Pentostatin drug data and news

Pentostatin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Pentostatin
Brand Names/Synonyms 2'-DCF; 2'-Deoxycoformycin; 2'-Dexoycoformycin; 2’-Dexoycoformycin; CI-825; CL67310465; Co-V; Co-Vidarabine; Covidarabine; Dcf; Deaminase Inhibitor; Deoxycoformycin; Nipent; PD-ADI; Pentostatin; Vidarbine; Vira a Deaminase Inhibitor
Indication For the treatment of hairy cell leukaemia refractory to alpha interferon
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Description Not Available
Pharmacology Pentostatin is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia and hairy cell leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. 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).
Mechanism Of Action 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).
Pentostatin News
(When available)
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Dosage Forms POWDER FOR SOLUTION
Drug_Category Immunosuppressive Agents; Antibiotics; Antineoplastic Agents; ATC:L01XX08
Absorption Not absorbed orally, crosses blood brain barrier.
Interactions Interactions for Pentostatin:
Interactions with cylcopholsphamide, fludarabine and vidarabine
Toxicity LD50=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression.
Organisms Affected Humans and other mammals
Chemical IUPAC Name 8-[4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-4,6,8,10-tetrazabicyclo[5.3.0]deca-4,9,11-trien-2-ol
Chemical Formula C11H16N4O4
Molecular Weight 268.269 g/mol
Smiles String C1C(C(OC1N2C=NC3=C2NC=NCC3O)CO)O
Melting Point 220 °C
Water Solubility 30 mg/mL
State Solid
LogP/Hphobicity -1.58
Isoelectric Point 5.2
Biotransformation Primarily hepatic, but only small amounts are metabolized
Half Life 5.7 hours (with a range between 2.6 and 16 hrs)
Protein Binding [%] 4%
RxList Link Not Available>RXlist
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Drug Reference http://www.drugs.com/cons/Pentostatin.html
http://www.bccancer.bc.ca/HPI/DrugDatabase/DrugIndexPro/Pentostatin.htm
Drug Type Approved Drug
Accession No APRD00202
CAS Registry Number 53910-25-1
KEGG Compound ID C02267
PubChem ID SID:181721
PharmGKB ID PA450863
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2011247

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