Synthesis and pharmacokinetic and pharmacodynamic evaluation of the forodesine HCl analog BCX-3040.
Nucleosides Nucleotides Nucleic Acids
; 24(10-12): 1817-30, 2005.
Article
em En
| MEDLINE
| ID: mdl-16438050
ABSTRACT
Forodesine HCl is a potent inhibitor of the enzyme purine nucleoside phosphorylase (PNP) and is currently in clinical trials for the treatment of leukemia and lymphoma. Animal models indicated that forodesine HCl would have low oral bioavailability in humans and it was initially developed as an intravenous formulation. We were interested in identifying analogs of forodesine HCl with improved oral bioavailability. The 2'-deoxy analog (BCX-3040) was synthesized and its pharmacokinetic and pharmacodynamic properties compared with forodesine HCl.
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Base de dados:
MEDLINE
Assunto principal:
Leucemia
/
Purina-Núcleosídeo Fosforilase
/
Inibidores Enzimáticos
/
Hexosaminas
/
Linfoma
Limite:
Animals
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article