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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB00552
rdf:type
n5:Drug
n5:description
A potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. [PubChem]
n5:dosage
n10:271B450B-363D-11E5-9242-09173F13E4C5
n5:generalReferences
# "Link":http://www.bccancer.bc.ca/HPI/DrugDatabase/DrugIndexPro/Pentostatin.htm
n5:group
investigational approved
n5:halfLife
5.7 hours (with a range between 2.6 and 16 hrs)
n5:indication
For the treatment of hairy cell leukaemia refractory to alpha interferon.
n5:manufacturer
n12:271B4507-363D-11E5-9242-09173F13E4C5 n12:271B4508-363D-11E5-9242-09173F13E4C5
owl:sameAs
n15:DB00552 n18:DB00552
dcterms:title
Pentostatin
adms:identifier
n4:DB00552 n6:PA450863 n7:439693 n8:D00155 n11:0409-0801-01 n13:50003603 n22:46507116 n25:Pentostatin n27:C02267 n28:37371
n5:mechanismOfAction
Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in cells of the lymphoid system. T-cells have higher ADA activity than B-cells, and T-cell malignancies have higher activity than B-cell malignancies. The cytotoxicity that results from prevention of catabolism of adenosine or deoxyadenosine is thought to be due to elevated intracellular levels of dATP, which can block DNA synthesis through inhibition of ribonucleotide reductase. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase).
n5:packager
n12:271B4503-363D-11E5-9242-09173F13E4C5 n12:271B4504-363D-11E5-9242-09173F13E4C5 n12:271B4502-363D-11E5-9242-09173F13E4C5 n12:271B4505-363D-11E5-9242-09173F13E4C5 n12:271B4506-363D-11E5-9242-09173F13E4C5
n5:routeOfElimination
In man, following a single dose of 4 mg/m2 of pentostatin infused over 5 minutes, approximately 90% of the dose was excreted in the urine as unchanged pentostatin and/or metabolites as measured by adenosine deaminase inhibitory activity.
n5:synonym
Co-vidarabine Pentostatin Pentostatinum Nipent Pentostatina Pentostatine
n5:toxicity
LD<sub>50</sub>=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression.
n5:proteinBinding
4%
n5:synthesisReference
Nadji Sourena, "Process for the production of pentostatin aglycone and pentostatin." U.S. Patent US20040181052, issued September 16, 2004.
n23:hasConcept
n24:M0023987
foaf:page
n17:pentostatin.html
n5:IUPAC-Name
n9:271B4510-363D-11E5-9242-09173F13E4C5
n5:InChI
n9:271B4516-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n9:271B4515-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n9:271B4512-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n9:271B4513-363D-11E5-9242-09173F13E4C5
n5:SMILES
n9:271B4514-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n9:271B4526-363D-11E5-9242-09173F13E4C5 n9:271B450E-363D-11E5-9242-09173F13E4C5
n5:logP
n9:271B450C-363D-11E5-9242-09173F13E4C5 n9:271B450F-363D-11E5-9242-09173F13E4C5 n9:271B4528-363D-11E5-9242-09173F13E4C5
n5:logS
n9:271B450D-363D-11E5-9242-09173F13E4C5
n5:pKa
n9:271B4529-363D-11E5-9242-09173F13E4C5
n20:hasATCCode
n21:L01XX08
n5:H-Bond-Acceptor-Count
n9:271B451C-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n9:271B451D-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n9:271B4517-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n9:271B4518-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n9:271B451A-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n9:271B4519-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n9:271B451B-363D-11E5-9242-09173F13E4C5
n5:absorption
Not absorbed orally, crosses blood brain barrier.
n5:affectedOrganism
Shigella Borrelia burgdorferi Escherichia coli Leptospira interrogans Klebsiella Staphylococcus aureus Salmonella typhi Mycobacterium tuberculosis Serratia marcescens Pseudomonas aeruginosa Proteus vulgaris Vibrio cholerae Humans and other mammals
n5:casRegistryNumber
53910-25-1
n5:category
n5:clearance
* 68 mL/min/m2
n5:containedIn
n26:271B450A-363D-11E5-9242-09173F13E4C5 n26:271B4509-363D-11E5-9242-09173F13E4C5
n5:Bioavailability
n9:271B4522-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n9:271B4524-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n9:271B4525-363D-11E5-9242-09173F13E4C5
n5:Melting-Point
n9:271B4527-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n9:271B4521-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n9:271B4520-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n9:271B4523-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n9:271B4511-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-acidic-
n9:271B451E-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-basic-
n9:271B451F-363D-11E5-9242-09173F13E4C5