Therapy Areas: Inflammatory Diseases
Concert Pharmaceuticals Presents Preclinical Data on CTP-692, a Novel Drug Candidate for Schizophrenia, Supporting Potential to Improve Safety Profile of D-Serine
8 November 2018 - - US-based biopharmaceutical company Concert Pharmaceuticals, Inc. (NASDAQ: CNCE) has presented preclinical results that support the potential of CTP-692, the company's novel drug candidate for schizophrenia, to improve the safety profile of D-serine, the company said.

CTP-692 is a deuterated form of D-serine, an endogenous co-agonist of the N-methyl-D-aspartate receptor.

In preclinical evaluation, Concert demonstrated that selective deuterium modification resulted in increased exposure of CTP-692 compared to a similar dose of D-serine.

Unlike D-serine, CTP-692 did not cause undesirable changes in important markers of kidney function.

These findings will be presented as a poster at the American College of Toxicology 2018 annual meeting being held November 4-7, 2018 in West Palm Beach, FL.

In preclinical evaluation, CTP-692 and D-serine were shown to have similar functional activation of the NMDA receptor in the presence of glutamate.

Relative to D-serine, CTP-692 showed increased metabolic stability in the preclinical study.

CTP-692 provided greater exposure, based on area under the curve analysis, and a longer half-life than corresponding doses of D-serine in vivo.

Notably, in animal models, serum creatinine and blood urea nitrogen, important markers of kidney function, were highly elevated upon acute dosing with D-serine but stayed within the normal range with CTP-692.

CTP-692 is a deuterium-modified analog of endogenous D-serine.

Based on documented effects of D-serine, the company is pursuing the development of CTP-692 as a treatment of schizophrenia by potentially restoring NMDA receptor activity in key disease-related areas of the brain.

CTP-692 is expected to have similar pharmacology to D-serine with the potential for an improved safety profile and improved clinical outcomes in the treatment of schizophrenia.

Concert is developing CTP-692 as an adjunctive therapy administered in addition to standard antipsychotic medicines with the potential to improve both positive and negative symptoms as well as cognitive function in patients with schizophrenia.

There is an extensive body of evidence supporting NMDA receptor hypofunction as a key underlying mechanism of schizophrenia.

The NMDA receptor comprises two binding domains and, in addition to requiring glutamate binding, activation with a co-agonist such as D-serine or glycine is necessary for NMDA receptor activation. D-serine is the most important human NMDA synaptic co-agonist.

It has been postulated for some time that administration of NMDA co-agonists could benefit patients with schizophrenia since there is evidence that plasma and cerebrospinal fluid levels of endogenous D-serine are reduced in patients with schizophrenia.

Concert Pharmaceuticals is a clinical stage biopharmaceutical company focused on applying its DCE Platform(deuterated chemical entity platform) to create novel medicines designed to treat serious diseases and address unmet patient needs.

The company's approach starts with previously studied compounds, including approved drugs, in which deuterium substitution has the potential to enhance clinical safety, tolerability or efficacy.

Concert has a broad pipeline of innovative medicines targeting autoimmune and inflammatory diseases and central nervous systems disorders.
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