablet
    Giá bán buôn : USD >92.57
    Đơn vị tính : tablet
  • Biệt dược thương mại : Fludarabine 50 mg vial
    Giá bán buôn : USD >240.0
    Đơn vị tính : vial
  • Biệt dược thương mại : Fludara 50 mg vial
    Giá bán buôn : USD >367.02
    Đơn vị tính : vial
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Fludara
  • Công ty :
    Sản phẩm biệt dược : Fludura
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01073
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=30751
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507525
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01907
ChemSpider
http://www.chemspider.com/Chemical-Structure.28532.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0024-5820-15
PharmGKB
http://www.pharmgkb.org/drug/PA449655
Wikipedia
http://en.wikipedia.org/wiki/Fludarabine
RxList
http://www.rxlist.com/cgi/generic/fludarabine.htm
Drugs.com
http://www.drugs.com/cdi/fludarabine.html
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