Rubin Lewis J, Roux Sébastien
Division of Pulmonary & Critical Care Medicine, Department of Medicine, University of California at San Diego, School of Medicine, 9300 Campus Point Drive, 7372, La Jolla, CA 92037, USA.
Expert Opin Investig Drugs. 2002 Jul;11(7):991-1002. doi: 10.1517/13543784.11.7.991.
The peptide endothelin plays a significant role in a wide array of pathological conditions, including primary pulmonary hypertension and pulmonary arterial hypertension associated with collagen vascular disease. These are life-threatening conditions that can severely compromise the function of the lungs and heart. Inhibiting the actions of endothelin by blockade of its receptors provides a new and effective approach to therapy for patients with these conditions. Bosentan (Tracleer ) is the first orally-active dual endothelin receptor antagonist and has recently been approved in the US, Canada, Switzerland and the EU for the treatment of pulmonary arterial hypertension. Bosentan significantly improves exercise capacity, symptoms and functional status in patients with this disease and also slows clinical deterioration, which may be indicative of a delay of disease progression. Results from large-scale studies of bosentan in patients with pulmonary arterial hypertension and chronic heart failure have established its long-term safety and tolerability profiles. The introduction of the dual endothelin receptor antagonist bosentan has provided an essential treatment for pulmonary arterial hypertension and ongoing trials are evaluating its potential role in the management of other endothelin-mediated disease states.
肽内皮素在多种病理状况中发挥着重要作用，包括原发性肺动脉高压以及与胶原血管病相关的肺动脉高压。这些都是危及生命的病症，会严重损害肺和心脏的功能。通过阻断内皮素受体来抑制其作用，为患有这些病症的患者提供了一种新的有效治疗方法。波生坦（全可利）是首个口服活性双内皮素受体拮抗剂，最近已在美国、加拿大、瑞士和欧盟获批用于治疗肺动脉高压。波生坦可显著改善该病患者的运动能力、症状和功能状态，还能减缓临床恶化，这可能表明疾病进展得到了延缓。在肺动脉高压和慢性心力衰竭患者中进行的波生坦大规模研究结果已确定了其长期安全性和耐受性。双内皮素受体拮抗剂波生坦的推出为肺动脉高压提供了重要治疗手段，正在进行的试验正在评估其在管理其他内皮素介导的疾病状态中的潜在作用。
