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levosimendan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| cardiac stimulants, pimobendan derivatives | 1576 | 141505-33-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A hydrazone and pyridazine derivative; the levo-form is a phosphodiesterase III inhibitor, calcium-sensitizing agent, and inotropic agent that is used in the treatment of HEART FAILURE.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 11 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 85 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.24 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.02 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.10 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT2,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MARK4,MELK,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM1,PIM2,PIM3,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 64 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK9,EIF2AK3,GRK2,MAP2K6,MAP3K14,MAPK7,STK33,TEK,TTK | 11 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Lymphatic fistula | 213.77 | 102.87 | 37 | 2599 | 1424 | 90624387 |
| Femoral hernia incarcerated | 212.60 | 102.87 | 37 | 2599 | 1471 | 90624340 |
| Wound infection pseudomonas | 201.74 | 102.87 | 37 | 2599 | 1986 | 90623825 |
| Pancreatic steatosis | 196.17 | 102.87 | 35 | 2601 | 1607 | 90624204 |
| Arterial haemorrhage | 193.58 | 102.87 | 37 | 2599 | 2486 | 90623325 |
| Seroma | 180.43 | 102.87 | 36 | 2600 | 3024 | 90622787 |
| Haemarthrosis | 170.87 | 102.87 | 36 | 2600 | 3958 | 90621853 |
| Aortic valve stenosis | 168.72 | 102.87 | 36 | 2600 | 4204 | 90621607 |
| Tachyarrhythmia | 160.01 | 102.87 | 36 | 2600 | 5370 | 90620441 |
| Hepatic cyst | 158.30 | 102.87 | 37 | 2599 | 6531 | 90619280 |
| Diverticulum intestinal | 156.09 | 102.87 | 39 | 2597 | 9103 | 90616708 |
| Eructation | 154.19 | 102.87 | 40 | 2596 | 10842 | 90614969 |
| Wound dehiscence | 151.99 | 102.87 | 35 | 2601 | 5787 | 90620024 |
| Faecaloma | 146.13 | 102.87 | 38 | 2598 | 10393 | 90615418 |
| Inflammatory marker increased | 145.85 | 102.87 | 37 | 2599 | 9177 | 90616634 |
| Groin pain | 144.88 | 102.87 | 39 | 2597 | 12174 | 90613637 |
| Aortic arteriosclerosis | 142.33 | 102.87 | 35 | 2601 | 7649 | 90618162 |
| Cardiovascular disorder | 136.44 | 102.87 | 38 | 2598 | 13454 | 90612357 |
| Cardiogenic shock | 134.41 | 102.87 | 43 | 2593 | 24425 | 90601386 |
| Left ventricular dysfunction | 133.29 | 102.87 | 38 | 2598 | 14631 | 90611180 |
| Postoperative wound infection | 132.04 | 102.87 | 37 | 2599 | 13389 | 90612422 |
| Escherichia infection | 130.28 | 102.87 | 38 | 2598 | 15857 | 90609954 |
| Aplastic anaemia | 127.91 | 102.87 | 36 | 2600 | 13233 | 90612578 |
| Mitral valve incompetence | 125.42 | 102.87 | 40 | 2596 | 22484 | 90603327 |
| Anuria | 123.98 | 102.87 | 36 | 2600 | 14782 | 90611029 |
| Tricuspid valve incompetence | 119.66 | 102.87 | 36 | 2600 | 16695 | 90609116 |
| Osteopenia | 108.38 | 102.87 | 36 | 2600 | 22966 | 90602845 |
| Myelodysplastic syndrome | 107.69 | 102.87 | 35 | 2601 | 20868 | 90604943 |
| Pulmonary hypertension | 107.61 | 102.87 | 42 | 2594 | 42481 | 90583330 |
| Hiatus hernia | 104.94 | 102.87 | 36 | 2600 | 25325 | 90600486 |
| Haematuria | 104.55 | 102.87 | 39 | 2597 | 34898 | 90590913 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Jugular vein distension | 73.95 | 64.14 | 12 | 574 | 672 | 42620077 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Lymphatic fistula | 215.69 | 83.04 | 37 | 2945 | 1458 | 110584859 |
| Femoral hernia incarcerated | 215.34 | 83.04 | 37 | 2945 | 1472 | 110584845 |
| Wound infection pseudomonas | 198.03 | 83.04 | 37 | 2945 | 2374 | 110583943 |
| Pancreatic steatosis | 195.16 | 83.04 | 35 | 2947 | 1787 | 110584530 |
| Arterial haemorrhage | 181.05 | 83.04 | 37 | 2945 | 3782 | 110582535 |
| Seroma | 180.40 | 83.04 | 36 | 2946 | 3265 | 110583052 |
| Aortic valve stenosis | 156.93 | 83.04 | 36 | 2946 | 6314 | 110580003 |
| Hepatic cyst | 154.81 | 83.04 | 37 | 2945 | 7746 | 110578571 |
| Haemarthrosis | 151.79 | 83.04 | 36 | 2946 | 7293 | 110579024 |
| Diverticulum intestinal | 149.38 | 83.04 | 39 | 2943 | 11680 | 110574637 |
| Tachyarrhythmia | 147.51 | 83.04 | 36 | 2946 | 8225 | 110578092 |
| Eructation | 147.00 | 83.04 | 40 | 2942 | 14017 | 110572300 |
| Wound dehiscence | 143.71 | 83.04 | 35 | 2947 | 7927 | 110578390 |
| Groin pain | 138.75 | 83.04 | 39 | 2943 | 15389 | 110570928 |
| Faecaloma | 135.50 | 83.04 | 38 | 2944 | 14870 | 110571447 |
| Aortic arteriosclerosis | 132.67 | 83.04 | 35 | 2947 | 10903 | 110575414 |
| Inflammatory marker increased | 132.05 | 83.04 | 37 | 2945 | 14432 | 110571885 |
| Postoperative wound infection | 128.93 | 83.04 | 37 | 2945 | 15716 | 110570601 |
| Mitral valve incompetence | 128.42 | 83.04 | 44 | 2938 | 33285 | 110553032 |
| Cardiogenic shock | 125.76 | 83.04 | 50 | 2932 | 57288 | 110529029 |
| Left ventricular dysfunction | 122.57 | 83.04 | 39 | 2943 | 23454 | 110562863 |
| Cardiovascular disorder | 119.63 | 83.04 | 38 | 2944 | 22722 | 110563595 |
| Escherichia infection | 117.94 | 83.04 | 38 | 2944 | 23778 | 110562539 |
| Osteopenia | 112.28 | 83.04 | 36 | 2946 | 22173 | 110564144 |
| Tricuspid valve incompetence | 109.72 | 83.04 | 36 | 2946 | 23837 | 110562480 |
| Aplastic anaemia | 109.08 | 83.04 | 36 | 2946 | 24272 | 110562045 |
| Anuria | 109.03 | 83.04 | 36 | 2946 | 24305 | 110562012 |
| Joint dislocation | 108.22 | 83.04 | 39 | 2943 | 34151 | 110552166 |
| Hiatus hernia | 104.59 | 83.04 | 36 | 2946 | 27570 | 110558747 |
| Pulmonary hypertension | 100.03 | 83.04 | 42 | 2940 | 55178 | 110531139 |
| Myelodysplastic syndrome | 90.27 | 83.04 | 35 | 2947 | 37449 | 110548868 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C01CX08 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Other cardiac stimulants |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D010726 | Phosphodiesterase Inhibitors |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D058987 | Phosphodiesterase 3 Inhibitors |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
| CHEBI has role | CHEBI:38147 | cardiotonic drug |
| CHEBI has role | CHEBI:50568 | EC 3.1.4.17 (3,5-cyclic-nucleotide phosphodiesterase) inhibitor |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
C01CX Other cardiac stimulants 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Congestive heart failure | indication | 42343007 | DOID:6000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.04 | acidic |
| pKa2 | 11.34 | acidic |
| pKa3 | 4.67 | Basic |
| pKa4 | 4.04 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Troponin C, slow skeletal and cardiac muscles | Cytosolic other | OPENER | Kd | 3.16 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Enzyme | WOMBAT-PK | |||||||
| ATP-sensitive inward rectifier potassium channel 11 | Ion channel | WOMBAT-PK | |||||||
| ATP-sensitive inward rectifier potassium channel 8 | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D04720 | KEGG_DRUG |
| C0246904 | UMLSCUI |
| CHEBI:50567 | CHEBI |
| CHEMBL2051955 | ChEMBL_ID |
| DB00922 | DRUGBANK_ID |
| D000077464 | MESH_DESCRIPTOR_UI |
| 3033825 | PUBCHEM_CID |
| 7020 | INN_ID |
| C6T4514L4E | UNII |
| 73107 | RXNORM |
| 009718 | NDDF |
| 442790008 | SNOMEDCT_US |
| 442795003 | SNOMEDCT_US |
| C6T4514L4E | INXIGHT DRUGS |
Pharmaceutical products:
None