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药品详细

Fludarabine (氟达拉滨 )

化学结构式图
中文名
氟达拉滨
英文名
Fludarabine
分子式
Not Available
化学名
{[(2R,3S,4S,5R)-5-(6-amino-2-fluoro-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}phosphonic acid
分子量
Average: 365.2117
Monoisotopic: 365.053662512
CAS号
75607-67-9
ATC分类
L01B 抗代谢药
药物类型
small molecule
阶段
商品名
Fludara;Fludura;
同义名
FAMP;Fludarabine 5'-monophosphate;Fludarabine monophosphate;Fludarabine phosphate;
基本介绍

Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a chemotherapy drug used in the treatment of hematological malignancies. [Wikipedia]

生产厂家
  • Actavis totowa llc
  • App pharmaceuticals llc
  • Genzyme corp
  • Hospira inc
  • Sandoz inc
  • Sanofi aventis us llc
  • Teva parenteral medicines inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Rai KR, Peterson BL, Appelbaum FR, Kolitz J, Elias L, Shepherd L, Hines J, Threatte GA, Larson RA, Cheson BD, Schiffer CA: Fludarabine compared with chlorambucil as primary therapy for chronic lymphocytic leukemia. N Engl J Med. 2000 Dec 14;343(24):1750-7. Pubmed
  2. Gonzalez H, Leblond V, Azar N, Sutton L, Gabarre J, Binet JL, Vernant JP, Dighiero G: Severe autoimmune hemolytic anemia in eight patients treated with fludarabine. Hematol Cell Ther. 1998 Jun;40(3):113-8. Pubmed
  3. Tournilhac O, Cazin B, Lepretre S, Divine M, Maloum K, Delmer A, Grosbois B, Feugier P, Maloisel F, Villard F, Villemagne B, Bastit D, Belhadj K, Azar N, Michallet M, Manhes G, Travade P: Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia. Blood. 2004 Jan 1;103(1):363-5. Epub 2003 Sep 11. Pubmed
剂型
Form Route Strength
Powder, for solution Intravenous
Tablet Oral
规格
Unit description Cost Unit
Fludara 50 mg vial 367.02 USD vial
Fludarabine 50 mg vial 240.0 USD vial
Oforta 10 mg tablet 92.57 USD tablet
化合物类型
Type small molecule
Classes
  • Purines and Purine Derivatives
  • Carbohydrates
Substructures
  • Glycerol and Derivatives
  • Hydroxy Compounds
  • Phosphonic Acids and Derivatives
  • Organophosphate Esters
  • Aliphatic and Aryl Amines
  • Ethers
  • Pyrimidines and Derivatives
  • Alcohols and Polyols
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Purines and Purine Derivatives
  • Phosphinic Acids and Derivatives
  • Furans
  • Cyanamides
  • Aryl Halides
  • Carbohydrates
适应症
Cancer 癌症;
药理
Indication 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
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Bioavailability is 55% following oral administration.
Volume of distribution Not Available
Protein binding 19-29%
Metabolism
Route of elimination Not Available
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]
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point 260 oC
Experimental Properties
Property Value Source
water solubility 3.53 mg/ml PhysProp
logP -2.8 PhysProp
Predicted Properties
Property Value Source
water solubility 2.97e+00 g/l ALOGPS
logP -2.51 ALOGPS
logP -3.97 ChemAxon Molconvert
logS -2.09 ALOGPS
pKa 6.26 ChemAxon Molconvert
hydrogen acceptor count 10 ChemAxon Molconvert
hydrogen donor count 5 ChemAxon Molconvert
polar surface area 186.07 ChemAxon Molconvert
rotatable bond count 4 ChemAxon Molconvert
refractivity 74.93 ChemAxon Molconvert
polarizability 28.88 ChemAxon Molconvert
药物相互作用
Drug Interaction
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.
食物相互作用
  • Food slightly increases product bioavailability.
  • Take without regard to meals.

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