Concert Pharmaceuticals Initiates CTP-347 Phase I Clinical Trial
News Sep 26, 2008
Concert Pharmaceuticals, Inc. announced has that it has initiated a Phase I study in healthy volunteers to evaluate the safety, tolerability and pharmacokinetics of CTP-347, a deuterium-containing serotonin modulator created by Concert researchers.
Concert intends to evaluate CTP-347 as a non-hormonal treatment for vasomotor symptoms (VMS or hot flashes) in patients with increased risk of adverse effects due to, or contraindicated to using, hormone therapy, as well as in the larger menopausal population. Results of this Phase I study are expected to be available in the first half of 2009.
“We are pleased to have advanced our first compound from concept to clinical testing in less than two years. We believe our deuterium chemistry platform holds great promise in creating novel compounds with superior safety and efficacy as compared to existing therapies. We look forward to advancing and introducing a number of first-in-class agents for unmet medical needs, of which CTP-347 is our first to enter the clinic,” said Roger Tung, Ph.D., President and Chief Executive Officer of Concert Pharmaceuticals.
CTP-347 is Concert’s first compound to advance into clinical trials. CTP-347 is a new chemical entity developed from Concert’s deuterium chemistry platform by replacing key hydrogen atoms of paroxetine with deuterium. Paroxetine has been shown to be an effective treatment for VMS.
However, it is a potent and irreversible inactivator of CYP2D6 (cytochrome P450 2D6), a key liver enzyme responsible for the metabolism of many commonly-prescribed drugs.
In preclinical testing, CTP-347 demonstrated improved metabolic properties, significantly reducing CYP2D6 inhibition while preserving paroxetine’s pharmacological activity. Based on these results, Concert believes CTP-347 may avoid adverse interactions with many drugs, including tamoxifen and certain antiarrhythmics, beta-blockers, analgesics, and antipsychotics. The Company expects to investigate CTP-347’s drug-drug interaction profile as part of the Phase I study.
Currently, there is no FDA-approved non-hormonal treatment for VMS, a serious and sometimes long-term condition associated with a range of undesirable effects including depression, insomnia and lost productivity. Hormone replacement therapy can effectively treat VMS.
However, patients who currently or previously have been treated for cancers of the breast or ovary, or who have a familial history of these cancers, are often advised to avoid hormonal treatment. A non-hormonal therapy may also be preferred by women who experience VMS following menopause in whom hormone therapy is contraindicated or who have concerns about long-term health risks posed by hormone replacement therapy.