Phase 1 stage s-EH Inhibitor
In October 2007, Arête commenced phase 1 clinical trials with AR9281 in healthy volunteers. This novel, first-in-class compound is being developed to treat patients with hypertension. The first in human, single dose, placebo-controlled study is evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of AR9281. As part of the pharmacodynamic assessment, levels of s-EH-specific biomarkers will be quantified, along with detailed blood pressure measurements.
Following completion of the single dose study, a multiple dose phase 1 study as well as a food effect study and studies in special populations are planned. This comprehensive phase 1 program will provide the necessary safety and tolerance information to rapidly move into phase 2 proof-of-concept studies in the target population of patients with hypertension. Based on positive preclinical data, additional studies are planned to explore the impact of s-EH inhibition on inflammation and metabolic syndrome.
AR9281 has shown activity in multiple animal mode of hypertension and vascular inflammation. In addition, AR9281 has been evaluated in various published and proprietary in vitro and in vivo assays for potency, selectivity, efficacy, ADME, toxicity and safety, with very favorable results.
In addition to AR9281, Arête is in the process of identifying and developing back-up and second generation expanded profile anti-hypertensive agents.
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