The Phase I clinical study tested escalating single doses of G4544 in 30 normal volunteers. The endpoints of the study were to determine safety and to assess pharmacokinetics and oral bioavailability. The drug was tested over a range of doses from 30 to 150mg.
Results showed that the drug was very well-tolerated, and that blood levels were achieved in a range that is known to be clinically bioactive. The mean peak plasma concentration at the highest dose was approximately 0.4micrograms/ml with a mean area under the plasma x concentration curve of approximately 20micrograms/ml x hr.
Raymond Warrell, Jr, chairman and CEO of Genta, said: “G4544 offers both ease of administration and patient convenience that could considerably expand the usefulness of this highly active compound. Completion of abbreviated toxicology work should enable multi-dose studies to proceed that are needed to secure regulatory approval.”