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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

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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...
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Drug Clearance: Overview01:06

Drug Clearance: Overview

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Drug elimination refers to drug removal from the body, either through urine or bile, by the kidneys or liver, respectively. A pharmacokinetic parameter, drug clearance, measures the efficiency of drug removal from the bloodstream within a specific time frame. It is calculated as the rate at which a drug is eliminated from plasma divided by the drug's concentration in plasma.
Drug clearance is not limited to renal excretion but encompasses all organs involved in drug elimination, including...
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Drug Administration and Therapy Phases: Overview01:26

Drug Administration and Therapy Phases: Overview

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Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
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Preclinical Development: Overview01:28

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Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...
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Prescription, Nonprescription and Orphan Drugs01:02

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Prescription drugs require a prescription from a medical practitioner and can only be obtained from a pharmacy. They have many applications, including treating pain, anxiety, and hypertension.
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Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

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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.
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Optimized LC-MS/MS Method for the High-throughput Analysis of Clinical Samples of Ivacaftor, Its Major Metabolites, and Lumacaftor in Biological Fluids of Cystic Fibrosis Patients
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Clazosentan: First Approval.

Arnold Lee1

  • 1Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. dru@adis.com.

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This summary is machine-generated.

Clazosentan is a new drug approved in Japan to prevent brain artery spasms after brain bleeds. This endothelin A receptor antagonist helps reduce related strokes and symptoms.

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Area of Science:

  • Neurology
  • Pharmacology
  • Cardiovascular Research

Background:

  • Subarachnoid hemorrhage frequently leads to cerebral vasospasm.
  • Cerebral vasospasm can cause ischemic stroke and neurological deficits.
  • Endothelin A receptor activation contributes to cerebral vasospasm.

Purpose of the Study:

  • To summarize the development of clazosentan.
  • To highlight milestones leading to its first approval.
  • To detail its use in preventing complications after aneurysmal subarachnoid hemorrhage.

Main Methods:

  • Review of clinical trial data (JapicCTI163369, JapicCTI163368).
  • Analysis of clazosentan's mechanism as an endothelin A receptor antagonist.
  • Summary of regulatory submission and approval process in Japan.

Main Results:

  • Clazosentan demonstrated efficacy in preventing cerebral vasospasm.
  • The drug also showed effectiveness in reducing vasospasm-related cerebral infarction.
  • Prevention of cerebral ischemic symptoms was observed with clazosentan treatment.

Conclusions:

  • Clazosentan is the first approved therapy for preventing cerebral vasospasm post-subarachnoid hemorrhage in Japan.
  • The drug's development signifies a therapeutic advance in managing aneurysmal subarachnoid hemorrhage complications.
  • Endothelin A receptor antagonism is a validated strategy for mitigating cerebral vasospasm.