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

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1631 89226-50-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • manidipine dihydrochloride
  • manidipine
  • (+/-)-Manidipine
  • franidipine
  • manidipine hydrochloride
  • manidipine HCl
  • Molecular weight: 610.71
  • Formula: C35H38N4O6
  • CLOGP: 7.02
  • LIPINSKI: 2
  • HAC: 10
  • HDO: 1
  • TPSA: 114.25
  • ALOGS: -5.79
  • ROTB: 12

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.879 Moderate 0.68
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.279 Moderate 0.68
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 4.688 10^-6 cm/s Moderate 0.68
dh-clint Dog hepatocyte intrinsic clearance 84.723 uL/min/10^6 cells Moderate 0.68
dppb Dog plasma protein binding (% unbound) 0.140 % Moderate 0.68
fcs-ppb Fetal calf serum protein binding (% unbound) 0.220 % Moderate 0.68
herg hERG pIC50 5.481 pIC50 Moderate 0.68
hh-clint Human hepatocyte intrinsic clearance 80.724 uL/min/10^6 cells Moderate 0.68
hlm-clint Human liver microsomal intrinsic clearance 279.254 uL/min/mg protein Moderate 0.68
hppb Human plasma protein binding (% unbound) 0.260 % Moderate 0.68
kinase-safety-class ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ZAP70 44
kinase-selectivity-class AXL,BRAF,GRK2,PDK4 4
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.175 Moderate 0.68
mh-clint Mouse hepatocyte intrinsic clearance 161.808 Moderate 0.68
mppb Mouse plasma protein binding (% unbound) 0.170 Moderate 0.68
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 4.786 Moderate 0.68
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 Moderate 0.66
pppb Pig plasma protein binding (% unbound) 0.210 % Moderate 0.68
rh-clint Rat hepatocyte intrinsic clearance 157.761 uL/min/10^6 cells Moderate 0.68
rh-fuinc Rat hepatocyte fraction unbound in incubation 1.060 % Moderate 0.68
rppb Rat plasma protein binding (% unbound) 0.150 % Moderate 0.68
solubility-dd Solubility at pH 7.4 in DMSO 0.541 uM Moderate 0.68

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
Hyponatraemia 66.60 37.66 29 742 133509 90494167
Parkinsonism 48.17 37.66 13 758 14052 90613624
Drug interaction 44.14 37.66 28 743 276425 90351251

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
Trichoglossia 80.73 37.00 13 1053 374 42619895
Drug interaction 70.93 37.00 56 1010 266943 42353326
Hypomagnesaemia 47.58 37.00 20 1046 28468 42591801
Immune-mediated thyroiditis 43.75 37.00 8 1058 491 42619778
Dermatitis bullous 40.83 37.00 13 1053 8443 42611826

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
Drug interaction 116.33 32.31 85 1905 500098 110087211
Hyponatraemia 94.90 32.31 55 1935 217598 110369711
Trichoglossia 74.29 32.31 13 1977 867 110586442
Acute kidney injury 70.99 32.31 71 1919 635359 109951950
Parkinsonism 47.24 32.31 17 1973 22170 110565139
Hypomagnesaemia 45.38 32.31 22 1968 60348 110526961
Immune-mediated thyroiditis 40.08 32.31 8 1982 1088 110586221
Dermatitis bullous 35.70 32.31 13 1977 17516 110569793

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA11 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
ATC C09BB12 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs
amlodipinebarnidipinebenidipinecelecoxibcilnidipineclevidipinefelodipineisradipinelacidipinelercanidipinelevamlodipinenicardipine show all 17 →
C09BB ACE inhibitors and calcium channel blockers 13 drugs
amlodipinebenazeprildelaprilenalaprilfelodipinelercanidipinelisinoprilnitrendipineperindoprilramipriltrandolaprilverapamil show all 13 →

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 6.7 Basic
pKa2 2.87 Basic
pKa3 2.2 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
Cruzipain Enzyme IC50 5.22 CHEMBL

External reference:

IDSource
D01553 KEGG_DRUG
C0065656 UMLSCUI
CHEBI:749150 CHEBI
CHEMBL1085699 ChEMBL_ID
DB09238 DRUGBANK_ID
C054218 MESH_SUPPLEMENTAL_RECORD_UI
11739 IUPHAR_LIGAND_ID
6300 INN_ID
89226-75-5 SECONDARY_CAS_RN
6O4754US88 UNII
4008 PUBCHEM_CID
259487 RXNORM
008164 NDDF
008165 NDDF
765322004 SNOMEDCT_US
765323009 SNOMEDCT_US

Pharmaceutical products:

None