levamlodipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 4099 103129-82-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • levamlodipine malate
  • levamlodipine besylate
  • (S)-amlodipine
  • levamlodipine
  • levoamlodipine
  • l-Amlodipine
used to treat angina and hypertension
  • Molecular weight: 408.88
  • Formula: C20H25ClN2O5
  • CLOGP: 3.43
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 99.88
  • ALOGS: -4.74
  • ROTB: 10

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.817 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 19.011 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 6.871 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 7.447 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 5.810 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 12.550 % High 1
herg hERG pIC50 5.331 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.097 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 6.095 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 7.050 % High 1
kinase-safety-class ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,IGF1R,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 43
kinase-selectivity-class AXL,BRAF,GRK2,PDK4,PIK3CD 5
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 15.066 High 1
mh-clint Mouse hepatocyte intrinsic clearance 27.164 High 1
mppb Mouse plasma protein binding (% unbound) 5.070 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 51.404 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 11.180 % High 1
rh-clint Rat hepatocyte intrinsic clearance 37.325 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 21.090 % High 1
rppb Rat plasma protein binding (% unbound) 7.730 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 48.529 uM High 1

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood urea increased 44.90 33.58 16 724 54941 110533618
Neutrophil count increased 43.77 33.58 14 726 34638 110553921
Lymphocyte count decreased 40.54 33.58 15 725 57228 110531331
Incision site pain 33.73 33.58 7 733 3128 110585431

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA17 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.0 Basic
pKa2 1.55 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-gated L-type calcium channel Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
736178-83-9 SECONDARY_CAS_RN
150566-71-5 SECONDARY_CAS_RN
D08941 KEGG_DRUG
4039729 VANDF
C2717539 UMLSCUI
6UB PDB_CHEM_ID
CHEMBL2111097 ChEMBL_ID
CHEMBL2107350 ChEMBL_ID
DB09237 DRUGBANK_ID
C542574 MESH_SUPPLEMENTAL_RECORD_UI
C000711385 MESH_SUPPLEMENTAL_RECORD_UI
8835 INN_ID
0P6NLP6806 UNII
9822750 PUBCHEM_CID
2376944 RXNORM
360548 MMSL
d08466 MMSL
018248 NDDF
1217308000 SNOMEDCT_US
1217324004 SNOMEDCT_US
1217325003 SNOMEDCT_US

Pharmaceutical products:

None