Montreal, Canada, September 30, 2005 ConjuChem Inc. (TSX: CJC) today announced that further development activities for its DAC:GLP-1 compound have been put on hold pending completion of the Phase I study in patients with PC-DAC:Exendin-4 in the first half of 2006.
The Phase 1 single dose trial in patients with diluent (D23) improved the tolerability profile of the in vivo DAC:GLP-1 compound. However, the three-month D23 toxicity studies in animals failed to provide sufficient safety margins to advance D23 as a diluent into chronic dosing regimes. Additionally, the pharmacokinetic and pharmacodynamic profile of DAC:GLP-1, using diluent D23 did not lend itself to once weekly dosing.
"ConjuChem's goal is to develop a best in class GLP-1 analogue," said Dr. Jean Paul Castaigne, ConjuChem's COO. "The data generated to date with PC-DAC:Exendin-4 program indicates that this compound has the strongest potential to emerge as the leader in the GLP-1 class of drug therapies. Proof of concept data in patients is expected in the first half of 2006."
PC-DAC:Exendin-4 will be administered to Type 2 diabetic patients in a Phase 1/2 clinical program starting in Q1 2006. To date, the pre-clinical data has been very encouraging, demonstrating a significantly extended half-life of 30 fold relative to native exendin-4. This longer half-life resulted in a longer duration of therapeutic activity. Full glucose control was obtained for more than a week after a single injection of PC-DAC:Exendin-4 in ZDF rats (ZDF rats are obese rats with Type 2 diabetes). Finally, a significantly better tolerability profile was observed compared to exendin-4 in two independent rat models, which assessed GI tolerance and nausea. PC-DAC:Exendin-4 is expected to be stable at room temperature, thus being highly convenient for patients.
Developed to treat Type 2 diabetes, exendin-4 is a close analogue to GLP-1, the human body's most potent insulinotropic hormone. It has been shown to normalize blood glucose levels by a) stimulating insulin secretion and lowering glucagons secretion in a glucose-dependent manner; b) delaying gastric emptying; c) induces Beta cell proliferation (demonstrated only in animals to date); d) restores Beta cell sensitivity to glucose; and e) increases peripheral sensitivity to insulin . Moreover, it appears to have a very attractive safety profile, with a low probability of inducing hypoglycemia.
About ConjuChem
ConjuChem, developers of next generation medicines from therapeutic peptides, is creating long-acting compounds based on bioconjugation platform technologies. When applied to peptides, the Company's systemic DACTM Technologies enable the creation of new drugs with significantly enhanced therapeutic properties as compared to the original peptide. The Company is developing compounds to treat various disorders including diabetes, human growth deficiencies, HIV/AIDS, and congestive heart failure.
Detailed descriptions of the Company can be viewed on the Company's website www.conjuchem.com.