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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.
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| 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 | ||
| Sponsored links | 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 | ||
| Sponsored links | |||
| 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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