| Istaroxime, a first in class new chemical entity exhibiting SERCA-2 activation and Na-K-ATPase inhibition: a new promising treatment for acute heart failure syndromes? | |
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MedLine Citation:
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PMID: 19238540 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Acute heart failure syndromes (AHFS) are associated with the rapid onset of heart failure (HF) signs and symptoms. Hospitalizations for AHFS continue to rise and are associated with significant mortality and morbidity. Several pharmacological agents are currently approved for the treatment of AHFS, but their use is associated with an increase in short-term mortality. There is a need for new agents that can be given in the acute setting with increased efficacy and safety. Istaroxime is a unique agent with both inotropic and lusitropic properties which is currently being studied for the treatment of AHFS. Istaroxime inhibits the sodium-potassium adenosine triphosphatase (ATPase) and stimulates the sarcoplasmic reticulum calcium ATPase isoform 2 (SERCA-2) thereby improving contractility and diastolic relaxation. Early data from human studies reveal that istaroxime decreases pulmonary capillary wedge pressure (PCWP) and possibly improves diastolic function without causing a significant change in heart rate (HR), blood pressure, ischemic or arrhythmic events. Most commonly reported side effects were related to gastrointestinal intolerance and were dose related. In conclusion, istaroxime is a novel agent being investigated for the treatment of AHFS whose mechanism of action and cellular targets make it a promising therapy. Further studies with longer infusion times in patients with hypotension are required to confirm its efficacy and safety. |
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Authors:
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Hashim Khan; Marco Metra; John E A Blair; Mark Vogel; Matthew E Harinstein; Gerasimos S Filippatos; Hani N Sabbah; Herve Porchet; Giovanni Valentini; Mihai Gheorghiade |
Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review Date: 2009-02-24 |
Journal Detail:
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Title: Heart failure reviews Volume: 14 ISSN: 1573-7322 ISO Abbreviation: Heart Fail Rev Publication Date: 2009 Dec |
Date Detail:
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Created Date: 2009-11-05 Completed Date: 2010-02-25 Revised Date: 2012-07-12 |
Medline Journal Info:
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Nlm Unique ID: 9612481 Medline TA: Heart Fail Rev Country: United States |
Other Details:
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Languages: eng Pagination: 277-87 Citation Subset: IM |
Affiliation:
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Northwestern University, Chicago, IL 60611, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Acute Disease Animals Cardiotonic Agents / administration & dosage, pharmacology*, therapeutic use* Dobutamine / pharmacology Etiocholanolone / administration & dosage, analogs & derivatives*, pharmacology, therapeutic use Heart Failure / drug therapy* Hemodynamics / drug effects Humans Pulmonary Wedge Pressure / drug effects Sarcoplasmic Reticulum Calcium-Transporting ATPases / drug effects* Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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0/3-((2-aminoethoxy)imino)androstane-6,17-dione; 0/Cardiotonic Agents; 34368-04-2/Dobutamine; 53-42-9/Etiocholanolone; EC 3.6.3.8/ATP2A2 protein, human; EC 3.6.3.8/Sarcoplasmic Reticulum Calcium-Transporting ATPases; EC 3.6.3.9/Sodium-Potassium-Exchanging ATPase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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