J.K.K. Nattraja College of Pharmacy, Kumarapalayam 638183, India.
College of Pharmacy, King Khalid University, Guraiger, Abha 62529, Saudi Arabia.
Curr Mol Pharmacol. 2019;12(3):195-201. doi: 10.2174/1874467212666190111165015.
Diabetes mellitus and concomitant dyslipidemia, being referred to as 'diabetic dyslipidemia', are the foremost detrimental factors documented to play a pivotal role in cardiovascular illness. Diabetic dyslipidemia is associated with insulin resistance, high plasma triglyceride levels, low HDL-cholesterol concentration and elevated small dense LDL-cholesterol particles. Maintaining an optimal glucose and lipid levels in patients afflicted with diabetic dyslipidemia could be a major task that might require a well-planned diet-management system and regular physical activity, or otherwise an intake of combined antidiabetic and antihyperlipidemic medications. Synchronized treatment which efficiently controls insulin resistance-associated diabetes mellitus and co-existing dyslipidemia could indeed be a fascinating therapeutic option in the management of diabetic dyslipidemia. Peroxisome proliferator-activated receptors α/γ (PPARα/γ) dual agonists are such kind of drugs which possess therapeutic potentials to treat diabetic dyslipidemia. Nevertheless, PPARα/γ dual agonists like muraglitazar, naveglitazar, tesaglitazar, ragaglitazar and aleglitazar have been reported to have undesirable adverse effects, and their developments have been halted at various stages. On the other hand, a recently introduced PPARα/γ dual agonist, saroglitazar is an emerging therapeutic agent of glitazar class approved in India for the management of diabetic dyslipidemia, and its treatment has been reported to be generally safe and well tolerated.
Some additional and new compounds, at initial and preclinical stages, have been recently reported to possess PPARα/γ dual agonistic potentials with considerable therapeutic efficacy and reduced adverse profile. This review sheds light on the current status of various PPARα/γ dual agonists for the management of diabetic dyslipidemia.
糖尿病和随之而来的血脂异常，被称为“糖尿病血脂异常”，是心血管疾病中最重要的致病因素。糖尿病血脂异常与胰岛素抵抗、高血浆甘油三酯水平、低高密度脂蛋白胆固醇浓度和升高的小而密低密度脂蛋白胆固醇颗粒有关。对于患有糖尿病血脂异常的患者，维持最佳的血糖和血脂水平可能是一项艰巨的任务，这可能需要一个精心策划的饮食管理系统和定期的体育活动，或者需要服用联合的降糖和调脂药物。同步治疗能有效控制与胰岛素抵抗相关的糖尿病和并存的血脂异常，这确实是治疗糖尿病血脂异常的一种有吸引力的治疗选择。过氧化物酶体增殖物激活受体 α/γ（PPARα/γ）双重激动剂就是这样一种药物，具有治疗糖尿病血脂异常的潜力。然而，PPARα/γ双重激动剂，如 muraglitazar、naveglitazar、tesaglitazar、ragaglitazar 和 aleglitazar，已被报道具有不良的不良反应，其开发已在不同阶段停止。另一方面，最近推出的 PPARα/γ 双重激动剂 saroglitazar 是一种新型的 glitazar 类药物，已在印度获得批准用于治疗糖尿病血脂异常，其治疗被报道通常是安全且耐受良好的。
一些新的和新的化合物，在初始和临床前阶段，最近被报道具有 PPARα/γ 双重激动剂的潜力，具有相当的治疗效果和降低的不良反应谱。这篇综述介绍了目前用于治疗糖尿病血脂异常的各种 PPARα/γ 双重激动剂的现状。
