lorcaserin and Mood-Disorders

The serotonin 5-HT2C receptor is a G-protein-coupled receptor and is one of the 14 subtypes that constitutes the serotonin receptor family. Agonists of 5-HT2C have been implicated as potential treatments for diseases of significant unmet medical need, including obesity and schizophrenia. Despite approximately 10 years of discovery efforts, 5-HT2C agonists have only recently advanced into the clinic, likely because many of the early drug discovery efforts experienced significant difficulties with attaining receptor selectivity. Several of these issues related to receptor selectivity have now been overcome, resulting in the entry of compounds into advanced clinical trials. This review summarizes the progress in 5-HT2C agonist discovery and clinical development over the last 3 years. [sw1]what are the several issues - several issues relating to receptor selectivity?

Topics: Animals; Anti-Obesity Agents; Antipsychotic Agents; Benzazepines; Drug Design; Drug Evaluation, Preclinical; Humans; Molecular Structure; Mood Disorders; Obesity; Ocular Hypertension; Receptor, Serotonin, 5-HT2C; Serotonin 5-HT2 Receptor Agonists; Serotonin Receptor Agonists; Treatment Outcome

Compared to the general population, individuals with psychiatric illness, especially serious and chronic mood and psychotic disorders, are more likely to be overweight or obese, have higher rates of weight-related medical conditions, and have greater non-suicide mortality rates. Lorcaserin (Belviq(®)), phentermine/topiramate combination (Qsymia(®)), and bupropion/naltrexone combination have been demonstrated to be effective for the treatment of obesity, as an adjunct to a reduced-calorie diet and physical activity, although their absolute safety has yet to be established with more widespread use or longer use. Bariatric surgery is an effective approach for morbid obesity, but careful psychiatric assessment before and follow up after surgery is necessary. Behavioral lifestyle interventions to promote weight loss are effective and should be implemented along with or instead of drug therapies or surgery.

Topics: Animals; Appetite Depressants; Bariatric Surgery; Benzazepines; Bupropion; Chronic Disease; Combined Modality Therapy; Diet, Reducing; Disease Models, Animal; Drug Combinations; Exercise; Fructose; Humans; Mood Disorders; Naltrexone; Obesity; Overweight; Phentermine; Psychotic Disorders; Randomized Controlled Trials as Topic