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Concert Pharmaceuticals’ Deuterium-Modified Boceprevir Demonstrates Enhanced Metabolic Stabilization and Improved Drug Properties

Findings Published in Journal of Labelled Compounds and Radiopharmaceuticals

July 20 , 2011

Lexington, MA –- Concert Pharmaceuticals, Inc. today announced the publication of a scientific paper describing the use of deuterium chemistry to enhance the pharmacokinetic properties of boceprevir.  Boceprevir is an HCV protease inhibitor that was recently approved by the FDA and European Commission, representing a major advance in the treatment of hepatitis C.  Using its DCE Platform^™ (deuterated chemical entity platform), Concert prepared several deuterium modified analogs of boceprevir that displayed substantial levels of in vitro metabolic stabilization. Deuterium modification significantly improved the compound’s in vitro half-life in human liver microsomal assays, to approximately double that of boceprevir.  In addition, based on laboratory studies, deuterium-modified boceprevir is expected to retain the biochemical potency and selectivity of this compound class.  These findings were published in the Journal of Labelled Compounds and Radiopharmaceuticals.

“This work highlights the utility of our DCE Platform to enhance important properties of this groundbreaking new drug. The efficacy of antiretroviral agents is often correlated with maintaining appropriate drug levels at the site of viral replication, so we are excited by the potential of deuterium substitution to improve boceprevir’s pharmacokinetic behavior,” said Scott Harbeson, Ph.D., Vice President, Drug Discovery and Basic Research.  “We have prepared a significant number of deuterium-containing compounds, such as deuterium-modified boceprevir, that are showing improved metabolic properties such as enhanced pharmacokinetics.  With some of these compounds now in clinical evaluation, we expect this approach will result in novel medicines across a wide range of therapeutic areas.”

A copy of the corresponding abstract is available on the Journal of Labelled Compounds and Radiopharmaceuticals website. 

About Deuterium

Deuterium is a safe, non-radioactive relative of hydrogen that can be isolated from sea water and has been used extensively in human metabolic and clinical studies.  Since deuterium is an isotope of hydrogen, deuterium-containing compounds are expected to have similar pharmacological activity as their hydrogen analogs.  However, because deuterium is heavier than hydrogen, it forms a stronger chemical bond to carbon.  The stronger chemical bond obtained by selective deuterium modification may, in certain cases, substantially improve the drug’s metabolic properties, potentially resulting in better safety, tolerability and/or efficacy. 

About Concert

Concert Pharmaceuticals is a clinical stage biotechnology company focused on applying the company’s DCE Platform™ (deuterated chemical entity platform) to create novel and differentiated small molecule drugs. Concert’s approach leverages decades of pharmaceutical and clinical experience to reduce the time, risk and expense needed to create important new medicines.  The Company has a broad research pipeline encompassing many therapeutic areas including antiviral disease, renal disease and CNS disorders, among others.  Founded in 2006, Concert has raised more than $110 million of venture and institutional capital.  For more information on Concert Pharmaceuticals, please visit www.concertpharma.com.

Concert Pharmaceuticals, the CoNCERT logo and the DCE Platform are trademarks of Concert Pharmaceuticals, Inc.

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