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news.Genelabs Technologies has advanced a non-nucleoside compound from its internal hepatitis C virus drug discovery program into preclinical development.
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The compound, designated GL60667, is the second Genelabs non-nucleoside compound to advance into preclinical development. Genelabs has also further advanced GL59728, its first non-nucleoside preclinical development candidate.
Genelabs plans to initiate preclinical studies on GL59728 which, if successful, would enable the company to file an Investigational New Drug Application for the compound. Genelabs retains all commercial rights to its non-nucleoside compounds.
The company based its decision to advance compound GL60667 on rigorous pre- determined standards, including various measures of potency, metabolism, pharmacokinetics and toxicity. Genelabs believes that compounds meeting these criteria should hold a competitive advantage over other non-nucleoside hepatitis C virus (HCV) inhibitors described in the scientific literature.
During in vitro assays GL60667 demonstrated a potency of approximately 40 nanomolar against an HCV replicon and potency against the major genotypes of HCV, including genotype 1, the most common genotype in the US and Western Europe.
The concentration of GL60667 that is effective in reducing HCV replication is more than 100 times lower than the concentration that causes toxicity to various human cell lines, as demonstrated in a battery of tests conducted by Genelabs.
Genelabs has also profiled the metabolic and pharmacokinetic properties of GL60667 in several different animal species. Extrapolating from this data, Genelabs believes the compound should be suitable for once-a-day dosing.