An up-to-date evaluation of lorcaserin hydrochloride for the treatment of obesity

ABSTRACT

Introduction: Obesity is a chronic disease caused by dysfunctional neurohormonal systems that result in excess weight, adiposopathy, and increased risk for many comorbidities including cardiovascular disease, type 2 diabetes, and certain types of cancer. Lorcaserin is a serotonergic agonist specific to the 5HT2C receptor that is FDA-approved for the long-term management of obesity in adults with BMI>30 kg/m2 or BMI>27 kg/m2 and at least one weight-related comorbidity.

Areas covered: The authors review the pharmacodynamics and pharmacokinetic properties of lorcaserin alongside updates on serotonin’s mechanism of action in the central nervous system. The efficacy of lorcaserin in the management of obesity, its related comorbidities, and potential therapeutic applications are also discussed.

Expert opinion: The future of obesity management requires a multimodal and personalized approach. The high medical complexity of patients warrants polypharmacotherapy to achieve their metabolic goals. Lorcaserin has proven efficacy and safety in the treatment of obesity and its weight-related comorbidities including type 2 diabetes, cardiovascular disease, and chronic kidney disease. New evidence elucidating its effects on dopaminergic pathways and on glucose homeostasis expands its prospective uses.

KEYWORDS:

• Lorcaserin
• obesity
• weight
• serotonin
• anti-obesity medication
• 5-HT2CR
• 5-HT2CR agonist
• serotonin receptor
• weight loss
• weight management

Article highlights

• In combination with lifestyle modifications, lorcaserin induces an average placebo-subtracted weight loss of about 3%

• Lorcaserin's beneficial effect on glycemic parameters appears to be independent of weight loss

• Safety issues regarding valvulopathy have not manifested in randomized controlled trials

• Data from the CAMELLIA trial demonstrates lorcaserin's safety in patients at high-risk for CVD and in patients with CKD

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

One referee has disclosed that they are an employee of InterVivo Solutions. Peer reviewers on this manuscript have no other relevant financial relationships or otherwise to disclose.

Additional information

Funding

This manuscript has not been funded.