Related Experiment Video
Updated: Jul 25, 2025
Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Repurposing of the Drug Tezosentan for Cancer Therapy
Eduarda Ribeiro1,2,3, Nuno Vale1,2,4
1OncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, Portugal.
Abstract:
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 ETA and ETB 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.
Insights
Tezosentan, a vasodilator, shows promise in oncology by targeting endothelin receptors on cancer cells. This drug repurposing strategy may overcome resistance to existing cancer therapies.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Tezosentan is a vasodilator developed for pulmonary arterial hypertension.
- It inhibits endothelin (ET) receptors (ETA and ETB), which are overexpressed in various cancer cells.
- Endothelin-1 (ET1) causes vasoconstriction and is implicated in cancer progression.
Purpose of the Study:
- To review the potential of tezosentan as an anticancer agent.
- To explore drug repurposing for enhancing antineoplastic therapies.
- To highlight tezosentan's mechanism against cancer-related cellular processes.
Main Methods:
- Literature review of tezosentan's pharmacology and anticancer properties.
- Analysis of endothelin receptor involvement in cancer biology.
- Evaluation of drug repurposing strategies in oncology.
Main Results:
- Tezosentan targets ET receptors, inhibiting cancer cell proliferation, survival, and neovascularization.
- It may improve blood flow and reduce cardiac workload.
- Tezosentan demonstrates potential in overcoming drug resistance in cancer treatment.
Conclusions:
- Tezosentan exhibits anticancer properties through endothelin receptor antagonism.
- Drug repurposing of tezosentan offers a novel approach to cancer therapy.
- Further research is warranted to establish tezosentan's efficacy in oncology.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:49Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
02:56Treatment Resistant Cancers