Ribeiro Eduarda, Vale Nuno
OncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, Portugal.
CINTESIS@RISE, Faculty of Medicine, University of Porto, Alameda Professor Hernâni Monteiro, 4200-319 Porto, Portugal.
Curr Issues Mol Biol. 2023 Jun 11;45(6):5118-5131. doi: 10.3390/cimb45060325.
Tezosentan is a vasodilator drug that was originally developed to treat pulmonary arterial hypertension. It acts by inhibiting endothelin (ET) receptors, which are overexpressed in many types of cancer cells. Endothelin-1 (ET1) is a substance produced by the body that causes blood vessels to narrow. Tezosentan has affinity for both ET and ET receptors. By blocking the effects of ET1, tezosentan can help to dilate blood vessels, improve the blood flow, and reduce the workload on the heart. Tezosentan has been found to have anticancer properties due to its ability to target the ET receptors, which are involved in promoting cellular processes such as proliferation, survival, neovascularization, immune cell response, and drug resistance. This review intends to demonstrate the potential of this drug in the field of oncology. Drug repurposing can be an excellent way to improve the known profiles of first-line drugs and to solve several resistance problems of these same antineoplastic drugs.
替唑生坦是一种血管扩张剂药物，最初开发用于治疗肺动脉高压。它通过抑制内皮素（ET）受体发挥作用，内皮素受体在多种癌细胞中过度表达。内皮素-1（ET1）是身体产生的一种使血管变窄的物质。替唑生坦对ET和ET受体均有亲和力。通过阻断ET1的作用，替唑生坦有助于扩张血管、改善血流并减轻心脏负担。由于替唑生坦能够靶向参与促进细胞增殖、存活、新血管形成、免疫细胞反应和耐药性等细胞过程的ET受体，已发现其具有抗癌特性。本综述旨在证明这种药物在肿瘤学领域的潜力。药物重新利用可能是改善一线药物已知特性并解决这些抗肿瘤药物若干耐药问题的绝佳方法。
