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

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 642 132203-70-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • FRC-8653
  • cilnidipine
  • cinaldipine
  • cinalong
has excitatory & inhibitory action on the Ca+ channels in the rabbit basilar artery; structure given in first source; RN given is for (+-) isomer
  • Molecular weight: 492.53
  • Formula: C27H28N2O7
  • CLOGP: 5.54
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 1
  • TPSA: 117
  • ALOGS: -5.94
  • ROTB: 12

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.623 Moderate 0.71
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.199 Moderate 0.71
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 4.989 10^-6 cm/s Moderate 0.71
dh-clint Dog hepatocyte intrinsic clearance 98.855 uL/min/10^6 cells Moderate 0.71
dppb Dog plasma protein binding (% unbound) 0.250 % Moderate 0.71
fcs-ppb Fetal calf serum protein binding (% unbound) 0.220 % Moderate 0.71
herg hERG pIC50 5.123 pIC50 Moderate 0.71
hh-clint Human hepatocyte intrinsic clearance 115.345 uL/min/10^6 cells Moderate 0.71
hlm-clint Human liver microsomal intrinsic clearance 240.991 uL/min/mg protein Moderate 0.71
hppb Human plasma protein binding (% unbound) 0.380 % Moderate 0.71
kinase-safety-class ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKDC,STK33,TEK,TTK 36
kinase-selectivity-class AXL,BRAF,GRK2,MAPK7,PDK4,STK33,TEK 7
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.333 Moderate 0.71
mh-clint Mouse hepatocyte intrinsic clearance 137.721 Moderate 0.71
mppb Mouse plasma protein binding (% unbound) 0.170 Moderate 0.71
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.999 Moderate 0.71
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 Moderate 0.71
pppb Pig plasma protein binding (% unbound) 0.270 % Moderate 0.71
rh-clint Rat hepatocyte intrinsic clearance 162.930 uL/min/10^6 cells Moderate 0.71
rh-fuinc Rat hepatocyte fraction unbound in incubation 1.610 % Moderate 0.71
rppb Rat plasma protein binding (% unbound) 0.230 % Moderate 0.71
solubility-dd Solubility at pH 7.4 in DMSO 3.412 uM Moderate 0.71

Approvals:

None

FDA Adverse Event Reporting System (Female)

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
Renal impairment 75.33 28.65 35 1327 105386 90521699
Hepatic function abnormal 58.34 28.65 23 1339 46265 90580820
Cardiac failure 42.15 28.65 24 1338 109472 90517613
Platelet count decreased 34.73 28.65 23 1339 136946 90490139
Nephrogenic anaemia 29.74 28.65 7 1355 2459 90624626
Myasthenic syndrome 28.73 28.65 5 1357 387 90626698

FDA Adverse Event Reporting System (Male)

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
Interstitial lung disease 64.76 27.40 44 2190 78418 42540683
Renal impairment 61.95 27.40 49 2185 110179 42508922
Hepatic function abnormal 52.48 27.40 33 2201 51534 42567567
Cerebral infarction 50.51 27.40 27 2207 31142 42587959
Hyperkinetic heart syndrome 48.69 27.40 8 2226 120 42618981
Hyperkalaemia 37.24 27.40 32 2202 80426 42538675
Cardiac vein perforation 35.33 27.40 5 2229 25 42619076
Stress cardiomyopathy 32.44 27.40 10 2224 2775 42616326
Echocardiogram abnormal 30.39 27.40 8 2226 1262 42617839
Hypoxic-ischaemic encephalopathy 29.97 27.40 11 2223 5191 42613910
Protein urine present 28.80 27.40 11 2223 5790 42613311

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
Renal impairment 120.33 25.14 78 3880 188367 110396974
Hepatic function abnormal 107.91 25.14 56 3902 89239 110496102
Cerebral infarction 75.75 25.14 37 3921 51801 110533540
Interstitial lung disease 72.83 25.14 51 3907 139283 110446058
Hyperkalaemia 60.22 25.14 45 3913 135751 110449590
Hyperkinetic heart syndrome 50.57 25.14 8 3950 140 110585201
Platelet count decreased 44.99 25.14 48 3910 230395 110354946
Hyperuricaemia 42.83 25.14 17 3941 14514 110570827
Cerebral haemorrhage 39.17 25.14 26 3932 64942 110520399
Cardiac vein perforation 37.24 25.14 5 3953 25 110585316
Cardiac failure 36.46 25.14 39 3919 187587 110397754
Embolic stroke 32.09 25.14 12 3946 8731 110576610
Stress cardiomyopathy 31.51 25.14 14 3944 15792 110569549
Nephrogenic anaemia 31.29 25.14 10 3948 4567 110580774
Chronic kidney disease 30.95 25.14 24 3934 76267 110509074
Hypoxic-ischaemic encephalopathy 28.36 25.14 11 3947 8836 110576505
Echocardiogram abnormal 27.51 25.14 8 3950 2666 110582675
Dehydration 26.96 25.14 41 3917 279470 110305871
Renal cyst haemorrhage 26.40 25.14 6 3952 755 110584586
Palmar-plantar erythrodysaesthesia syndrome 26.13 25.14 17 3941 41008 110544333
Hyperkinesia 26.13 25.14 8 3950 3176 110582165
Pemphigoid 25.61 25.14 13 3945 19694 110565647

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA14 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:38215 calcium channel blocker

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs
amlodipinebarnidipinebenidipinecelecoxibclevidipinefelodipineisradipinelacidipinelercanidipinelevamlodipinemanidipinenicardipine show all 17 →

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 2.67 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
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel IC50 4.62 CHEMBL
Voltage-dependent N-type calcium channel subunit alpha-1B Ion channel IC50 4.58 CHEMBL
Voltage-dependent N-type calcium channel subunit alpha-1B Ion channel BLOCKER IC50 6.70 IUPHAR

External reference:

IDSource
D01173 KEGG_DRUG
C0378675 UMLSCUI
CHEBI:31399 CHEBI
CHEMBL452076 ChEMBL_ID
DB09232 DRUGBANK_ID
C065927 MESH_SUPPLEMENTAL_RECORD_UI
7767 IUPHAR_LIGAND_ID
6880 INN_ID
97T5AZ1JIP UNII
5282138 PUBCHEM_CID
010899 NDDF
1177123004 SNOMEDCT_US
1179035008 SNOMEDCT_US

Pharmaceutical products:

None