ConjuChem Reports Final Results of PC-DAC: Exendin-4 Phase I/II Multiple-Dose Study for Type 2 Diabetes Confirming Safety and Efficacy at Once-Weekly Dosing

Additional Analyses Confirm Significant Glucose Reductions   

MONTREAL, Oct. 17, 2007/CNW/ - ConjuChem Biotechnologies Inc. (TSX:CJB) today  announced that final data from its Phase I/II multiple-dose clinical study for  the treatment of Type 2 diabetes using the Company's proprietary  PC-DAC(TM):Exendin-4 compound confirmed the preliminary data reported on March  27, 2007. Final results demonstrated that the compound was well tolerated and  effective in lowering blood glucose when administered once-weekly at each of  the dosing levels tested.      

The Phase I/II trial, a randomized, double-blind, multiple-dose study,  evaluated safety and tolerability of PC-DAC(TM):Exendin-4 in patients with  stable Type 2 diabetes. Pharmacokinetic and pharmacodynamic parameters were  also evaluated. All patients were on stable doses of Metformin with HbA1c  levels between 7.0% and 10.6%. The trial enrolled 70 patients at seven centers  in the U.S. and Canada with patients randomized to one of four parallel  treatment groups: 1 mg (n=18), 2 mg (n=17), 3 mg (n=17) or placebo (n=18).  Sixty-nine patients received five doses over a one month period. The product  is a highly soluble liquid formulation injected with a fine, 30 gauge needle.      

Reductions in mean fasting plasma glucose (FPG) were statistically  significant in all treatment groups versus baseline and placebo over the  five-week treatment period (FPG was measured Days 1 and 7 post-dosing). The  average reductions from baseline values for the 1 mg, 2 mg, and 3 mg treatment  arms were -9% (baseline 154 mg/dL), -11% (baseline 172 mg/dL), and -7%  (baseline 170 mg/dL), respectively, versus -1% (baseline 158 mg/dL) in the  placebo group. The reductions were statistically significant versus baseline  (p less than 0.005 for all cohorts) and versus placebo (p less than 0.005 for  1 mg and 2 mg cohorts, p less than 0.03 for the 3 mg cohort).      

HbA1c levels declined in all three treatment groups with median HbA1c  decreasing 0.5%, 0.8%, and 0.6% in the 1 mg, 2 mg, and 3 mg groups at the end  of the five-week dosing period (day 35). Decreases of 0.7%, 0.6%, and 0.7%  were observed at day 49 and decreases of 0.7%, 0.8%, and 0.9% were observed at  the end of the study period (day 63) versus baseline. HbA1c levels of the  placebo group declined 0.35% at five weeks, 0.3% at day 49, and 0.2% at the  end of the study period. The reduction for the pooled treatment groups was  statistically significant versus placebo at day 49 and at the end of the study  period (p less than 0.03, ANCOVA).      

Pharmacokinetic analysis showed dose proportionality and drug  concentration approaching steady-state after five weeks with a terminal  half-life of approximately one week. The drug was generally well tolerated. The most common side effects  during the 35-day treatment included headache occurring in 2 out of 18 placebo  patients (11%) and 15 out of 52 treated patients (29%) and nausea which was  reported in 3 out of 18 placebo patients (17%) and 11 out of 52 treated  patients (21%). There were no cases of drug-related vomiting in either the  1 mg or 2 mg cohorts; vomiting occurred in five patients in the 3 mg cohort,  none of which led to patient drop-out. GI tolerability to the drug generally  improved over time consistent with the known development of GI tolerance of  this drug class. There were no skin reactions in the 2 mg and 3 mg treatment  groups; skin reactions were reported in four placebo patients and one patient  in the 1 mg cohort. Generally low-level antibodies were detected in 11 out of  52 treated patients (21%). There were no drug-related serious adverse events  during the study.      

Further analysis of the 1 mg and 2 mg treatment cohorts showed  significant decreases in mean daily plasma glucose (6 time points before and  after meals on Days 1, 7, 14, 21, and 28) versus both baseline and placebo  (p values ranging from 0.0001 to 0.002). Decreases in post-prandial glucose  excursions were also noted in the 6-point plasma glucose profile. Additionally, decreases in mean weekly blood glucose (based on daily  paired glucometer readings) for the 1 mg and 2 mg cohorts were significant  versus both baseline and placebo for all five weeks of the treatment period  (p values ranging from 0.0001 to 0.02).   

Next Steps   

ConjuChem also reported that product development programs including  manufacturing process improvements have been completed and will be included in  all future development programs. ConjuChem is moving to a multi-dose Phase II  study in which the product will be administered once-a-week for three months.  Preparations are ongoing with initial dosing expected to commence in the first  quarter.   

About PC-DAC(TM):Exendin-4   

PC-DAC(TM):Exendin-4 is a therapy being developed for Type II diabetes.  Exendin-4, like Glucagon-like peptide-1 (GLP-1), is an insulinotropic peptide  and an agonist for the GLP-1 receptor. Exendin-4 decreases glucagon and  increases insulin secretion in a glucose-dependent manner. Exendin-4 may  stimulate beta-cell proliferation, restore beta-cell sensitivity to glucose,  delay gastric emptying, and increase peripheral sensitivity to glucose. The  clinical utility of Exendin-4 is somewhat limited by its relatively short  half-life in plasma. Developed with ConjuChem's proprietary PC-DAC(TM)  technology, PC-DAC(TM):Exendin-4 is a modified Exendin-4 analogue that is  covalently bound to recombinant human albumin (Recombumin(R), provided by  Novozymes Delta Limited). Data from Phase I/II clinical studies have  demonstrated that the preformed albumin-peptide conjugate has a much longer  half-life than the peptide alone. The product is a highly soluble liquid  formulation that is injectable in a small volume with a small gauge needle.   

About ConjuChem Biotechnologies   

ConjuChem, developer 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 DAC(TM) and  PC-DAC(TM) Technologies enable the creation of new drugs with significantly  enhanced therapeutic properties as compared to the original peptide.       Detailed descriptions of the Company can be viewed on the Company's  website http://www.conjuchem.com.

Forward-Looking Statements   

Some of the statements made herein may constitute forward-looking  statements. These statements relate to future events or our future financial  performance and involve known and unknown risks, uncertainties and other  factors that may cause ConjuChem's actual results, performance or achievements  to be materially different from those expressed or implied by any of the  Company's statements. Actual events or results may differ materially. We  disclaim any intention, and assume no obligation, to update these  forward-looking statements.   

For further information: Lennie Ryer, CA, Vice President Finance, CFO,  ConjuChem Biotechnologies, Inc., (514) 844-5558 ext 224, ryer@conjuchem.com;  James Smith, Investor Relations, (416) 815-0700 ext. 229, (416) 815-0080,  jsmith@equicomgroup.com/

   


 

Posted: October 2007

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