Versartis, Inc., an emerging biotechnology company developing novel therapeutics for patients with metabolic diseases, disclosed that it has begun dosing patients in a phase 1a clinical trial of the company’s lead product VRS-859 (exenatide-XTEN) for type 2 diabetes mellitus (T2DM). VRS-859 is a once monthly form of the GLP-1 analog, exenatide.
The phase 1a multi-centre, blinded, placebo-controlled, single-ascending dose study is designed to demonstrate safety and the ability to maintain glycemic control for one month in T2DM patients after a single dose. The Phase 1a study will be followed by a repeat dose (3 month) phase 1b study comparing Byetta to VRS-859 in T2DM patients, which is planned to begin in the fourth quarter of 2010.
“We are pleased that the investigational compound VRS-859 is proceeding into human clinical trials, because it addresses significant unmet needs for the treatment of patients with type 2 diabetes,” commented Mark Kipnes, M.D., executive vice president, Medical Affairs, Cetero Research/DGD Research, San Antonio, TX, and a member of the Versartis Clinical Advisory Board. “A once monthly form of the GLP-1 analog exenatide could offer multiple patient benefits including increased efficacy and safety, as well as convenience and potentially better patient compliance.”
The primary objective of this first study is to determine the safety and tolerability of a single subcutaneous (SC) dose of VRS-859 in patients with T2DM. In addition, the study is designed 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.
“In just over a year since our Series A financing, Versartis has quickly and efficiently executed on its development plans,” noted Jeffrey L. Cleland, Ph.D., Versartis chief executive officer. “We have successfully begun a Phase I patient study for our lead programme, VRS-859; further validating our capital-efficient model, which minimizes expenditures through proof-of-concept for products addressing both significant unmet medical needs and large market opportunities.”
Previously, VRS-859 was studied in preclinical animal models of T2DM to assess the drug’s pharmacokinetics (PK) in multiple animal species and to determine the relationship between PK and pharmacodynamics (PD). The preclinical data on VRS-859, which is an 84 kDa fusion protein, indicate that the dose required to sustain a therapeutic level in type 2 diabetes patients is less than 100 mg once per month as a single subcutaneous injection via a small-gauge needle. As a result of the long projected half-life of VRS-859 in humans, active drug levels are expected to be sustained throughout each month, potentially increasing the efficacy and decreasing the acute side effects of the drug relative to other GLP-1 analogs.
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 Versartis using the XTEN technology are expected to provide improved therapeutic outcomes such as enhanced efficacy, fewer side effects, prolonged half-life (up to monthly dosing), as well as low cost production and enhanced stability.