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Tamás Solymosi

NanGenex Inc., Hungary

Title: Nano-amorphous Abiraterone acetate formulation with improved bioavailability and eliminated food effect
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Biography

Biography: Tamás Solymosi

Abstract

Abiraterone acetate (AA) is a poorly water soluble drug molecule indicated for metastatic castration resistant prostate cancer. The drug product Zytiga possesses the highest food effect of all marketed drugs. Despite of the extremely poor absorption of AA in fasted conditions, Zytiga is to be taken strictly without food. We have developed a nano-amorphous abiraterone acetate formulation prepared by controlled precipitation followed by lyophilization. The formulation exhibited higher apparent solubility and passive permeability when compared to either the crystalline AA or Zytiga. DLS (Dynamic Light Scattering) measurements and filtration experiments yielded particle size in the 100-200 nanometer range when the solid formula was reconstituted in water. The active ingredient in the formulation was amorphous by XRD (X-ray Powder Diffraction). Beagle dog studies showed 10-fold increase in exposure from the novel formulation when compared to the marketed drug. Also, the marked food effect seen with Zytiga was not observed for the nano-amorphous AA. A first-in-human clinical trial was conducted with a lyophilized powder-in bottle formulation in healthy male volunteers. The active ingredient was rapidly absorbed in both the fasted and the fed states. Based on the PK (Pharmacokinetics) analysis a 250 mg dose of the novel formulation is predicted to give the same exposure as 1000 mg Zytiga in the fasted state. As in preclinical studies, the significant positive food effect was eliminated. Moreover, variability of exposure was reduced when compared to Zytiga. In conclusion we have developed a novel nano-amorphous AA formulation that significantly outperformed the marketed product in in vitro and in vivo tests. Ultimately, the formulation might allow a 75% dose reduction and negate the restriction of a food label.