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Tuesday, March 31, 2009 12:23:50 PM
Nucleoside vs Nucleotide (updated for VRUS’ PSI-7851)
[The old post (#msg-34771363) contained a statement at the very end that IDX-184 was the only nucleotide polymerase inhibitor in development, which is no longer true.]
A nucleotide (right) consists of a nucleoside (left) and one-to-three
phosphate groups. (The depiction below contains one phosphate group.)
Why does this distinction matter?
The nucleotide with three phosphates is the active agent for all drugs in this class. IDIX found that a major reason for the failure of NM283, a nucleoside, was the variability of the phosphorylation step to produce the triphosphate nucleotide from the nucleoside. With IDIX’s IDX184 and VRUS’ PSI-7851, this variability is eliminated because the prodrug resolves directly to the triphosphate nucleotide in vivo.
[The old post (#msg-34771363) contained a statement at the very end that IDX-184 was the only nucleotide polymerase inhibitor in development, which is no longer true.]
A nucleotide (right) consists of a nucleoside (left) and one-to-three
phosphate groups. (The depiction below contains one phosphate group.)
Why does this distinction matter?
The nucleotide with three phosphates is the active agent for all drugs in this class. IDIX found that a major reason for the failure of NM283, a nucleoside, was the variability of the phosphorylation step to produce the triphosphate nucleotide from the nucleoside. With IDIX’s IDX184 and VRUS’ PSI-7851, this variability is eliminated because the prodrug resolves directly to the triphosphate nucleotide in vivo.
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