RenaSci Consultancy Ltd, BioCity, Nottingham, UK.
Br J Pharmacol. 2011 Oct;164(4):1248-62. doi: 10.1111/j.1476-5381.2011.01245.x.
The global incidence of obesity continues to rise and is a major driver of morbidity and mortality through cardiovascular and cerebrovascular diseases. Animal models used in the discovery of novel treatments for obesity range from straightforward measures of food intake in lean rodents to long-term studies in animals exhibiting obesity due to the continuous access to diets high in fat. The utility of these animal models can be extended to determine, for example, that weight loss is due to fat loss and/or assess whether beneficial changes in key plasma parameters (e.g. insulin) are evident. In addition, behavioural models such as the behavioural satiety sequence can be used to confirm that a drug treatment has a selective effect on food intake. Typically, animal models have excellent predictive validity whereby drug-induced weight loss in rodents subsequently translates to weight loss in man. However, despite this, at the time of writing orlistat (Europe; USA) remains the only drug currently marketed for the treatment of obesity, with sibutramine having recently been withdrawn from sale globally due to the increased incidence of serious, non-fatal cardiovascular events. While the utility of rodent models in predicting clinical weight loss is detailed, the review also discusses whether animals can be used to predict adverse events such as those seen with recent anti-obesity drugs in the clinic.
肥胖的全球发病率持续上升,通过心血管和脑血管疾病成为发病率和死亡率的主要驱动因素。在发现肥胖症新疗法的动物模型中,从简单测量瘦老鼠的食物摄入量,到因长期连续食用高脂肪饮食而导致肥胖的动物的长期研究,范围广泛。这些动物模型的用途可以扩展,例如,确定体重减轻是由于脂肪减少和/或评估关键血浆参数(例如胰岛素)是否有明显的有益变化。此外,还可以使用行为模型,例如行为饱食序列,来确认药物治疗对食物摄入有选择性影响。通常,动物模型具有出色的预测有效性,即啮齿动物的药物诱导性体重减轻随后转化为人类的体重减轻。然而,尽管如此,在撰写本文时,奥利司他(欧洲;美国)仍然是唯一一种目前用于治疗肥胖症的药物,而西布曲明由于严重的非致命性心血管事件发生率增加,已在全球范围内停止销售。虽然详细介绍了啮齿动物模型在预测临床体重减轻方面的用途,但本文还讨论了动物是否可用于预测临床中最近的抗肥胖药物出现的不良事件。