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Identification
NameCladribine
Accession NumberDB00242  (APRD00260)
Typesmall molecule
Groupsapproved, investigational
Description

An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
2-CdANot AvailableNot Available
2-Chloro-2'-deoxy-beta-adenosineNot AvailableNot Available
2-Chloro-2'-deoxyadenosineNot AvailableNot Available
2-ChlorodeoxyadenosineNot AvailableNot Available
2ClAdoNot AvailableNot Available
CldAdoNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
LeustatinNot Available
LitakNot Available
MovectroNot Available
MylinaxNot Available
Brand mixturesNot Available
Categories
CAS number4291-63-8
WeightAverage: 285.687
Monoisotopic: 285.062866982
Chemical FormulaC10H12ClN5O3
InChI KeyInChIKey=PTOAARAWEBMLNO-KVQBGUIXSA-N
InChI
InChI=1S/C10H12ClN5O3/c11-10-14-8(12)7-9(15-10)16(3-13-7)6-1-4(18)5(2-17)19-6/h3-6,17-18H,1-2H2,(H2,12,14,15)/t4-,5+,6+/m0/s1
IUPAC Name
(2R,3S,5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-2-(hydroxymethyl)oxolan-3-ol
SMILES
NC1=C2N=CN([C@H]3C[C@H](O)[C@@H](CO)O3)C2=NC(Cl)=N1
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassOrganooxygen Compounds
ClassCarbohydrates and Carbohydrate Conjugates
SubclassGlycosyl Compounds
Direct parentPurine 2'-deoxyribonucleosides and Analogues
Alternative parentsPentoses; Purines and Purine Derivatives; Aminopyrimidines and Derivatives; Halopyrimidines; Primary Aromatic Amines; Aryl Chlorides; N-substituted Imidazoles; Oxolanes; Tetrahydrofurans; Secondary Alcohols; Ethers; Polyamines; Primary Alcohols; Organochlorides
Substituentspentose monosaccharide; purine; imidazopyrimidine; aminopyrimidine; halopyrimidine; n-substituted imidazole; aryl halide; primary aromatic amine; monosaccharide; aryl chloride; pyrimidine; tetrahydrofuran; imidazole; oxolane; azole; secondary alcohol; ether; polyamine; primary alcohol; organohalogen; primary amine; organochloride; alcohol; organonitrogen compound; amine
Classification descriptionThis compound belongs to the purine 2'-deoxyribonucleosides and analogues. These are compounds consisting of a purine linked to a ribose which lacks an hydroxyl group at position 2.
Pharmacology
IndicationFor the treatment of active hairy cell leukemia (leukemic reticuloendotheliosis) as defined by clinically significant anemia, neutropenia, thrombocytopenia, or disease-related symptoms. Also used as an alternative agent for the treatment of chronic lymphocytic leukemia (CLL), low-grade non-Hodgkin's lymphoma, and cutaneous T-cell lymphoma.
PharmacodynamicsCladribine is a synthetic purine nucleoside that acts as an antineoplastic agent with immunosuppressive effects. Cladribine differs structurally from deoxyadenosine only by the presence of a chlorine atom at position 2 of the purine ring, which results in resistance to enzymatic degradation by adenosine deaminase. Due to this resistance, cladribine exhibits a more prolonged cytotoxic effect than deoxyadenosine against resting and proliferating lymphocytes. Cladribine is one of a group of chemotherapy drugs known as the anti-metabolites. Anti-metabolites stop cells from making and repairing DNA, which are processes that are necessary for cancer cells to grow and multiply.
Mechanism of actionCladribine is structurally related to fludarabine and pentostatin but has a different mechanism of action. Although the exact mechanism of action has not been fully determined, evidence shows that cladribine is phosphorylated by deoxycytidine kinase to the nucleotidecladribine triphosphate (CdATP; 2-chloro-2′-deoxyadenosine 5′-triphosphate), which accumulates and is incorporated into DNA in cells such as lymphocytes that contain high levels of deoxycytidine kinase and low levels of deoxynucleotidase, resulting in DNA strand breakage and inhibition of DNA synthesis and repair. High levels of CdATP also appear to inhibit ribonucleotide reductase, which leads to an imbalance in triphosphorylated deoxynucleotide (dNTP) pools and subsequent DNA strand breaks, inhibition of DNA synthesis and repair, nicotinamide adenine dinucleotide (NAD) and ATP depletion, and cell death. Unlike other antimetabolite drugs, cladribine has cytotoxic effects on resting as well as proliferating lymphocytes. However, it does cause cells to accumulate at the G1/S phase junction, suggesting that cytotoxicity is associated with events critical to cell entry into S phase. It also binds purine nucleoside phosphorylase (PNP), however no relationship between this binding and a mechanism of action has been established.
AbsorptionOral bioavailability is 34 to 48%.
Volume of distribution
  • 4.5 ± 2.8 L/kg [patients with hematologic malignancies]
  • 9 L/kg
Protein binding20%
Metabolism

Metabolized in all cells with deoxycytidine kinase activity to 2-chloro-2'-deoxyadenosine-5'-triphosphate

SubstrateEnzymesProduct
Cladribine
    2-chloro-2'-deoxyadenosine-5'-triphosphateDetails
    Route of eliminationNot Available
    Half life5.4 hours
    Clearance
    • 978 +/- 422 mL/h/kg
    ToxicitySymptoms of overdose include irreversible neurologic toxicity (paraparesis/quadriparesis), acute nephrotoxicity, and severe bone marrow suppression resulting in neutropenia, anemia and thrombocytopenia.
    Affected organisms
    • Humans and other mammals
    PathwaysNot Available
    SNP Mediated EffectsNot Available
    SNP Mediated Adverse Drug ReactionsNot Available
    ADMET
    Predicted ADMET features
    Property Value Probability
    Human Intestinal Absorption + 1.0
    Blood Brain Barrier + 0.9386
    Caco-2 permeable - 0.7394
    P-glycoprotein substrate Non-substrate 0.6469
    P-glycoprotein inhibitor I Non-inhibitor 0.9139
    P-glycoprotein inhibitor II Non-inhibitor 0.8526
    Renal organic cation transporter Non-inhibitor 0.8722
    CYP450 2C9 substrate Non-substrate 0.8948
    CYP450 2D6 substrate Non-substrate 0.8145
    CYP450 3A4 substrate Non-substrate 0.5
    CYP450 1A2 substrate Non-inhibitor 0.7226
    CYP450 2C9 substrate Non-inhibitor 0.8803
    CYP450 2D6 substrate Non-inhibitor 0.9007
    CYP450 2C19 substrate Non-inhibitor 0.8856
    CYP450 3A4 substrate Non-inhibitor 0.831
    CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8761
    Ames test Non AMES toxic 0.8673
    Carcinogenicity Non-carcinogens 0.6795
    Biodegradation Not ready biodegradable 1.0
    Rat acute toxicity 2.2055 LD50, mol/kg Not applicable
    hERG inhibition (predictor I) Weak inhibitor 0.9326
    hERG inhibition (predictor II) Non-inhibitor 0.8344
    Pharmacoeconomics
    Manufacturers
    • App pharmaceuticals llc
    • Bedford laboratories div ben venue laboratories inc
    • Ortho biotech products lp
    Packagers
    Dosage forms
    FormRouteStrength
    SolutionIntravenous
    Prices
    Unit descriptionCostUnit
    Leustatin 10 mg/10 ml vial102.78USDml
    Cladribine 10 mg/10 ml vial34.2USDml
    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    PatentsNot Available
    Properties
    Statesolid
    Experimental Properties
    PropertyValueSource
    melting point215 °CNot Available
    logP-0.1Not Available
    Predicted Properties
    PropertyValueSource
    water solubility6.35e+00 g/lALOGPS
    logP-0.12ALOGPS
    logP-0.28ChemAxon
    logS-1.6ALOGPS
    pKa (strongest acidic)13.89ChemAxon
    pKa (strongest basic)1.33ChemAxon
    physiological charge0ChemAxon
    hydrogen acceptor count7ChemAxon
    hydrogen donor count3ChemAxon
    polar surface area119.31ChemAxon
    rotatable bond count2ChemAxon
    refractivity67.18ChemAxon
    polarizability25.93ChemAxon
    number of rings3ChemAxon
    bioavailability1ChemAxon
    rule of fiveYesChemAxon
    Ghose filterYesChemAxon
    Veber's ruleNoChemAxon
    MDDR-like ruleNoChemAxon
    Spectra
    SpectraNot Available
    References
    Synthesis Reference

    Szepsel Gerszberg, “Method for the production of 2-chloro-2' -deoxyadenosine (cladribine) and its 3,5-di-O-p-toluoyl derivative.” U.S. Patent US20020052491, issued May 02, 2002.

    US20020052491
    General Reference
    1. Warnke C, Wiendl H, Hartung HP, Stuve O, Kieseier BC: Identification of targets and new developments in the treatment of multiple sclerosis – focus on cladribine. Drug Des Devel Ther. 2010 Jul 21;4:117-26. Pubmed
    2. Sigal DS, Miller HJ, Schram ED, Saven A: Beyond hairy cell: the activity of cladribine in other hematologic malignancies. Blood. 2010 Jul 15. Pubmed
    3. Khalid BA, Hamilton NT, Cauchi MN: Binding of thyroid microsomes by lymphocytes from patients with thyroid disease and normal subjects. Clin Exp Immunol. 1976 Jan;23(1):28-32. Pubmed
    4. Sampat K, Kantarjian H, Borthakur G: Clofarabine: emerging role in leukemias. Expert Opin Investig Drugs. 2009 Oct;18(10):1559-64. Pubmed
    5. Kantarjian HM, Jeha S, Gandhi V, Wess M, Faderl S: Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30. Pubmed
    6. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    7. Larson ML, Venugopal P: Clofarabine: a new treatment option for patients with acute myeloid leukemia. Expert Opin Pharmacother. 2009 Jun;10(8):1353-7. Pubmed
    External Links
    ResourceLink
    KEGG DrugD01370
    PubChem Compound20279
    PubChem Substance46504588
    ChemSpider19105
    ChEBI567361
    ChEMBLCHEMBL1619
    Therapeutic Targets DatabaseDAP000565
    PharmGKBPA449027
    Drug Product Database2022117
    RxListhttp://www.rxlist.com/cgi/generic3/cladribine.htm
    Drugs.comhttp://www.drugs.com/cdi/cladribine.html
    WikipediaCladribine
    ATC CodesL01BB04
    AHFS Codes
    • 10:00.00
    PDB Entries
    FDA labelNot Available
    MSDSshow(43.7 KB)
    Interactions
    Drug Interactions
    Drug
    LeflunomideImmunosuppressants such as cladribine may enhance the adverse/toxic effect of leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Consider eliminating the use of a leflunomide loading dose in patients who are receiving other immunosuppressants in order to reduce the risk for serious adverse events such as hematologic toxicity. Also, patients receiving both leflunomide and another immunosuppressive medication should be monitored for bone marrow suppression at least monthly throughout the duration of concurrent therapy.
    NatalizumabImmunosuppressants such as cladribine may enhance the adverse/toxic effect of natalizumab. Specifically, the risk of concurrent infection may be increased. Patients receiving natalizumab should not use concurrent immunosuppressants, and patients receiving chronic corticosteroids prior to natalizumab should be tapered off of steroids prior to starting natalizumab.
    PimecrolimusPimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as cladribine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants.
    RoflumilastRoflumilast may enhance the immunosuppressive effect of immunosuppressants such as cladribine. The Canadian roflumilast product monograph recommends avoiding concurrent use of roflumilast with any immunosuppressant medications due to the antiinflammatory/immune altering effects of roflumilast and the lack of relevant clinical experience with such use. Of note, this recommendation to avoid concurrent use does not apply to either inhaled corticosteroids (which have much more limited systemic immune-suppressing actions) or short-term systemic corticosteroid use. U.S. prescribing information does not contain this warning; but it appears prudent to avoid this combination when possible.
    TacrolimusTacrolimus (Topical) may enhance the adverse/toxic effect of immunosuppressants such as tacrolimus. Avoid use of tacrolimus ointment in patients receiving immunosuppressants.
    TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
    Food Interactions
    • Echinacea should be used with caution, if at all, in patients receiving therapeutic immunosuppressants. Monitor for reduced efficacy of the immunosuppressant during concomitant use.

    1. Ribonucleoside-diphosphate reductase large subunit

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Ribonucleoside-diphosphate reductase large subunit P23921 Details

    References:

    1. Sampat K, Kantarjian H, Borthakur G: Clofarabine: emerging role in leukemias. Expert Opin Investig Drugs. 2009 Oct;18(10):1559-64. Pubmed
    2. Kantarjian HM, Jeha S, Gandhi V, Wess M, Faderl S: Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30. Pubmed
    3. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    4. Kline JP, Larson RA: Clofarabine in the treatment of acute myeloid leukaemia and acute lymphoblastic leukaemia: a review. Expert Opin Pharmacother. 2005 Dec;6(15):2711-8. Pubmed
    5. Takahashi T, Kanazawa J, Akinaga S, Tamaoki T, Okabe M: Antitumor activity of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) adenine, a novel deoxyadenosine analog, against human colon tumor xenografts by oral administration. Cancer Chemother Pharmacol. 1999;43(3):233-40. Pubmed

    2. Ribonucleoside-diphosphate reductase subunit M2

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Ribonucleoside-diphosphate reductase subunit M2 P31350 Details

    References:

    1. Sampat K, Kantarjian H, Borthakur G: Clofarabine: emerging role in leukemias. Expert Opin Investig Drugs. 2009 Oct;18(10):1559-64. Pubmed
    2. Kantarjian HM, Jeha S, Gandhi V, Wess M, Faderl S: Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30. Pubmed
    3. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    4. Kline JP, Larson RA: Clofarabine in the treatment of acute myeloid leukaemia and acute lymphoblastic leukaemia: a review. Expert Opin Pharmacother. 2005 Dec;6(15):2711-8. Pubmed
    5. Takahashi T, Kanazawa J, Akinaga S, Tamaoki T, Okabe M: Antitumor activity of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) adenine, a novel deoxyadenosine analog, against human colon tumor xenografts by oral administration. Cancer Chemother Pharmacol. 1999;43(3):233-40. Pubmed

    3. Ribonucleoside-diphosphate reductase subunit M2 B

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Ribonucleoside-diphosphate reductase subunit M2 B Q7LG56 Details

    References:

    1. Sampat K, Kantarjian H, Borthakur G: Clofarabine: emerging role in leukemias. Expert Opin Investig Drugs. 2009 Oct;18(10):1559-64. Pubmed
    2. Kantarjian HM, Jeha S, Gandhi V, Wess M, Faderl S: Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30. Pubmed
    3. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    4. Kline JP, Larson RA: Clofarabine in the treatment of acute myeloid leukaemia and acute lymphoblastic leukaemia: a review. Expert Opin Pharmacother. 2005 Dec;6(15):2711-8. Pubmed
    5. Takahashi T, Kanazawa J, Akinaga S, Tamaoki T, Okabe M: Antitumor activity of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) adenine, a novel deoxyadenosine analog, against human colon tumor xenografts by oral administration. Cancer Chemother Pharmacol. 1999;43(3):233-40. Pubmed

    4. DNA

    Kind: nucleotide

    Organism: Human

    Pharmacological action: yes

    Actions: other/unknown

    Components

    Name UniProt ID Details

    References:

    1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
    2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
    3. Sampat K, Kantarjian H, Borthakur G: Clofarabine: emerging role in leukemias. Expert Opin Investig Drugs. 2009 Oct;18(10):1559-64. Pubmed
    4. Kantarjian HM, Jeha S, Gandhi V, Wess M, Faderl S: Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30. Pubmed
    5. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    6. Kline JP, Larson RA: Clofarabine in the treatment of acute myeloid leukaemia and acute lymphoblastic leukaemia: a review. Expert Opin Pharmacother. 2005 Dec;6(15):2711-8. Pubmed
    7. Hartman WR, Hentosh P: The antileukemia drug 2-chloro-2’-deoxyadenosine: an intrinsic transcriptional antagonist. Mol Pharmacol. 2004 Jan;65(1):227-34. Pubmed

    5. DNA polymerase alpha catalytic subunit

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    DNA polymerase alpha catalytic subunit P09884 Details

    References:

    1. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    2. Kline JP, Larson RA: Clofarabine in the treatment of acute myeloid leukaemia and acute lymphoblastic leukaemia: a review. Expert Opin Pharmacother. 2005 Dec;6(15):2711-8. Pubmed
    3. Takahashi T, Kanazawa J, Akinaga S, Tamaoki T, Okabe M: Antitumor activity of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) adenine, a novel deoxyadenosine analog, against human colon tumor xenografts by oral administration. Cancer Chemother Pharmacol. 1999;43(3):233-40. Pubmed
    4. Hartman WR, Hentosh P: The antileukemia drug 2-chloro-2’-deoxyadenosine: an intrinsic transcriptional antagonist. Mol Pharmacol. 2004 Jan;65(1):227-34. Pubmed

    6. DNA polymerase epsilon catalytic subunit A

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    DNA polymerase epsilon catalytic subunit A Q07864 Details

    References:

    1. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed

    7. DNA polymerase epsilon subunit 2

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    DNA polymerase epsilon subunit 2 P56282 Details

    References:

    1. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed

    8. DNA polymerase epsilon subunit 3

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    DNA polymerase epsilon subunit 3 Q9NRF9 Details

    References:

    1. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed

    9. DNA polymerase epsilon subunit 4

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    DNA polymerase epsilon subunit 4 Q9NR33 Details

    References:

    1. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed

    10. Purine nucleoside phosphorylase

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inducer

    Components

    Name UniProt ID Details
    Purine nucleoside phosphorylase P00491 Details

    References:

    1. Bzowska A, Kazimierczuk Z: 2-Chloro-2’-deoxyadenosine (cladribine) and its analogues are good substrates and potent selective inhibitors of Escherichia coli purine-nucleoside phosphorylase. Eur J Biochem. 1995 Nov 1;233(3):886-90. Pubmed
    2. Dumontet C, Fabianowska-Majewska K, Mantincic D, Callet Bauchu E, Tigaud I, Gandhi V, Lepoivre M, Peters GJ, Rolland MO, Wyczechowska D, Fang X, Gazzo S, Voorn DA, Vanier-Viornery A, MacKey J: Common resistance mechanisms to deoxynucleoside analogues in variants of the human erythroleukaemic line K562. Br J Haematol. 1999 Jul;106(1):78-85. Pubmed
    3. Dumontet C, Bauchu EC, Fabianowska K, Lepoivre M, Wyczechowska D, Bodin F, Rolland MO: Common resistance mechanisms to nucleoside analogues in variants of the human erythroleukemic line K562. Adv Exp Med Biol. 1999;457:571-7. Pubmed
    4. Takimoto T, Kubota M, Tsuruta S, Kitoh T, Tanizawa A, Akiyama Y, Kiriyama Y, Mikawa H: Changes in sensitivity to anticancer drugs during TPA-induced cellular differentiation in a human T-lymphoblastoid cell line (MOLT-4). Leukemia. 1988 Jul;2(7):443-6. Pubmed
    5. Carson DA, Wasson DB, Lakow E, Kamatani N: Possible metabolic basis for the different immunodeficient states associated with genetic deficiencies of adenosine deaminase and purine nucleoside phosphorylase. Proc Natl Acad Sci U S A. 1982 Jun;79(12):3848-52. Pubmed

    1. Deoxycytidine kinase

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Deoxycytidine kinase P27707 Details

    References:

    1. Warnke C, Wiendl H, Hartung HP, Stuve O, Kieseier BC: Identification of targets and new developments in the treatment of multiple sclerosis – focus on cladribine. Drug Des Devel Ther. 2010 Jul 21;4:117-26. Pubmed
    2. Sigal DS, Miller HJ, Schram ED, Saven A: Beyond hairy cell: the activity of cladribine in other hematologic malignancies. Blood. 2010 Jul 15. Pubmed
    3. Kantarjian HM, Jeha S, Gandhi V, Wess M, Faderl S: Clofarabine: past, present, and future. Leuk Lymphoma. 2007 Oct;48(10):1922-30. Pubmed
    4. Sampat K, Kantarjian H, Borthakur G: Clofarabine: emerging role in leukemias. Expert Opin Investig Drugs. 2009 Oct;18(10):1559-64. Pubmed
    5. Zhenchuk A, Lotfi K, Juliusson G, Albertioni F: Mechanisms of anti-cancer action and pharmacology of clofarabine. Biochem Pharmacol. 2009 Dec 1;78(11):1351-9. Epub 2009 Jul 1. Pubmed
    6. Larson ML, Venugopal P: Clofarabine: a new treatment option for patients with acute myeloid leukemia. Expert Opin Pharmacother. 2009 Jun;10(8):1353-7. Pubmed

    1. Solute carrier family 22 member 2

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 2 O15244 Details

    References:

    1. Chen R, Nelson JA: Role of organic cation transporters in the renal secretion of nucleosides. Biochem Pharmacol. 2000 Jul 15;60(2):215-9. Pubmed

    2. Solute carrier family 22 member 1

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Solute carrier family 22 member 1 O15245 Details

    References:

    1. Chen R, Nelson JA: Role of organic cation transporters in the renal secretion of nucleosides. Biochem Pharmacol. 2000 Jul 15;60(2):215-9. Pubmed

    3. ATP-binding cassette sub-family G member 2

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

    References:

    1. de Wolf C, Jansen R, Yamaguchi H, de Haas M, van de Wetering K, Wijnholds J, Beijnen J, Borst P: Contribution of the drug transporter ABCG2 (breast cancer resistance protein) to resistance against anticancer nucleosides. Mol Cancer Ther. 2008 Sep;7(9):3092-102. Epub 2008 Sep 2. Pubmed

    4. Solute carrier family 28 member 3

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Components

    Name UniProt ID Details
    Solute carrier family 28 member 3 Q9HAS3 Details

    References:

    1. Badagnani I, Chan W, Castro RA, Brett CM, Huang CC, Stryke D, Kawamoto M, Johns SJ, Ferrin TE, Carlson EJ, Burchard EG, Giacomini KM: Functional analysis of genetic variants in the human concentrative nucleoside transporter 3 (CNT3; SLC28A3). Pharmacogenomics J. 2005;5(3):157-65. Pubmed

    Comments
    Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:08