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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3901 |
2.5 nM [EC50] | ||
Target ID: Na+/K+-ATPase (dog) Sources: https://www.ncbi.nlm.nih.gov/pubmed/12388640 |
0.43 µM [IC50] | ||
Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27027435 |
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Target ID: map04210 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27027435 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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: |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00616161
0.5 or 1.0 or 1.5 ug/kg body weight/minute for six hours
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27027435
Istaroxime (5 uM) over a period of 24 hours increased the number of apoptotic cells in DU145 prostate cancer cells culture from 9.48% in control samples to 46.54% following treatment.
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DBSALT001993
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N24U08609A
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All of the following components must be present:
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SUBSTANCE RECORD