Tezosentan. Actelion/Genentech

Enrico Rossetti1, Stefano De Servi

  • 1UO Cardiologia, Ospedale Civile di Legnano 20025 Legano, Milan, Italy.

Current Opinion in Investigational Drugs (London, England : 2000)
|May 9, 2003
PubMed

Insights

Tezosentan, an endothelin receptor antagonist, showed disappointing results in a Phase III acute heart failure trial. A new study using lower doses was planned, with results anticipated by early 2005.

Area of Science:

  • Cardiovascular medicine
  • Pharmacology

Background:

  • Tezosentan is an endothelin receptor antagonist developed for cardiovascular disorders.
  • Acute heart failure (AHF) and congestive heart failure are target conditions.

Purpose of the Study:

  • To evaluate the efficacy and safety of tezosentan in AHF patients.
  • To assess mortality and morbidity in a Phase III trial.

Main Methods:

  • A Phase III clinical study was conducted in AHF patients.
  • Lower doses of tezosentan were planned for a subsequent Phase III study following initial disappointing results.

Main Results:

  • Initial Phase III trial results for tezosentan in AHF were disappointing.
  • A new Phase III study was planned with adjusted dosing.

Conclusions:

  • Further investigation with modified dosing was deemed necessary for tezosentan in AHF.
  • Clinical trial outcomes guide the development of cardiovascular therapies.

Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

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 (ECE). Of...
Gene Therapy01:22

Gene Therapy

Gene therapy is a technique where a gene is inserted into a person’s cells to prevent or treat a serious disease. The added gene may be a healthy version of the gene that is mutated in the patient, or it could be a different gene that inactivates or compensates for the patient’s disease-causing gene. For example, in patients with severe combined immunodeficiency (SCID) due to a mutation in the gene for the enzyme adenosine deaminase, a functioning version of the gene can be inserted. The...
Gene Therapy01:22

Gene Therapy

Gene therapy is a technique where a gene is inserted into a person’s cells to prevent or treat a serious disease. The added gene may be a healthy version of the gene that is mutated in the patient, or it could be a different gene that inactivates or compensates for the patient’s disease-causing gene. For example, in patients with severe combined immunodeficiency (SCID) due to a mutation in the gene for the enzyme adenosine deaminase, a functioning version of the gene can be inserted. The...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

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...