PHILADELPHIA, PA--(Marketwire - June 09, 2012) - Diartis Pharmaceuticals, Inc. today presented positive data from its recently completed Phase 1 multicenter clinical trial of VRS-859 (exenatide-XTEN) at the American Diabetes Association's 72nd Scientific Sessions, which began yesterday in Philadelphia. VRS-859, a long-acting glucagon-like peptide-1 (GLP-1) analog, is being developed as a once monthly treatment for patients with type 2 diabetes mellitus (T2DM). The Diartis poster -- "Safety, Pharmacokinetics, and Pharmacodynamics of a Single Subcutaneous Administration of VRS-859 in Patients with Type 2 Diabetes" -- was presented today, June 9, in the 11:30 am to 12:30 pm Clinical Therapeutics/NewTechnology session (Poster Presentation 1105-P).
Jeffrey L. Cleland, Ph.D., Diartis Chief Executive Officer, was present at the poster session to discuss the recently completed safety, pharmacokinetic (PK) and pharmacodynamics (PD) results from the company's Phase 1 clinical trial in T2DM patients. The Phase 1 multicenter, blinded, placebo-controlled, single-ascending dose study was designed to evaluate the safety and tolerability of VRS-859 as well as the ability to maintain glycemic control for one month in T2DM patients after a single dose.
"We are very encouraged by the robust results seen in this initial Phase 1 study, most notably the statistically significant reductions in HbA1c levels at 30 days after only a single 200 mg dose of VRS-859," commented Dr. Cleland. "We are also quite pleased by the dose-proportional decreases in body weight observed within 30 days after a single treatment."
The Phase 1 results in T2DM patients demonstrate that all doses administered (up to 200 mg) were well tolerated and no unexpected adverse events were noted. Furthermore, the PK of VRS-859 in these patients was dose linear and comparable to the profile predicted from preclinical studies, validating the half-life extension capability of the XTEN technology and supporting a once monthly dosing regimen for VRS-859.
The Phase 1 Trial
The primary objective of the study was to determine the safety and tolerability of a single subcutaneous dose of VRS-859 in patients with T2DM. Secondary objectives included single dose pharmacokinetics, assessment to evaluate evidence of VRS-859 activity by measurement of fasting plasma glucose and response to oral glucose tolerance tests at selected times post-dose, as well as to evaluate post-challenge glucose excursions. Seventy T2DM patients concurrently on metformin were enrolled in the study: 18 patients received placebo and 52 patients received one of six dose levels: 12.5, 25, 50, 100, 150 and 200 mg.
The study demonstrated that a single dose of VRS-859 achieved very high plasma concentrations and provided statistically significant and persistent improvements in glycemic control. There were no reported SAEs in the study. Adverse events, including those related to GI tolerability, were primarily mild and transient. These results support the company's plan to conduct a 6-month repeat dose study to determine a safe and efficacious subcutaneous dose of VRS-859 in patients with T2DM. It is hoped that upon successful development of this compound, VRS-859 may allow T2DM patients to safely manage their glucose with a therapy that is superior to current treatments for diabetes.
About Diabetes Treatment
Treatment of diabetes involves lowering blood glucose levels. Despite the availability of current therapies, more than 60 percent of people with diabetes do not achieve their target levels with their current treatment regimen. In addition, approximately 80 percent of type 2 diabetes patients are either overweight or obese. After diagnosis, type 2 diabetes patients are often placed on a diet and exercise program to control blood glucose levels and reduce body weight, but these patients usually progress to oral drug therapy, metformin and/or sulfonylurea. However it has been demonstrated that many patients are still unable to achieve adequate glycemic control on diet and exercise plus these oral therapies.
The compound has been designed to provide improved therapeutic outcomes for T2DM patients including robust and sustained improvements in HbA1c, improved tolerability, prolonged half-life (up to monthly dosing), as well as enhanced administration of a liquid formulation via a fine-gauge needle. The development goal is to satisfy the unmet needs of T2DM patients as well as contribute to treatment of the worldwide healthcare problem of obesity.
About Diartis Pharmaceuticals
Diartis Pharmaceuticals, Inc. is a privately held biopharmaceutical company with headquarters in Redwood City, CA. Diartis develops novel biologics with enhanced properties to provide improved therapeutic outcomes to patients with metabolic diseases. The company's initial focus is the development of a long-acting GLP-1 receptor agonist that conveniently delivers maximum glucose control, aids compliance and adherence via less frequent administrations, and has improved GI tolerability. Diartis acquired the VRS-859 (exenatide-XTEN) program from Versartis, Inc. and continues its development for T2DM.
XTEN is a novel hydrophilic sequence of natural amino acids and is expressed as a fusion protein with a therapeutically active peptide or protein. New compounds developed by Diartis using the XTEN technology are expected to provide improved therapeutic outcomes such as enhanced efficacy/compliance, fewer side effects, prolonged half-life (up to monthly dosing), as well as low-cost production and enhanced stability. Further information on Diartis can be found at www.diartispharma.com.