Innovation Pharmaceuticals Inc (IPIX)

[georgejjl]

Cellceutix has decided to pursue an oral formulation for Kevetrin to improve patient convenience and potentially increase therapeutic efficacy given the drug’s short half-life and other pharmacokinetics, as discussed below.

As background, pre-clinical work determined the bioavailability of Kevetrin was 79 percent when given orally in Sprague-Dawley rats. To further establish the efficacy of oral Kevetrin, in vivo mouse studies were carried out in an ascites ovarian tumor model using OVCAR-3 and OV-90 tumor models, both of which possess different mutant p53 genes. Importantly, these pre-clinical results showed that the overall efficacy of Kevetrin was similar across both oral and intraperitoneal routes of drug administration.

Cellceutix has initiated a series of GLP (Good Laboratory Practice) studies to assess the safety of Kevetrin given orally. Considering that Kevetrin is a non-cytotoxic drug, our intent, with FDA permission, is to next proceed with a Phase 1 clinical trial in healthy volunteers using the oral route. These studies are being conducted by approved vendors and include: photosafety testing, pharmacokinetics, in vivo metabolism, metabolic stability, protein binding, and genetic and physiological toxicology reports.

Preliminary data analyses in a pharmacokinetic study in rats revealed a half-life of approximately 1 hour and a clearance of 78ml/min/kg for both oral and intravenous (IV) dosing. Results of an initial photosafety study demonstrated a molar extinction coefficient value of less than 5 L/mol*cm over a range of wavelengths above 290 nm, well below the 1000 L/mol*cm limit stated in ICH guidelines—indicating Kevetrin has no phototoxicity. A preliminary toxicity study showed that at doses up to 500 mg/kg given orally daily for 7 days, Kevetrin was well-tolerated by the rats as indicated by an 11 percent increase in body weight and no abnormal clinical observations. Further, this dose was greater than the doses used in the preclinical efficacy study. Remaining safety studies will be completed in the second half of this year.

Good luck and GOD bless,

George