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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C11H16N4O4
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RX_link
No information avaliable
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
Showalter, HD et al., J. Med. Chem. 26:1478 (1983)
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Molecular Weight
268.269 g/mol
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Melting Point
220 oC
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H2O Solubility
30 mg/mL
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State
Solid
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LogP
-1.58
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Dosage Forms
Powder for solution
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Indication
For the treatment of hairy cell leukaemia refractory to alpha interferon.
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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).
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Absorption
Not absorbed orally, crosses blood brain barrier.
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side effects and Toxicity
LD50=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression.
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Patient Information
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Organisms Affected
Humans and other mammals