ANGPTL3 和 ApoC-III 抑制剂用于治疗高甘油三血症在背景下:马的课程?
Dick C Chan1, Gerald F Watts1,2
1Medical School, University of Western Australia.
Current opinion in lipidology
|February 19, 2024
概括
针对angiopoietin-like protein 3 (ANGPTL3) 和apolipoprotein C-III (apoC-III) 的新疗法有效地降低了过高甘油三血症 (HTG) 中的甘油三. 这些治疗方法有望降低动脉样硬化心血管疾病 (ASCVD) 风险.
科学领域:
- 心血管医学 心血管医学
- 代谢障碍 代谢障碍 代谢障碍
- 药理学 药理学是指药理学的学科.
背景情况:
- 过高甘油三血症 (HTG) 是动脉样硬化心血管疾病 (ASCVD) 的重要危险因素.
- 目前对HTG的治疗有局限性,这凸显了对更有效疗法的未满足需求.
- 血管蛋白样蛋白3 (ANGPTL3) 和阿波利波蛋白C-III (apoC-III) 是三甘油丰富的脂蛋白 (TRL) 代谢的关键调节者.
研究的目的:
- 审查最近的临床试验,评估针对HTG的新疗法,针对ANGPTL3和apoC-III.
- 评估ANGPTL3和apoC-III抑制在管理HTG中的有效性和潜在机制.
- 讨论这些新药对ASCVD风险降低的影响.
主要方法:
- 最近的临床试验综述,涉及单克隆抗体和基于核酸的疗法 (抗意义寡核酸,小干扰RNA).
- 对抗ANGPTL3和apoC-III抑制对血甘油三,TRL,LDL胆固醇和apoB水平的影响数据的分析.
- 对降低甘油三的潜在机制的评估,包括对TRL生产和代谢的影响.
主要成果:
- ANGPTL3和apoC-III的抑制剂在降低血甘油三和TRL方面表现出显著的有效性.
- 与ANGPTL3抑制相比,抑制apoC-III可能具有更大的降甘油三效应.
- 抑制ANGPTL3有效降低LDL胆固醇和apoB,而抑制apoC-III对这些参数的影响很小或不存在.
结论:
- 针对ANGPTL3和apoC-III的新型药物代表了纠正HTG的有希望的治疗策略.
- 这些新型疗法有可能降低HTG患者的ASCVD风险.
- 长期的安全性和成本效益需要在正在进行的和未来的研究中进行进一步的调查.
相关概念视频
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
181
Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
181
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
523
Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
523
Lipid-Lowering Drugs: Statins and Miscellaneous Agents
661
Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
661
Dipeptidyl Peptidase 4 Inhibitors
187
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
187
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
175
α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
Acarbose and miglitol are...
175
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
165
Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
165


