Oral
lorcaserin (
BELVIQ(®)), a selective
serotonin 5-HT2C receptor agonist, is indicated in the US as an adjunct to diet and exercise in the chronic weight management of obese adults, or
overweight adults with at least one weight-related comorbidity (e.g. dyslipidaemia,
hypertension,
type 2 diabetes). This article reviews the pharmacological properties, therapeutic efficacy and tolerability of oral
lorcaserin in this patient population. In three large randomized, double-blind, multicentre studies, oral
lorcaserin was more effective than placebo in the management of obese and
overweight adults with or without
type 2 diabetes mellitus. Following 12 months'
therapy, significantly higher proportions of
lorcaserin than placebo recipients achieved a ≥5 and ≥10 % reduction from baseline in their bodyweight and a significant between-group difference favouring
lorcaserin over placebo was observed for the change from baseline in bodyweight. Moreover, among patients who had achieved a ≥5 % reduction in their bodyweight after 12 months'
therapy with
lorcaserin, a significantly higher proportion who received
lorcaserin for a further 12 months than those who switched to placebo maintained ≥5 %
weight loss at 24 months. In general, oral
lorcaserin was well tolerated in clinical studies, with hypoglycaemia and
headache the most frequently reported adverse events in those with or without
type 2 diabetes, respectively. According to a pooled analysis, the risk of US-FDA-defined valvulopathy with
lorcaserin is generally low and not statistically significantly different from placebo. From these and other data, the FDA has concluded that
lorcaserin is unlikely to elevate the risk of valvulopathy.