Istaroxime is a novel intravenous agent with luso-inotropic properties that acts by inhibition of Na( )/K( ) adenosine triphosphatase and stimulation of sarco/ endoplasmic reticulum calcium ATPase isoform 2. It is significantly decreased left ventricular end-diastolic pressure, pulmonary capillary wedge pressure, heart rate and increased systolic blood pressure and cardiac index with no change in neurohormones, renal function or troponin I. Istaroxime has successfully concluded phase II clinical trials in cardiac failure patients. Istaroxime induced apoptosis, affected the key proliferative and apoptotic mediators c-Myc and caspase-3 and modified actin cytoskeleton dynamics and RhoA activity in prostate cancer cells – this provides novel insights into the anti-cancer properties of istaroxime further supporting the development of this agent as a novel anti-cancer drug candidate.
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
14.46 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17239705/ |
0.5 μg/kg/min 1 times / hour single, intravenous dose: 0.5 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered: |
ISTAROXIME plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
90.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17239705/ |
5 μg/kg/min single, intravenous dose: 5 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered: |
ISTAROXIME plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
18.3 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17239705/ |
5 μg/kg/min single, intravenous dose: 5 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered: |
ISTAROXIME plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
16.6 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17239705/ |
3.33 μg/kg/min single, intravenous dose: 3.33 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered: |
ISTAROXIME plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
Disc. AE: Arrhythmia, Nausea... Other AEs: Cardiac failure, ventricular tachycardia... AEs leading to discontinuation/dose reduction: Arrhythmia (2.5%) Other AEs:Nausea (2.5%) vomiting (2.5%) Cardiac failure (17.5%) Sources: ventricular tachycardia (17.5%) Infusion site pain (32.5%) arrhythmia (17.5%) atrial fibrillatio (17.5%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Cardiac failure | 17.5% | 1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| arrhythmia | 17.5% | 1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| atrial fibrillatio | 17.5% | 1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| ventricular tachycardia | 17.5% | 1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| Arrhythmia | 2.5% Disc. AE |
1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| Nausea | 2.5% Disc. AE |
1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| vomiting | 2.5% Disc. AE |
1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
| Infusion site pain | 32.5% | 1 ug/kg/min single, intravenous (unknown) Studied dose Dose: 1 ug/kg/min Route: intravenous Route: single Dose: 1 ug/kg/min Sources: |
unhealthy, ADULT n = 40 Health Status: unhealthy Condition: acute heart failure Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 40 Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Sarcoendoplasmic reticulum Ca(2+) ATPase. A critical target in chlorine inhalation-induced cardiotoxicity. | 2015 Apr |
|
| Functional characterization and anti-cancer action of the clinical phase II cardiac Na+/K+ ATPase inhibitor istaroxime: in vitro and in vivo properties and cross talk with the membrane androgen receptor. | 2016 Apr 26 |
|
| Istaroxime, a potential anticancer drug in prostate cancer, exerts beneficial functional effects in healthy and diseased human myocardium. | 2017 Jul 25 |
Patents
Sample Use Guides
0.5 or 1.0 or 1.5 ug/kg body weight/minute for six hours
Route of Administration:
Intravenous
| Substance Class |
Mixture
Created
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admin
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Edited
Sat Dec 16 15:41:37 UTC 2023
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N24U08609A
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Validated (UNII)
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72941813
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DBSALT001993
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374559-48-5
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N24U08609A
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