AEterna Zentaris Presents Two Posters on its PI3K Inhibitor Compound, AEZS-126, at AACR Annu...( In Vitro and In Vivo Data Show AEZS-1...)

In Vitro and In Vivo Data Show AEZS-126 as Promising Oral Compound for

Future Clinical Development in Cancer

QUEBEC CITY, April 21 /PRNewswire-FirstCall/ - AEterna Zentaris Inc. (TSX: AEZ; NASDAQ: AEZS), a global biopharmaceutical company focused on endocrine therapy and oncology, today presented two posters on AEZS-126, a promising compound for clinical intervention of the PI3K/ Akt pathway in human tumors. The posters were presented at the American Association for Cancer Research (AACR) Annual Meeting in Denver, Colorado.

Poster #3705

Entitled, "AEZS-126, a new orally bioavailable PI3K inhibitor with antitumor effects", I. Seipelt, S. Baasner, M. Gerlach, M. Teifel, J. Fensterle, L. Blumenstein, G. Mueller and E. Guenther, the poster focuses on ADMET and safety profiling of the compound, as well as in vivo pharmacokinetic experiments and mouse xenograft antitumor studies.

Results

AEZS-126 was identified as a potent inhibitor of class I PI3Ks in biochemical and cellular assays and demonstrated favorable properties in early in vitro ADMET screening including microsomal stability, plasma stability and screening against a large safety profile composed of receptors, enzymes and cardiac ion-channels. During the course of in vivo pharmacokinetic experiments and mouse xenograft antitumor studies, the oral bioavailability in mice was determined to be about 60%, leading to micromolar plasma levels which are well above the nanomolar IC50 values in in vitro studies. Significant antitumor activity was observed at 30mg/kg daily oral administration in Hct116 and A549 models.

Conclusion

These data suggest that AEZS-126 is a promising compound for clinical intervention of the PI3K/Akt pathway in human tumors.

Poster #3706