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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

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Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
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Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

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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.
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...
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Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

126
Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
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Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
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Positioning Imatinib for Pulmonary Arterial Hypertension: A Dose-Finding Phase 2 Study.

Alexander M K Rothman1,2, Sofia Villar3,4, Jennifer Middleton1,2

  • 1Sheffield Pulmonary Vascular Disease Unit, Royal Hallamshire Hospital, Sheffield Teaching Hospitals NHS Foundation Trust, Sheffield, United Kingdom.

American Journal of Respiratory and Critical Care Medicine
|March 13, 2025
PubMed
Summary

A 200 mg daily dose of oral imatinib is safe and effective for treating pulmonary arterial hypertension. This dose reduced pulmonary vascular resistance and was well-tolerated by patients.

Keywords:
adaptive trial designimplanted hemodynamic sensorsremote monitoring

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Area of Science:

  • Cardiology
  • Pharmacology
  • Pulmonology

Background:

  • Imatinib (400 mg daily) shows efficacy in pulmonary arterial hypertension (PAH) but has safety concerns.
  • A lower, well-tolerated dose is needed for PAH treatment.

Purpose of the Study:

  • To determine a safe and tolerated oral imatinib dose between 100 mg and 400 mg daily.
  • To evaluate the efficacy of this dose in PAH patients.

Main Methods:

  • A continuous reassessment dose-finding model was used for 17 PAH patients.
  • Imatinib doses ranged from 100 mg to 400 mg daily, with most patients receiving 200 mg.
  • Cardiopulmonary hemodynamics and physical activity were monitored.

Main Results:

  • The recommended starting dose was 200 mg daily, with nausea as the most common side effect.
  • Imatinib (200 mg daily) significantly reduced mean pulmonary artery pressure and total pulmonary resistance.
  • Reductions in total pulmonary resistance were dose-dependent and sustained after treatment cessation.

Conclusions:

  • Oral imatinib, 200 mg daily, is a well-tolerated add-on therapy for pulmonary arterial hypertension.
  • Imatinib treatment led to sustained improvements in cardiopulmonary hemodynamics.
  • A delayed return to baseline hemodynamics was observed post-imatinib withdrawal.