A selective Kappa opioid receptor (KOR) antagonist that may affect stress, mood and addiction


Targeting Depression and Addiction

CERC-501 is an oral, potent and selective kappa opioid receptor, or KOR, antagonist being developed as an adjunctive treatment of major depressive disorder (MDD) and secondarily for substance use disorders (e.g., nicotine, alcohol and/or cocaine).

of CERC-501

  • KOR system plays a key role in stress, mood and addictive disorders
  • Exposure to stress and addiction to substances causes KOR upregulation in the brain
  • KOR antagonists improve mood and reduce symptoms of nicotine and drug withdrawal

About MDD

Depression is one of the most common serious medical and psychiatric disorders

Numerous studies have shown that many patients do not respond to their initial antidepressant therapy. For example, according to a 2006 report funded by the NIMH and titled “Acute and Longer-Term Outcomes in Depressed Outpatients Requiring One of Several Treatment Steps: A STAR-D Report”, or the STAR-D Report, 51.4% of patients failed to respond, defined as achieving a 50% reduction in symptoms, and only 36.8% became symptom free, or achieved remission, after their initial 12-week treatment course with monoamine antidepressants. As such, physicians commonly will switch patients' antidepressants to manage depression, and patients may require two or three courses of treatment, before achieving satisfactory relief. The depression may persist following a course of treatment and additional medications may need to be used adjunctively. These adjunctive agents may include atypical antipsychotics, like aripiprazole and quetiapine, or other agents such as buproprion, and lithium. While certain patients experience improvement in their depressive symptoms when these additional therapies are added to their existing treatments, many do not.

About Substance Abuse

Drug abuse is a major public health problem that impacts society on multiple levels

According to Results from the 2013 National Survey on Drug Use and Health, a survey conducted by the Substance Abuse and Mental Health Services Administration, in 2013, an estimated 21.6 million people in the U.S. aged 12 or older were classified with substance dependence or abuse in the past year based on criteria specified in the Diagnostic and Statistical Manual of Mental Disorders, 4th edition. Of these 21.6 million classified with dependence or abuse of both alcohol and illicit drugs, 4.3 million had dependence or abuse of illicit drugs but not alcohol, and 14.7 million had dependence or abuse of alcohol but not illicit drugs. Illicit drugs include marijuana/hashish, cocaine (including crack), heroin, hallucinogens, inhalants, or prescription‑type psychotherapeutics (pain relievers, tranquilizers, stimulants, and sedatives) used non-medically. Furthermore, in 2013, heavy drinking was reported by 6.3% of the U.S. population aged 12 or older or 16.5 million people. Cigarette smoking and exposure to tobacco smoke are the leading causes of preventable disease and death in the U.S., resulting in more than 480,000 premature deaths and $289 billion in direct health care expenditures and productivity losses each year. In 2013, 55.8 million people (21.3% of the population) were current cigarette smokers. Despite progress over the past several decades, millions of adults still smoke cigarettes, the most commonly used tobacco product in the United States, and this continues to be a major public health problem.

Mechanism of Action

Selective kappa opioid receptor (KOR) antagonist

Kappa opioid receptor (KOR) antagonists, including CERC-501, have demonstrated efficacy in multiple mood and addiction animal models, and been shown to reduce addictive behavior with all major classes of abused substances. This new mechanism is unique in that it possesses anti-depressant-like, anti-stress-like and anxiolytic-like effects.