- All three AEZS-112 follow-up candidates were equal to or more efficient
in exerting cytotoxic activity in tumor cell lines and inhibiting
tubulin polymerization than AEZS-112, whereas induction of cell cycle
arrest and apoptosis was slightly improved;
- An interesting difference to the AEZS-112 profile is the inhibition of
topoisomerase I by compounds 2 and 3. Moreover, compound 2 displayed
significant higher potency for topoisomerase II inhibition than
- In vitro plasma and liver microsomal stability of the follow-up
candidates are comparable to AEZS-112, thus demonstrating suitability
for in vivo efficacy studies;
- Interference with clonogenic growth of xenograft-derived cells revealed
variability in the response of the different tumor classes to AEZS-112
and compound 1 treatment as a basis for selection of the most
appropriate in vivo efficacy models.
Based on their interesting in vitro profiles, all three follow-up candidates will be subjected to human tumor xenograft in vivo models aimed at selecting an AEZS-112 follow-up candidate for preclinical development.
The poster presentation is available in the Investor section of the Company's website under "Events and Webcasts" at http://www.aeternazentaris.com.
AEZS-112 is a novel oral multi-targeted cytotoxic compound with inhibitory effects on tubulin polymerization, topoisomerase II and angiogenesis. In January 2007, the Company initiated a Phase 1 clinical trial for solid tumors and lymphoma; primary endpoints will focus on determining the safety and tolerability of the compound.
AEZS-112 has shown potent in vitro anti-proliferative activity at
nanomolar concentrations against human tumor cell lines of diff
|SOURCE AETERNA ZENTARIS INC.|
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