Concert Pharmaceuticals Announces Preclinical Results Suggesting Potential for Once Daily Dosing of Novel Oxazolidinone Antibiotic
Concert Pharmaceuticals, Inc. today announced findings from a preclinical study suggesting that C-20081, a novel, deuterium-containing oxazolidinone antibiotic, may be suitable for once-daily oral and intravenous dosing. In the preclinical study, C-20081 had a 43% increase in plasma half-life compared to linezolid, which might allow for lower overall drug exposure and improved tolerability with a once-daily dose. These findings were presented in a poster presentation at the 48th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) and the 46th Annual Meeting of the Infectious Diseases Society of America (IDSA), a joint meeting being held in Washington, DC.
“We are pleased to present our data on this potential best-in-class oxazolidinone antibiotic at the ICAAC/IDSA meeting,” stated Roger Tung, Ph.D., President and Chief Executive Officer of Concert Pharmaceuticals. “Based on our preclinical results, we believe that C-20081 warrants further investigation as a potential once-daily antibiotic for serious bacterial infections. These include methicillin-resistant staphylococcus aureus (MRSA), a virulent hospital and, increasingly, community-acquired infection with high rates of morbidity and mortality, as well as drug-resistant tuberculosis. With its pharmacokinetic profile, we believe C-20081 holds promise for improving patient compliance and thereby enhancing efficacy in both outpatient and long-term care settings.”
C-20081 is a novel compound in the same chemical class as linezolid developed from Concert’s deuterium chemistry platform. Linezolid is an FDA-approved antibiotic for the treatment of serious bacterial infections including MRSA, for which it is the only currently-approved oral therapy, and cSSSI (complicated skin and skin structure infection). Linezolid is approved both for oral and intravenous dosing at 600 mg every 12 hours.
Concert evaluated the effect of selective deuterium modification on linezolid’s metabolic and pharmacokinetic properties in primates. C-20081 demonstrated an I.V. half life of 6.3 hours, compared to 4.5 hours for linezolid. The human single-dose IV half-life of linezolid is reported to be 4.4 to 4.9 hours. Compared to linezolid, C-20081 had equal in vitro potency across hundreds of bacterial strains. Concert believes that the combination of potent anti-bacterial activity and long plasma half-life could result in a superior dosing profile.
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 resembles hydrogen, deuterium-containing compounds are expected to preserve the pharmacological activity of their hydrogen analogs. An important difference is that deuterium is heavier than hydrogen and therefore forms a stronger chemical bond. The stronger chemical bond obtained by selective deuterium modification in select instances might substantially improve the drug’s metabolic properties, potentially resulting in better safety, tolerability and efficacy.
Concert Pharmaceuticals, Inc. is a clinical stage biotechnology company dedicated to creating medically and commercially important new medicines through a novel approach utilizing the naturally-occurring element deuterium. Concert applies its innovative platform to create highly differentiated compounds based on well-understood biological targets and drug molecules, yielding a rich pipeline of new chemical entities (NCEs). By leveraging decades of pharmaceutical experience to design NCEs from proven therapies, Concert’s drug candidates have potential for first-in-class use in under-served medical conditions, as well as best-in-class efficacy and safety, while reducing R&D risk, time, and expense. The Company has over 100 patent applications for new drug candidates addressing a broad range of therapeutic areas, including vasomotor symptoms, HIV/AIDS and fibrotic diseases, among others. Since its inception in 2006, Concert has raised more than $96 million and has been financed by leading venture capitalists and institutional investors. A listing of Concert’s institutional shareholders and additional corporate information is available online at http://www.concertpharma.com. CoNCERT and CoNCERT Pharmaceuticals are trademarks of Concert Pharmaceuticals, Inc.