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news.Procyon Biopharma has unveiled the first pharmacokinetics results with its HIV protease inhibitor, PPL-100, revealing positive pharmacokinetic results compared to the drug's precursor, PL-100.
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Initial in vitro study results have indicated that PPL-100, a phosphorylated pro-drug of PL-100, is 1,000-fold more water soluble than its precursor. More importantly, pharmacokinetics studies conducted in rats showed a two- to three-fold improvement in key pharmacokinetic parameters such as maximum plasma concentration (Cmax) and oral bioavailability compared to PL-100.
Plasma levels obtained with PPL-100 in rats suggest that PPL-100’s previously-reported broad and favorable cross resistance profile will be supported in a clinical setting by encouraging pharmacokinetics results at this time.
“As oral bioavailability remains a challenge for the HIV protease inhibitor class, we are most happy to report significant progress with the development of PPL-100,” said Hans Mader, president and CEO of Procyon.
“PPL-100 presents the same favorable cross-resistance profile as the original molecule acquired from Pharmacor. However, its improved solubility and bioavailability should allow for the same therapeutic effect on drug-resistant HIV-infection but with potentially improved dosing characteristics,” he added.